Article

Efficacy and Safety of White Willow Bark ( Salix alba ) Extracts: Willow Bark Extract Efficacy and Safety

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Abstract

Willow bark extract has been used for thousands of years as an anti-inflammatory, antipyretic, and analgesic. In spite of its long history of use, relatively few human and animal studies have been published that confirm anecdotal observations. A small number of clinical studies have been conducted that support the use of willow bark extracts in chronic lower back and joint pain and osteoarthritis. Willow bark extracts also are widely used in sports performance and weight loss products presumably because of anti-inflammatory and analgesic activities, although no human studies have been published that specifically and directly document beneficial effects. In recent years, various in vitro and animal studies have demonstrated that the anti-inflammatory activity of willow bark extract is associated with down regulation of the inflammatory mediators tumor necrosis factor-α and nuclear factor-kappa B. Although willow bark extracts are generally standardized to salicin, other ingredients in the extracts including other salicylates as well as polyphenols, and flavonoids may also play prominent roles in the therapeutic actions. Adverse effects appear to be minimal as compared to non-steroidal anti-inflammatory drugs including aspirin. The primary cause for concern may relate to allergic reactions in salicylate-sensitive individuals. Copyright © 2015 John Wiley & Sons, Ltd. Copyright © 2015 John Wiley & Sons, Ltd.

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... alternaria, A. niger, M. hiemalis, P. notatum and S. commune) with remarkable effect [14]. Analysis of aqueous extracts of willow bark has shown the presence of at least 11 related salicylate compounds including salicin, saligenin, salicylic acid, isosalicin, salidroside, picein, triandrin, salicoylsalicin, salicortin, isosalipurpuroside and salipurpuroside (Scheme 2) [15]. ...
... alternaria, A. niger, M. hiemalis, P. notatum and S. commune) with remarkable effect [14]. Analysis of aqueous extracts of willow bark has shown the presence of at least 11 related salicylate compounds including salicin, saligenin, salicylic acid, isosalicin, salidroside, picein, triandrin, salicoylsalicin, salicortin, isosalipurpuroside and salipurpuroside (Scheme 2) [15]. Silver compounds are known antimicrobial agents [9,16]. ...
... Molecular formulae of the main components of willow bark extract[15]. Scheme 2. Molecular formulae of the main components of willow bark extract[15]. ...
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Eucalyptus leaves (ELE) and willow bark (WBE) extracts were utilized towards the formation of silver nanoparticles (AgNPs(ELE), AgNPs(WBE)). AgNPs(ELE) and AgNPs(WBE) were dispersed in polymer hydrogels to create pHEMA@AgNPs(ELE)_2 and pHEMA@AgNPs(WBE)_2 using hydroxyethyl-methacrylate (HEMA). The materials were characterized in a solid state by X-ray fluorescence (XRF) spectroscopy, X-ray powder diffraction analysis (XRPD), thermogravimetric differential thermal analysis (TG-DTA), differential scanning calorimetry (DTG/DSC) and attenuated total reflection spectroscopy (ATR-FTIR) and ultraviolet visible (UV-vis) spectroscopy in solution. The antimicrobial potential of the materials was investigated against the Gram-negative bacterial strain Pseudomonas aeruginosa (P. aeruginosa) and the Gram-positive bacterial strain of the genus Staphylococcus epidermidis (S. epidermidis) and Staphylococcus aureus (S. aureus), which are involved in microbial keratitis. The percentage of bacterial viability of P. aeruginosa and S. epidermidis upon their incubation over the pHEMA@AgNPs(ELE)_2 discs is interestingly low (28.3 and 6.8% respectively), while the inhibition zones (IZ) formed are 12.3 ± 1.7 and 13.2 ± 1.2 mm, respectively. No in vitro toxicity of this material towards human corneal epithelial cells (HCEC) was detected. Despite its low performance against S. aureus, pHEMA@AgNPs(ELE)_2 could be an efficient candidate towards the development of contact lenses that reduces microbial infection risk.
... Subsequent structure elucidation revealed five salicylates relevant for bioactive effects in different potencies. Moreover, some studies discuss positive bioactive effects of willow bark in other fields, e. g. in the field of anticarcinogenic activities [14,15] and recently also in the context of SARS-CoV-2 due to anti-inflammatory effects [16]. Thereby, differences between Salix species in terms of bioactive potency have been observed. ...
... Salicin was detected in ZB29 as well as 91/02, but not in ZA20. ZB29 also differed from the other two genotypes in containing neochlorogenic acid (6), chlorogenic acid (13), rosin (15), and tremulacin (25), while ampelopsin (17) was not detected. In turn, S. triandra ZA20 was found to contain salidroside (3), which was not found in genotypes ZB29 and 91/02. ...
Article
Due to their content of phenolic compounds, willow bark preparations are used as an herbal remedy. The large diversity of phenolic secondary metabolites in Salix still provides a resource for the identification of bioactive compounds in particular species, including species not yet in focus from a phytopharmaceutical perspective. The present study describes the bark phenolic profile of 13 Salix species analyzed by HPLC-MS: Salix alba, Salix babylonica, Salix daphnoides, Salix fragilis, Salix hastata, Salix myrsinifolia, Salix pentandra, Salix purpurea, Salix repens (including subspecies S. repens ssp. arenaria and S. repens ssp. repens), Salix rosmarinifolia, Salix sachalinensis, Salix triandra and Salix viminalis. The analyzed profiles comprised the chemical groups of salicylates, flavonoids, procyanidins, phenolic acid derivatives, and some unclassified phenolics. Particular compounds were detected in species where they have not been previously reported. Apart from interspecific diversity, qualitative variability within species was observed as certain components were detected only in some of the analyzed genotypes. The knowledge on specific phenolic profiles of species and genotypes is the basis for the selection of suitable willow bark material with certain desired bioactive properties. Furthermore, the high inter- and intraspecific variability points out the necessity for product standardization of willow bark raw material.
... Other species of Salix, such as S. pentandra extracts, were reported to suppress cytokines (L-6, IL-1β, IL-10), and prostaglandin E2 [50]. The anti-inflammatory properties of white willow bark extracts are mainly due to the downregulation of the pro-inflammatory effects of NF-κB, COX-2, and TNF-α [51]. In this study, our hypothesis is that the anti-inflammatory activity of the SA-ME was primarily due to soluble compounds in ethanol. ...
... As described previously [49,51], monocultures of Caco-2 cells were harvested with Trypsin-EDTA and seeded on the apical chamber of 12-well ThinCert ® inserts (0.4 m PET pore membrane, Greiner Bio-One, Frickenhausen, Germany) to reach a final density of 3 × 105 cells/cm 2 . The cells were co-cultured for 19-21 days in a humidified incubator with a 5% CO 2 /95% air environment, with the apical and basolateral media changed every 2-3 days. ...
Article
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White willow (Salix alba) is a medicinal plant used in folk medicine. In this study, aqueous and ethanolic willow bark extracts were obtained via ultrasonic-assisted extraction (UAE) and microwave-assisted extraction (MAE), and analyzed regarding their phytochemical (total phenolics, phenolic acids, flavonoids, and tannins) content and in vitro biological properties (antibacterial and antifungal activity, acetylcholinesterase AChE inhibitory activity and anti-inflammatory effects). The highest phenolic, tannin, and flavonoid contents were found for willow bark extracts obtained via microwave-assisted extraction using ethanol as a solvent (SA-ME). The polyphenol load of all MAE and UAE extracts was higher when conventional solid-liquid extraction was applied (ρ < 0.05). The antioxidant capacities were stronger for microwave-assisted ethanolic extracts, with the lowest IC 50 values of 12 µg/mL for DPPH • and a value of 16 µg/mL for ABTS•+, whereas the conventional extraction had the highest IC 50 values (22 µg/mL and 28 µg/mL, respectively). Willow bark extract showed antibacterial activity against Gram-positive bacteria S. aureus and P. aeruginosa. AChE inhibitory activity was dependent on the extraction method and solvent used, and the highest inhibition among samples was observed for SAME. Taken altogether, our findings suggest that willow (Salix alba) bark extract obtained via ethanolic microwave-assisted extraction is a phytochemical-rich resource with in vitro, anti-inflammatory, and AchE inhibitory properties and, therefore, potential multiple medicinal end-uses.
... In the 1900s, the active compound of willow, salicin, was modified to create aspirin. Because salicin is very similar to the active compound in aspirin, willow bark powder or extract could potentially be substituted for aspirin to relieve mild pain 21 . This notion has not been thoroughly studied, but researchers found that willow bark extract can treat lower back pains, joint pains associated with arthritis, fever, and general body aches 20,21 . ...
... Because salicin is very similar to the active compound in aspirin, willow bark powder or extract could potentially be substituted for aspirin to relieve mild pain 21 . This notion has not been thoroughly studied, but researchers found that willow bark extract can treat lower back pains, joint pains associated with arthritis, fever, and general body aches 20,21 . ...
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Humans have used plants to treat illnesses since prehistoric times. Though modern Western medicine consists of pills and injections rather than leaves and flowers, the plant-derived compounds in many medications show evidence of this history. This project aims to connect medicinal plants’ traditional and historical uses with the findings of modern scientists. Medicinal Plants of Iowa provides Iowa residents who are interested in herbal remedies with a resource that describes the healing properties of plants commonly found in the state. As well as healing properties, a description of each plant’s appearance and preferred habitat type is provided, allowing users to identify plants more easily. The book uses jargon-free, comprehensible language to describe the outcomes of clinical trials involving medicinal plants and compare these findings to the plants’ uses in traditional medicine. Traditional medicine practices were built through generations of experimentation but are often intertwined with religion and ritual. While this can paint traditional medicine in an unscientific light, it is evident that these practices have inspired contemporary scientific research and have thus contributed to modern medicine as we know it.
... Among the examples of elite plant material of global interest is the white willow. The bark of Salix alba has been traditionally used as an anti inflammatory, antipyretic, and analgesic (Shara et al., 2015). Salicin, a predecessor of salicylic acid, has been extracted from white willow bark (Pincock, 2005), whose extracts have been shown to act as mediators of the anti inflammatory metabolites factor α and nuclear factor-kappa B present in tumor necrosis processes (Shara et al., 2015). ...
... The bark of Salix alba has been traditionally used as an anti inflammatory, antipyretic, and analgesic (Shara et al., 2015). Salicin, a predecessor of salicylic acid, has been extracted from white willow bark (Pincock, 2005), whose extracts have been shown to act as mediators of the anti inflammatory metabolites factor α and nuclear factor-kappa B present in tumor necrosis processes (Shara et al., 2015). The limited reproductive potential of the white willow constraints large scale production of salicin. ...
Book
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Biotechnology is a broad interdisciplinary branch of biological sciences that consists of any technological application that uses biological systems and living organisms or their derivatives for the creation or modification of products or processes for specific uses. Within these organisms they may or may not be genetically modified. The bases of this interdisciplinary are biology, engineering, physics, chemistry, and biomedicine. Over the years the field of this science has shown relevance in pharmacology, medicine, food science, the treatment of solid, liquid and gaseous waste, industry, livestock and agriculture. Biotechnology is present day by day in our daily lives, in the foods that we consume are sometimes supplemented with compounds, enzymes and proteins that help improve the taste, texture or general properties of food. Biotechnology has also presented great impact on the generation of raw materials to minimize the use of fossil fuels. Through different crop optimization systems and genetic manipulation, it has been possible to improve the properties of biomass in crops or biological models that are used as raw material to obtain fatty acids and alcohols. During the year 2020, the COVID-19 pandemic was experienced worldwide, the participation of biotechnologists for the synthesis of new vaccines or establishing methodologies for rapid detection of the virus, was decisive to control the spread of the virus among the world population. This book describes what has been the biotechnological advance in selected topics related to genetic improvement of crops, enzyme biotechnology, plant tissue culture, metabolites extraction, advances in the generation of biofuels and generation of vaccines. The goal of this book is to emphasize the importance of biotechnology today. The editors hope that this book is to your liking and helps you in the different disciplines in which they are developed.
... In "Das Seelenleben der Tiere" (Wohlleben 2016) (Wohlleben 2015: 16), was Shara & Stohs (2015) und Schmid et al. (2001) bestätigen, und die Birke Betulin (Wohlleben 2015: 164, 165), was unter anderem Šiman et al. (2015) nachweisen. ...
... unter Beleg 65 auf ein Paper vonLi et al. (2008), welches zumindest bestätigt, dass nach mehrstündigem Waldaufenthalt die Konzentration an krebshemmenden Proteinen und Zellen im Blut von Proband:innen für mehrere Tage erhöht war.Hansen et al. (2017) fassen zudem viel Literatur zur positiven Auswirkung von Wäldern auf die Gesundheit von Menschen zusammen, welche in einigen Fällen auch direkt von Phytonziden als treibende Kraft für diese Wirkung spricht.Nicht unbedingt über die Atemluft aufgenommen, aber beispielsweise als Tee, soll Salicin (aus Weidenrinde, siehe oben) beim Menschen gegen Kopfschmerzen und Fieber wirken(Wohlleben 2015: 17). Eine Wirkung, dieShara & Stohs (2015) undSchmid et al. (2001) bestätigen.Betulin aus der Rinde der Birke (siehe oben) wiederum soll antibakterielle und antivirale Eigenschaften aufweisen, was in der Medizin und in Hautpflegeprodukten genutzt werden soll(Wohlleben 2015: 165). Dies soll auch die Studie von Ebeling et al. (2014) beweisen, die in "Das geheime Leben der Bäume" (Wohlleben 2015) unter dem Beleg Nummer 47 zu finden ist. ...
Thesis
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Im Kontext der Problematik von Fehlinformationen in der populärwissenschaftlichen Literatur widmet sich diese Arbeit in einer Fallstudie drei häufig verkauften Büchern Peter Wohllebens. Untersucht wird, wie nah diese Werke sich am aktuellen Stand der Forschung orientieren und wie gut die getätigten Aussagen nachvollziehbar sind. Für die Untersuchung wurde der Inhalt der Bücher codiert und die resultierenden 8899 Codiereinheiten quantitativ und qualitativ-vergleichend analysiert. Ergänzt wurde dies durch die qualitativ-vergleichende Analyse von drei Schwerpunktthemen. Aus den Ergebnissen wird geschlussfolgert, dass Wohllebens Nähe zum wissenschaftlichen Diskurs unter Einschränkungen ausreichend und die Nachvollziehbarkeit seiner Aussagen mangelhaft ist. Basierend auf diesen Erkenntnissen werden mögliche Maßnahmen und Handlungsfelder für eine Erhöhung der wissenschaftlichen Qualität populärwissenschaftlicher Werke diskutiert. Es werden weitere potentielle Forschungsmöglichkeiten für ein besseres Verständnis der Situation in den Populärwissenschaften identifiziert und vorgeschlagen. // English Title: "Sustainable Fairytale Forest? A contribution to the discussion on standards for popular science publications based on a case study on the factual content of selected works of Peter Wohlleben"
... The bark extract also contains phenolic and flavonoid compounds with antioxidant activity [20][21][22]. In addition to antioxidant and anti-inflammatory properties, willow bark extract is used in weight loss supplements [23], and for its hypocholesterolemic activity [24,25]. Few data are available on the use of Sa in poultry species, despite acetylsalicylic acid and sodium salicylate being considered safe for poultry and used in avian medicine [26]. ...
... Accordingly, Pozniak and a co-worker found that the BW gain decreased in broilers when the feed was supplemented with 0.04% of acetylsalicylic acid; this effect is presumably related to anti-inflammatory and analgesic activities of the phytocomplex [26]. However, a paucity of controlled clinical trials has been performed to evaluate the efficacy of willow bark extract and the use in association with other extracts hampers the evaluation of its direct efficacy on weight loss [23]. ...
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This study was conducted to evaluate the safety and the beneficial effects of dietary supplementation with Boswellia serrata (Bs) and Salix alba (Sa) in Leghorn hens during the critical pre-laying and laying phases. A total of 120 pullets, 17 weeks of age, were assigned to two groups (Control—C; Treated—T, n = 60 each). For 12 weeks, the T group received a diet supplemented with 0.3% of dry extracts of Bs (5%) and Sa (5%). The study lasted 19 weeks. Productive performance, serum analytes, H/L ratio, IgA and anti-IBV antibodies were investigated. Water intake was significantly higher, while body and egg weight was significantly lower for the T group (p < 0.05). No other differences were detected in performance parameters, serum analytes, IgA and H/L ratio excluding t0, with a significantly (p < 0.05) higher H/R ratio and higher titers of anti-IBV antibody for the T group. Overall, the data obtained in this study show that the supplementation with Bs and Sa was safe and resulted in an increase in water consumption, a decrease in egg weight, and a sedative effect in the hens. In the future, it would be interesting to test this supplement in hens reared on intensive farms.
... Ivanaga et al. (27) discussed that in patients with type 2 diabetes mellitus, the treatment of residual pockets (with PD ≥5 mm and BOP) with antimicrobial photodynamic therapy with 100 mg/L curcumin solution and LED irradiation as adjunctive therapy to scaling and root planing, may yield short-term (three months) clinical benefits regarding clinical attachment gain. 42 Sparabombe et al. (28) r eported that the use of a polyherbal mouthwash (Propolis resin extract, Plantago lanceolata, Salvia officinalis leaves extract, and 1.75% essential oil) in patients with moderate or severe periodontitis was safe and effective for BOP and PI after 3 months, in comparison with the control group; however, there was no significant difference between the two groups regarding PD and clinical attachment level. ...
... Microbial control in turn reduces the inflammatory response, which in turn decreases the plasma leakage in saliva through gingival crevicular fluid; this statement could be supported by the overall reduction in total salivary protein levels. (16) Further investigations: Several studies have reported anti-inflammatory effects of cocoa flavonoids,(36) thyme, (37) Artemisia annua, (38) Inonotus obliquus (chaga mushroom), (39) leaf extract of Ananas comosus, (40) Thykamine extracts from spinach (41) and White Willow Bark (Salix alba) (42) on different parts of the body. An analysis ...
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Background and Aim: The most common etiology of gingivitis is accumulation of bacterial plaque. The complete removal of microbial plaques by mechanical procedures is not possible in some situations, for example the aged and disabled patients, might not be capable of removing the bacterial plaques properly. And also chemical mouthwashes have some adverse effects. Therefore, finding a new treatment approach would be helpful. Global focus on the use of herbal medicine in the treatment of different health conditions has been rising. Present study aimed at searching and gathering scientific evidence of medicinal herbs to treat gingivitis and periodontitis. Materials and Methods: This article is a review of an electronic search of the literature which was conducted mostly through PubMed, Scopus, Google Scholar, and Wiley online library databases. Studies were considered for inclusion if they evaluated medicinal herbs affecting gingival and periodontal inflammation or periodontal pathogens.197 full text article were evaluated and finally, based on the inclusion criteria 22 articles were selected. Results: There are various medical herbs with antibacterial and anti-inflammatory properties, which can significantly reduce gingival and periodontal inflammation, bleeding on probing (BOP), plaque index (PI), probing depth (PD) and levels of major periodontal pathogens and promote clinical attachment level (CAL) gain. Conclusion: Introduced herbal products could be an efficient and safe alternative to chemical products.
... (El-Shemy et al., 2007;Ward et al., 2020). Willow extracts can also be used to relieve pain, inflammation, and fever in a wide variety of conditions with minor adverse effects (Chrubasik et al., 2000;Vlachojannis et al., 2009;Shara and Stohs, 2015). As only mild cytotoxicity has been discovered in willow bark extracts, willows are a promising biomass for various health applications (Ramos et al., 2019). ...
... However, extracts containing a mixture of willow compounds could also have synergistic effects. Similar observations were made by Shara and Stohs (2015), who concluded that the typical effective dosage of aspirin is twice that of salicin needed in willow bark extract, probably because of the presence of beneficial polyphenols and flavonoids in the bark extract. ...
Article
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Earlier studies have shown that the bark of Salix L. species (Salicaceae family) is rich in extractives, such as diverse bioactive phenolic compounds. However, we lack knowledge on the bioactive properties of the bark of willow species and clones adapted to the harsh climate conditions of the cool temperate zone. Therefore, the present study aimed to obtain information on the functional profiles of northern willow clones for the use of value-added bioactive solutions. Of the 16 willow clones studied here, 12 were examples of widely distributed native Finnish willow species, including dark-leaved willow ( S. myrsinifolia Salisb.) and tea-leaved willow ( S. phylicifolia L.) (3 + 4 clones, respectively) and their natural and artificial hybrids (3 + 2 clones, respectively). The four remaining clones were commercial willow varieties from the Swedish willow breeding program. Hot water extraction of bark under mild conditions was carried out. Bioactivity assays were used to screen antiviral, antibacterial, antifungal, yeasticidal, and antioxidant activities, as well as the total phenolic content of the extracts. Additionally, we introduce a fast and less labor-intensive steam-debarking method for Salix spp. feedstocks. Clonal variation was observed in the antioxidant properties of the bark extracts of the 16 Salix spp. clones. High antiviral activity against a non-enveloped enterovirus, coxsackievirus A9, was found, with no marked differences in efficacy between the native clones. All the clones also showed antibacterial activity against Staphylococcus aureus and Escherichia coli , whereas no antifungal ( Aspergillus brasiliensis ) or yeasticidal ( Candida albicans ) efficacy was detected. When grouping the clone extract results into Salix myrsinifolia , Salix phylicifolia , native hybrid, artificial hybrid, and commercial clones, there was a significant difference in the activities between S. phylicifolia clone extracts and commercial clone extracts in the favor of S. phylicifolia in the antibacterial and antioxidant tests. In some antioxidant tests, S. phylicifolia clone extracts were also significantly more active than artificial clone extracts. Additionally, S. myrsinifolia clone extracts showed significantly higher activities in some antioxidant tests than commercial clone extracts and artificial clone extracts. Nevertheless, the bark extracts of native Finnish willow clones showed high bioactivity. The obtained knowledge paves the way towards developing high value-added biochemicals and other functional solutions based on willow biorefinery approaches.
... Salix cortex is also used in dietary supplements, e.g., for weight reduction and to enhance performance in sports (Matyjaszczyk and Schumann, 2018). Despite its long history of use, so far only little data is available on the toxicity or potential adverse effects of Salix cortex preparations (Shara and Stohs, 2015). Based on a limited number of studies, one safety report by Shara and Stohs (2015) recommended that people who 1) are allergic to aspirin, 2) suffer from pathological conditions such as gastritis, stomach ulcers, diabetes, asthma, or hemophilia; or 3) are under anticoagulant-drug therapy, as well as beta-blockers, diuretics, and non-steroidal anti-inflammatory drugs (NSAIDs), may avoid Salix cortex. ...
... Despite its long history of use, so far only little data is available on the toxicity or potential adverse effects of Salix cortex preparations (Shara and Stohs, 2015). Based on a limited number of studies, one safety report by Shara and Stohs (2015) recommended that people who 1) are allergic to aspirin, 2) suffer from pathological conditions such as gastritis, stomach ulcers, diabetes, asthma, or hemophilia; or 3) are under anticoagulant-drug therapy, as well as beta-blockers, diuretics, and non-steroidal anti-inflammatory drugs (NSAIDs), may avoid Salix cortex. ...
Article
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Herbal preparations of willow bark (Salix cortex) are available in many countries as non-prescription medicines for pain and inflammation, and also as dietary supplements. Currently only little information on toxicity and drug interaction potential of the extracts is available. This study now evaluated the effects of two Salix cortex extracts on human hepatocyte-like HepaRG cells, in view of clinically relevant CYP450 enzyme activity modulation, cytotoxicity and production of reactive oxygen species (ROS). Drug metabolism via the CYP450 enzyme system is considered an important parameter for the occurrence of drug-drug interactions, which can lead to toxicity, decreased pharmacological activity, and adverse drug reactions. We evaluated two different bark extracts standardized to 10 mg/ml phenolic content. Herein, extract S6 (S. pentandra, containing 8.15 mg/ml total salicylates and 0.08 mg/ml salicin) and extract B (industrial reference, containing 5.35 mg/ml total salicylates and 2.26 mg/ml salicin) were tested. Both Salix cortex extracts showed no relevant reduction in cell viability or increase in ROS production in hepatocyte-like HepaRG cells. However, they reduced CYP1A2 and CYP3A4 enzyme activity after 48 h at ≥25 μg/ml, this was statistically significant only for S6. CYP2C19 activity inhibition (0.5 h) was also observed at ≥25 μg/ml, mRNA expression inhibition by 48 h treatment with S6 at 25 μg/ml. In conclusion, at higher concentrations, the tested Salix cortex extracts showed a drug interaction potential, but with different potency. Given the high prevalence of polypharmacy, particularly in the elderly with chronic pain, further systematic studies of Salix species of medical interest should be conducted in the future to more accurately determine the risk of potential drug interactions.
... On s'est ainsi rendu compte qu'en empêchant le corps de métaboliser naturellement son « aspirine naturelle », l'acide salicylique, la molécule de synthèse (acide acétylsalicylique) était certes un antidouleur probant, mais qu'elle présentait une action trop ciblée qui provoquait chez les malades qui en absorbaient de fortes doses des problèmes hémorragiques et digestifs. Ces vingt dernières années, plusieurs études ont permis de mieux comprendre l'action du principe actif : non seulement la molécule de salicyline est métabolisée de manière bien différente que les produits de synthèse que sont l'Aspirine ou le paracétamol, mais de plus, elle rentre en synergie avec une multitude d'autres composés naturels de la plante, notamment des flavonoïdes (Williamson, 2001 ;Khayyal et al., 2005 ;Shara & Stohs, 2015) et des polyphénols (Nahtstedt et al., 2007). Grâce à cela, les effets antidouleur, anti-inflammatoire et renforçateur du système immunitaire sont plus efficaces sur le long terme (Schmid et al., 2001). ...
Book
En marge de la médecine moderne, femmes et hommes du monde entier et de toutes les cultures cherchent à retrouver la santé par des moyens «naturels», en particulier par des traitements à base de végétaux. Or, les plantes n’ayant pas développé leurs molécules à l’intention d’ Homo sapiens , pourquoi sommes-nous si réceptifs à leurs principes actifs ? Ainsi débute cet étonnant récit sur le pouvoir des plantes et la volonté des humains à l’utiliser pour le bien de chacune et chacun. Autour de l’écologue Blaise Mulhauser, un groupe interdisciplinaire de spécialistes en biologie, médecine, ethnobotanique, anthropologie de la nature et anthropologie de l’alimentation reprend l’histoire des plantes soignantes là où la culture occidentale du 19<sup>e</sup> siècle l’avait abandonnée, à la frontière de l’intime, du rapport au corps, au moi et aux autres. Construit en trois parties, le livre traite d’abord de la raison d’être des substances actives des plantes pour elles-mêmes, avant d’aborder les sources de la connaissance phytothérapeutique dans les sociétés de peuples dits « autochtones » et en Occident. La dernière partie met en exergue le désir des individus à retrouver la maîtrise de leur santé (automédication par les plantes, alicaments, etc.) jusqu’à l’arrivée de la pandémie de Covid-19, perçue comme un point de basculement.
... Tanto en la región mediterránea como en algunas regiones de América, S. alba ha sido utilizado para tratar el dolor y la fiebre debido a sus efectos antipiréticos, analgésicos y antinflamatorios. 86 Su principal componente bioactivo es la salicina, un profármaco de varios derivados del salicilato. Contiene también otros compuestos como flavonoides, polifenoles y proantocianidinas. ...
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La osteoartrosis (OA) es la enfermedad reumática más frecuente y suele resultar en discapa-cidad. Su tratamiento debe ser integral y contemplar diversos aspectos. Sin embargo, el uso crónico de medi-camentos antinflamatorios se asocia con reacciones adversas graves de tipo gastrointestinal, cardiovascular, hematológico y renal. Hace siglos que las plantas medicinales se utilizan en el manejo de esta enfermedad. Ob-jetivo. El objetivo de este estudio fue realizar una revisión sistemática de la evidencia publicada de 13 plantas, cuyo uso en OA está reportado. Material y métodos. La estrategia de búsqueda incluyó los siguientes criterios: documentos en inglés y español, textos completos, estudios en humanos, guías clínicas, revisiones sistemáticas, metanálisis, estudios clínicos aleatorizados, estudios observacionales/ epidemiológicos/ económicos, revisiones, consensos. Se enfatizó especialmente en el mecanismo de acción farmacológico que pudiera justificar el uso, así como fundamentar la eficacia clínica. La evidencia obtenida se seleccionó mediante preguntas de trabajo y nivel de evidencia. Resultados. Se encontraron 734 artículos; se seleccionaron 346 artículos para su análisis; de éstos, 131 tuvieron utilidad por su nivel de evidencia. Entre los mecanismos de acción encontrados de las plantas investigadas se encuentra la inhibición de citocinas proinflamatorias, disminución de la señalización de TNF-α y NF-κB, reducción de la osteoclastogénesis, incremento de la diferenciación de los osteoclastos, descenso de la actividad de ciclooxigenasa 2 y de la síntesis de prostaglandinas. Conclusiones. Se concluye que las diversas plantas estudiadas tienen mecanismos de acción que apoyan su uso en el tratamiento de la OA y poseen diversos grados de efectividad demostrada.
... Salix alba L., called white willow, is found in various regions, including Egypt, Greece, China, Europe, North America, South America and the Caribbean regions. Salix alba L. bark has been used for over 2000 years to treat pain, inflammation, or fever such as joint or knee pain, acute back pain, osteoarthritis, headache, menstrual cramps, tendonitis and flu symptoms [16]. ...
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Objective: Dark circles in the infraorbital area are a common cosmetic concern among individuals because they exhibit fatigue and are undesirable across all ages. Of the dark circle etiologies, blood stasis by poor vascular integrity can cause darkening of the lower eyelid skin, which might be alleviated by reduced endothelial permeability. In this study, we investigated the effects of Salix alba bark extract (SABE) on the synthesis of hyaluronic acid (HA) in fibroblasts and vascular integrity protection from inflammatory cytokine. We also performed a clinical trial investigating the effect of SABE on dark circles. Methods: To confirm the effect of SABE on HA synthesis in human dermal fibroblasts (HDF), we performed ELISA and real-time PCR. We investigated interaction HDF-secreted substance with vascular integrity, and human dermal microvascular endothelial cells (HMEC-1) were treated with conditioned medium (CM) from HDF treated with or without SABE. Subsequently, we conducted a clinical study on 29 subjects by having them apply SABE containing cream for 8 weeks. Results: SABE treatment increased HA synthesis and regulated HMW-HA related gene expressions in HDF. CM from SABE-treated HDF alleviated endothelial permeability and led to improved vascular integrity in HMEC-1 cells. Treatment with the cream containing 2% SABE for 8 weeks improved the parameters measuring dark circles, skin microcirculation, and elasticity. Conclusion: Our results showed that SABE could protect against dark circles in vitro, and that topical treatment of SABE improved the clinical indexes of dark circles in a clinical study. Therefore, SABE can be used as an active ingredient for improving dark circles.
... Many ancient civilizations used extracts of willow bark and willow leaf because of their analgesic, antipyretic, and anti-inflammatory properties 19,20 . Many studies have documented the presence of bioactive secondary compounds, such as polyphenols, terpenoids, and most importantly, salicylate compounds, in these plants [21][22][23][24][25] , which play a critical role not only as a part of their defense mechanisms and signaling molecules, but also as therapeutic agents (especially salicin) 26,27 . Plants synthesize salicylic acid (SA) through two pathways: the isochorismate pathway (IC) and the phenylalanine ammonia-lyase (PAL) pathway 28 . ...
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Finding innovative eco-friendly agents for pest control may be aided by investigating the plant-derived extracts’ properties on economic pests. Therefore, the insecticidal, behavioral, biological and biochemical effects of Magnolia grandiflora (Magnoliaceae) leaf water and methanol extracts, Schinus terebinthifolius (Anacardiaceae) wood methanol extract, and Salix babylonica (Salicaceae) leaf methanol extract in comparison with a reference insecticide novaluron against S. littoralis were evaluated. The extracts were analyzed by High-Performance Liquid Chromatography (HPLC). The most abundant phenolic compounds were 4-hydroxybenzoic acid (7.16 mg/mL) and ferulic acid (6.34 mg/mL) in M. grandiflora leaf water extract; catechol (13.05 mg/mL), ferulic acid (11.87 mg/mL), and chlorogenic acid (10.33 mg/mL) in M. grandiflora leaf methanol extract; ferulic acid (14.81 mg/mL), caffeic acid (5.61 mg/mL), and gallic acid (5.07 mg/mL) In the S. terebinthifolius extract; cinnamic acid (11.36 mg/mL), and protocatechuic acid (10.33 mg/mL) In the methanol extract from S. babylonica extract. S. terebinthifolius extract had a highly toxic effect against second larvae after 96 h and eggs with LC50 values of 0.89 and 0.94 mg/L, respectively. Despite M. grandiflora extracts didn’t show any toxicity against S. littoralis stages, they had an attractant effect on fourth- and second larvae, with feeding deterrence values of − 2.7% and − 6.7%, respectively, at 10 mg/L. S. terebinthifolius extract significantly reduced the percentage of pupation, adult emergence, hatchability, and fecundity, with values of 60.2%, 56.7%, 35.3%, and 105.4 eggs/female, respectively. Novaluron and S. terebinthifolius extract drastically inhibited the activities of α-amylase and total proteases to 1.16 and 0.52, and 1.47 and 0.65 ΔOD/mg protein/min, respectively. In the semi-field experiment, the residual toxicity of tested extracts on S. littoralis gradually decreased over time compared to novaluron. These findings indicate that extract from S. terebinthifolius is a promising insecticidal agent against S. littoralis.
... Điều trị chủ yếu nhằm lưu thông khí huyết ở kinh lạc để đưa tà khí ra ngoài và bồi bổ chính khí chống lại tà khí. Bách Niên Kiện (BNK) thành phần gồm vỏ Liễu trắng, cây Móng quỷ, Hy thiêm,cao Lá chay là các loại thảo dược trong thành phần hóa học có chứa các hoạt chất có tác dụng giảm đau, chống viêm... và có tác dụng tốt trong điều trị bệnh lý về khớp 6,8 . Bách Niên Kiện cũng đã được thử an toàn độc tính cấp và độc tính bán trường diễn trên động vật thực nghiệm, tuy nhiên chưa có nghiên cứu đánh giá tác dụng của sản phẩm trong điều trị THK vì vậy chúng tôi thực hiện nghiên cứu đề tài này với 2 mục tiêu sau: Chẩn đoán xác định khi có yếu tố 1, 2 hoặc 1, 3, 5, 6 hoặc 1, 4, 5, 6. ...
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Mục tiêu: Đánh giá tác dụng hỗ trợ của viên nén Bách niên kiện trên bệnh nhân thoái hóa khớp gối nguyên phát và theo dõi tác dụng không mong muốn. Phương pháp: Tiến cứu, can thiệp lâm sàng, so sánh trước và sau điều trị trên 60 bệnh nhân chia thành hai nhóm. Kết quả: sau 30 ngày điều trị nhóm NC điểm VAS từ 4,53±1,36 xuống 1,50±1,14 và chỉ số WOMAC từ 44,03±10,60 xuống 23,13±8,99, giảm tốt hơn nhóm ĐC, sự khác biệt ó ý nghĩa thống kê (p < 0,05). Kết luận: Bách niên kiện có tác dụng giảm đau, tăng tầm vận động khớp, cải thiện chức năng khớp gối và không có tác dụng không mong muốn.
... Plants have the ability to produce an infinite number of these phytochemicals because they are synthesised in response to stressors such as herbivory or competition (3). Many chemicals have been extracted from plants and replicated to produce modern drugs, such as salicin (more commonly known as aspirin), which was extracted from the bark of a white willow tree (4). The use of traditional medicine is extensive and continues to increase. ...
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Introduction: Portulacaria afra is a medicinal plant commonly used among African traditional healers to treat skin conditions and dehydration. The aim of this study was to scientifically validate the use of P. afra among traditional healers. Methods: Standard phytochemical colour tests were used to determine the presence of ten phytochemicals, using four solvents of varying polarities (hexane, ethyl acetate, methanol, and water). The antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) and hydrogen peroxide scavenging assays. An agar-well diffusion assay was used to determine the antibacterial activities of the leaves, stems, and roots of P. afra against Staphylococcus aureus and Escherichia coli. Results: P. afra exhibited a high phytochemical presence in the methanolic extracts, with seven out of the 10 phytochemical groups present. Flavonoids and phlobatannins were absent in all of the plant’s extracts. The methanolic root extract exhibited the highest DPPH scavenging activity (IC50=0.39) whilst the hexane leaf extract (IC50= 14.83) was the only extract to exceed the acceptable upper limit. The scavenging activity of the plant was stronger against hydrogen peroxide than it was against DPPH. The methanolic and hot water stem extracts displayed the largest zone of inhibition (of 20 mm) against E. coli. The cold-water and room-temperature water extracts, of all three plant parts, showed no zone of inhibition against either bacterial strain. Conclusion: P. afra has the capacity to be used as a nutritional supplement for its antioxidant properties, while the antibacterial properties may provide relief against E. coli infections.
... Microbial control in turn reduces the inflammatory response, which in turn decreases the plasma leakage in saliva through gingival crevicular fluid; this statement could be supported by the overall reduction in total salivary protein levels. (16) Further investigations: Several studies have reported anti-inflammatory effects of cocoa flavonoids,(36) thyme, (37) Artemisia annua, (38) Inonotus obliquus (chaga mushroom), (39) leaf extract of Ananas comosus, (40) Thykamine extracts from spinach (41) and White Willow Bark (Salix alba) (42) on different parts of the body. An analysis 32 evaluating the influence of these products would be beneficial in order to elucidate their effects on periodontal disease. ...
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Article History Background and Aim: The most common etiology of gingivitis is accumulation of bacterial plaque. Complete removal of microbial plaque by mechanical procedures is not possible in some cases; for example, aged and disabled patients might not be capable of removing the bacterial plaques properly. Also, chemical mouthwashes have some adverse effects. Therefore, finding a new treatment approach would be helpful. The global focus on the use of herbal medicine for treatment of different health conditions is on the rise. The present study aimed at searching and collecting scientific evidence regarding medicinal herbs to treat gingivitis and periodontitis. Materials and Methods: In this review, an electronic search of the literature was conducted through PubMed, Scopus, Google Scholar, and Wiley online library databases. Studies were considered for inclusion if they evaluated medicinal herbs affecting gingival and periodontal inflammation or periodontal pathogens. Totally, 197 full-text articles were evaluated and finally, based on the inclusion criteria, 22 articles were selected. Results: There are various medical herbs with antibacterial and anti-inflammatory properties, which can significantly decrease gingival and periodontal inflammation , bleeding on probing (BOP), plaque index (PI), probing depth (PD) and the count of major periodontal pathogens, and promote clinical attachment gain. Conclusion: The introduced herbal products could be an efficient and safe alternative to chemical products.
... The reason for the ability of willow bark extract to reduce inflammation is due to the suppression of the two main inflammatory response mediators: tumour necrosis factor-α and nuclear factor-kappa B. Nevertheless, the recurrence of adverse side effects of willow bark extract is much lower than non-steroidal drugs such as aspirin. However, the high incidence of subjects allergic to salycilates might be considered a downside to using untreated willow bark extract over common aspirin (Shara and Stohs, 2015). ...
Article
Throughout history, the genus Salix (willow) has been an incredibly useful temperate plant for humans, with widespread global distribution and species indigenous to all continents except Antarctica. Estimations of the number of species range from 450 to 520 worldwide, and there are still more natural hybrids and multi-hybrid combinations. Several biomass willow breeding programmes have been established across the globe. All of these attempt to produce fast-growing, high-yielding stems with a straight habit and minimal side branching that are highly adaptable to different sites and are also disease and pest resistant. Short rotation coppice (SRC) cultivation involves growing willow at close spacings with a stocking rate of around 15,000 per hectare with harvests every 2–4 years. The crop is mechanically harvested, typically using a forager, and material has recently been used for bioenergy applications. Trial plots have achieved yields of up to 20 odt/ha/yr, whilst well-tended commercial crops have yielded up to 14 odt/ha/yr. Global willow breeding programmes have produced a wide variety of commercial genotypes that have suitable properties for easy planting and harvesting and have the added benefit of elevated levels of bioactive compounds, including salicin, present in the bark, which can be used in medical and veterinary applications. These high-yielding willow varieties grow well in the wetter regions of the globe, including NW Europe, and afford multiple harvests before re-planting. Salix's versatility and adaptability and the SRC cultivation process make them an ideal candidate feedstock for use in an integrated biorefinery to produce a range of biobased materials, including pharmaceuticals, and biocomposites, fuels, energy and fertiliser.
... It has also been used by animals and humans for its analgesic, antipyretic, and anti-inflammatory properties [77,78]. The antioxidative activity of Salix Sp. has also been identified and is mainly attributed to salicin [79], the mechanism of which is said to be the downregulation of the inflammatory mediators, tumor necrosis factor-α, and nuclear factor-kappa B [80]. Besides salicin, flavonoid and other phenolic compounds of Salix have also been identified to have anti-inflammatory properties and synergistic effects with coffee against scavenging free radicals and the inhibition of lipid peroxidation [81,82]. ...
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Neurodegenerative diseases (NDDs) are the main cause of dementia in the elderly, having no cure to date, as the currently available therapies focus on symptom remission. Most NDDs will progress despite treatment and eventually result in the death of the patient after several years of a burden on both the patient and the caregivers. Therefore, it is necessary to investigate agents that tackle the disease pathogenesis and can efficiently slow down or halt disease progression, with the hope of curing the patients and preventing further burden and mortality. Accordingly, recent research has focused on disease-modifying treatments with neuroregenerative or neuroprotective effects. For this purpose, it is necessary to understand the pathogenesis of NDDs. It has been shown that oxidative stress plays an important role in the damage to the central nervous system and the progression of neurodegenerative disorders. Furthermore, mitochondrial dysfunction and the accumulation of unfolded proteins, including beta-amyloid (Aβ), tau proteins, and α-synuclein, have been suggested. Accordingly, cellular and molecular studies have investigated the efficacy of several natural compounds (herbs and nutritional agents) for their neuroprotective and antioxidative properties. The most popular herbs suggested for the treatment and/or prevention of NDDs include Withania somnifera (ashwagandha), ginseng, curcumin, resveratrol, Baccopa monnieri, and Ginkgo biloba. In some herbs, such as ginseng, preclinical and clinical evidence are available for supporting its effectiveness; however, in some others, only cellular and animal studies are available. In line with the scant literature in terms of the effectiveness of herbal compounds on NDDs, there are also other herbal agents that have been disregarded. Picein is one of the herbal agents that has been investigated in only a few studies. Picein is the active ingredient of several herbs and can be thus extracted from different types of herbs, which makes it more available. It has shown to have anti-inflammatory properties in cellular and plant studies; however, to date, only one study has suggested its neuroprotective properties. Furthermore, some cellular studies have shown no anti-inflammatory effect of picein. Therefore, a review of the available literature is required to summarize the results of studies on picein. To date, no review study seems to have addressed this issue. Thus, in the present study, we gather the available information about the antioxidative and potential neuroprotective properties of picein and its possible effectiveness in treating NDDs. We also summarize the plants from which picein can be extracted in order to guide researchers for future investigations.
... It belongs to the endogenous plant hormones necessary for plant growth [27,28]. Salicylic acid is obtained from the white willow (Salix alba), mainly from its roots [29]. It is a safe compound for human health and the environment, additionally exhibits antifungal properties against many types of microorganisms [27,28]. ...
Article
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The presented work describes the effect of poly(hexamethylene biguanide) salicylate (PHMB-SA) ionic liquid on the properties of poly(vinyl alcohol) film. The ionic liquid synthetized is used as an antimicrobial agent. The ionic liquid consist of the poly(hexamethylene biguanide) cation and the salicylic anion, which exhibit synergistic antibacterial and bacteriostatic properties. The structure of obtained new ionic liquid was confirmed by infrared spectroscopy and nuclear magnetic resonance. Additionally, the article describes a simple method of producing an antibacterial PVA-based film with the addition of collagen and an ionic liquid. The study investigated the effect of the amount of the PHMB-SA on the mechanical properties, microorganism in liquid medium and the antibacterial properties of the PVA film. The obtained results indicate that the mechanical and antibacterial properties of the PVA/Col films depended on the amount of the ionic liquid. The higher value of the tensile strength (27.11 MPa) and the higher degree of microbial growth inhibition (7 mm) was obtained for the sample containing 0.75 g PHMB-SA.
... Nahrsted and his team also demonstrated the efficacy of willow bark extract as a natural substitute of aspirin, reducing common side effects of acetylsalicylic acid . A recent experiment comes in agreement, stating that the presence of polyphenolics with strong antioxidant and anti-inflammatory properties might play a major role in the beneficial effects provided by the consumption of willow extracts (Shara and Stohs, 2015). ...
Article
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Willow trees have maintained their place in medicine for many years as they are herbal source of various cures. Willow varieties are considered to contain a wide range of anti-inflammatory and anti-bacterial species such as salicylates and flavonoids. The current work is centred on the presence of high bioactive pharmaceutical constituents other than salicin such as flavan-3-ol catechin, salicortin, and other complex compounds, which contribute to the total medical value of willow extracts. To evaluate the distribution of these bioactives, bark, and wood fractions of 8 different willow varieties (S.X. Dasyclados, Endeavour, Cheviot, Tora, Resolution, S. Purpurea, Terranova, Endurance) were extracted using dispersive solid phase extraction and then analysed using LC-MS comprising quadrupole time-of-flight frequency. Indeed, various high value constituents such as salicortin, catechin, triandrin, acacetin-5-O-xyloside, picein, apigenin-7-O-glucoside, vitexin-2-rhamnoside, luteolin-7-glucoside, catechin gallate, and kaempferol as well as giberellic and 5-methoxysalicylic acid were detected in bark and wood fractions of the willow varieties 80:20 ethanol/water extracts.
... White willow (Salix alba) is a natural source of salicylic acid ( Figure 15) with roles in plant growth and development, photosynthesis, transpiration, ion uptake, and transport. 123 It can be a green, bio-based, efficient, readily available, and low-cost catalyst for chemical synthesis. ...
Article
The design and development of eco-friendly procedures for synthesizing organic compounds is an essential key to synthetic chemistry and has gained significant interest. The catalysts increase the rate of chemical reactions with additional advantages such as reduced energy input, diminished environmental impact, and overall financial benefit. The combined advantages of multicomponent reactions (MCRs) and natural catalysts will be an emerging and strategic area and is an ideal blend for the development of sustainable methodologies in organic synthesis. The plant, fruits, and their extracts and residues contain many useful chemical components lost during disposal. The crops contain renewable chemicals which are useful for catalysis and organic synthesis. Due to the excellent chemical properties of the natural extracts, they have gained great attention as cost-effective catalysts. In this review, we critically focus on using natural-based catalysts in multicomponent reactions that lead to synthetically and biologically relevant organic molecules and diverse heterocycles. The use of natural-based catalysts is cost-effective, favorable for work-up procedures, sustainable and industrial applications, and is usually more effective than traditional catalysts.
... Furthermore, several drugs used in conventional medicine were originally derived from plants. For example, salicylic acid, a precursor of aspirin, was first derived from Salix alba (white willow) tree bark [10]. Similarly, artemisinin is an antimalarial drug derived from Artemisia annua (sweet wormwood), a prominent herb in Chinese traditional medicine [11]. ...
Article
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This study investigated the toxicological implications of a commercial polyherbal formulation, KWAPF01. Twenty-four Wistar rats were randomized into six groups of four animals per group. The animals in Group 1 were administered placebo and designated as control, while the rats in Groups 2 to 6 were administered 1000, 1500, 2000, 2500, and 3000 mg/kg bodyweight single oral dose of KWAPF01, respectively, and subsequently monitored for gross morphological and behavioural changes for 72 h. Piloerection, reduced motility, and tremor were observed in experimental groups, and the median lethal dose (LD50) of the extract was 2225.94 mg/kg bodyweight. The 11 compounds identified through HPLC analysis of the extract were docked against acetylcholinesterase (AChE), and the docking scores ranged from −5.3 to −10.8 kcal/mol, with catechol (−5.3 kcal/mol) and berberine (−10.8 kcal/mol) having the highest and lowest binding energies, respectively. Judging by the results, it could be inferred that some of the constituents of KWAPF01 have a direct impact on the nervous system and this is possibly elicited via the cholinergic system as it contains a nicotinic acetylcholine receptors agonist and potential inhibitors of AChE. Therefore, the use of KWAPF01 needs to be cautiously guided.
... Compared to synthetic salicylates, the effect is slower, but lasts longer and has no negative effect on the gastrointestinal tract. The absence of ulcerogenic action, natural origin, as well as the presence of additional effects, hemostatic, disinfectant, antirheumatic, etc., are the undeniable advantages of using a dry extract of white willow bark as an active substance [14]. ...
Article
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The aim of the work is to develop the composition of the transdermal therapeutic system of anti-inflammatory action based on active pharmaceutical ingredients of natural origin. Materials and methods. Selection of adhesive materials, plasticizers and solvents, the effect of introduction to the base of active pharmaceutical ingredients, determination of optimal temperature and drying time, pharmacological screening was performed by physicochemical, biopharmaceutical and biological research methods. Results. The composition of the hydrophilic adhesive composition, which includes polyvinylpyrrolidone, eudragit (adhesives), PEO-400 (plasticizer), isopropyl alcohol (solvent) 50: 8: 12: 30, respectively. This composition has excellent organoleptic properties, is easily applied to the polymer base, holds its shape well (does not flow beyond the base), is applied in a thin layer and evenly distributed on the base. The optimal mode of drying of the adhesive composition based on PVP is 75 °C for 30 min, based on PVA – 75 °C for 35 min, the composition containing eudragit - 50 °C for 10 min. It is established that the addition of active substances to the adhesive composition does not adversely affect its properties. The study of antiexudative activity using different combinations of substances of natural origin as API and found that the best anti-inflammatory properties (25 %) have a sample No. 4, which includes dry extracts of white willow bark and sage leaves and quercetin 3:1:3 in accordance. Conclusions. Based on physicochemical, biopharmaceutical and pharmacological studies, the composition of the transdermal therapeutic system of anti-inflammatory action with active pharmaceutical ingredients of natural origin has been developed
... Obtaining digoxin from Digitalis purpurea L. allowed for an effective treatment of atrial fibrillation and heart failure 5 . Salicylic acid, which is found, among others, in Salix alba L., after esterification forms acetylsalicylic acid, used in pain and thrombotic diseases 6 . The isolated artimizin from Artemisia annua L. is used in the treatment of a resistant form of malaria 7 . ...
Article
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Human has used plants to treat many civilisation diseases for thousands of years. Examples include reserpine (hypertension therapy), digoxin (myocardial diseases), vinblastine and vincristine (cancers), and opioids (palliative treatment). Plants are a rich source of natural metabolites with multiple biological activities, and the use of modern approaches and tools allowed finally for more effective bioprospecting. The new phytochemicals are hyaluronidase (Hyal) inhibitors, which could serve as anti-cancer drugs, male contraceptives, and an antidote against venoms. In turn, tyrosinase inhibitors can be used in cosmetics/pharmaceuticals as whitening agents and to treat skin pigmentation disorders. However, the activity of these inhibitors is stricte dependent on their structure and the presence of the chemical groups, e.g. carbonyl or hydroxyl. This review aims to provide comprehensive and in-depth evidence related to the anti-tyrosinase and anti-Hyal activity of phytochemicals as well as confirming their efficiency and future perspectives.
... The genus Salix L. (willows) belongs to the Salicaceae family and includes 330-500 species of trees and shrubs with simple, stipulate leaves alternately arranged on woody stems [20]. The medicinal and economic value of willows are exploited in traditional medicine as well as in pharmacy, and willow-originated metabolites are known to be used in the food industry as natural additives and as ingredients in cosmetic products, including sunscreen and anti-aging cream formulations [21][22][23]. Willows are mostly known for their high levels of salicylates, becoming a major object of research after the discovery of aspirin. The pharmacological value of willows does not only arise from the salicin portion in the willow bark but from other components as well such as polyphenolics. ...
Article
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This study presents the first report on phenolic composition and bioactivity of ethanolic extracts of three plant species that grow in the western Balkan mountains and are used in traditional folk medicine: Valeriana montana, Salix retusa, and Campanula hercegovina. Phenolics were extracted from different aerial plant parts using 80% ethanol to assess the possibility of sustainable use of these plants as a source of bioactive compounds without disruption to the roots (for V. montana) or destruction of whole habitats (for S. retusa and C. hercegovina). The ethanolic extract of V. montana flower contained noticeable levels of apigenin and quercetin. The branches and bark of S. retusa were significantly rich in catechin, while rutin was the major phenolic found in the leaf extract of C. hercegovina. Furthermore, the flower extract of V. montana revealed the best antioxidant activity, which was comparable to 4-hydroxybenzoic acid and quercetin. Considering antimicrobial activity, the leaf extracts of V. montana and C. hercegovina demonstrated potent activity against all microbes tested, while the extracts of S. retusa were moderately effective. The presented results emphasize the potential of these plants as novel sources of bioactive compounds.
... In addition, modulation of specific signaling pathways, such as mitogen-activated protein kinases (MAPKs) and nuclear factor-kappa B (NF-κB), which can be induced by oxidative stress, are important targets in the discovery of new drugs for the treatment of a wide range of inflammatory disorders (Laufer et al. 2002). Natural products, including compounds derived from plants, have been used for the development of new drugs, one of the main examples being acetylsalicylic acid (Aspirin), extracted from the bark of the plant Salix alba L. Antioxidant substances based on natural compounds play a preventive role in protecting against the generation of free radicals and, therefore, are one of the most valuable therapeutic agents for reducing the various associated inflammatory diseases (Shara and Stohs 2015). For example, in addition to having antioxidant activities, flavonoids and phenolic compounds also play an effective role as anti-inflammatory factors, blocking two main signaling pathways, such as NF-κB and MAPKs, which have the main role in the production of several mediators proinflammatory (Arulselvan et al. 2016). ...
Article
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Myrciaria plinioides D. Legrand (Myrtaceae) is a native plant of Southern Brazil, which have potential in the food industry due to its edible fruits. Many plants belonging to this genus have been used for a variety of illnesses, including inflammatory disorders due to antioxidant properties. However, therapeutic uses of M. plinioides have been poorly studied. The aim of study was to assess the anti-inflammatory and anticoagulant activities of the ethanol leaf extract of M. plinioides . In M. plinioides extract-treated RAW 264.7 cells, assessments of cell viability, TNF-α release and p38 MAPK pathway-dependent protein expression were detected. In addition, rat paw edema models were used to analyze the anti-inflammatory effect of the extract. Macrophages cell line treated with M. plinioides extract showed a slight decrease in cell viability. In LPS-stimulated macrophages treated with different concentrations of the extract for 24 h, TNF-α release was inhibited, while modulation of p38 signaling pathway and inhibition of NF-κB p65 protein expression were dose-dependent. In rats, the extract inhibited the formation of paw edema, while an inhibitory effect on trypsin-like enzymes derived from mast cells was seen. Furthermore, the extract presented anticoagulant activity via extrinsic pathway, being able to block specifically factor Xa and thrombin. The study suggests that extract possess potent anti-inflammatory and anticoagulant effects. M. plinioides present great biological potential as a source for the development of anti-inflammatory and anticoagulant drugs. Additional studies can be proposed to better elucidate the mechanism by which M. plinioides exerts its effects.
... Debarked wood is more homogeneous, increasing its acceptability for the pulp and paper industry and its efficient biomass conversion into biofuels and bioproducts (Nurmi and Lehtimäki 2011, Jacob et al. 2013, Chahal and Ciolkosz 2019. Bark itself has a place in by-product markets, such as fiber, tannins, gums, resins, flavorings, antibiotics, mulch, building material, and/or medicinal products (Harkin and Rowe 1971, Kain et al. 2012, Marron 2015, Shara and Stohs 2015. Therefore, managing and dealing with wood and bark material of small-diameter woody material separately has commercial relevance both to enhance the value of wood and to create additional products from bark. ...
Article
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Sufficiently valuing small-diameter-stem (diameter < 9 in.) woody material in Pennsylvania forest product markets may incentivize increased utilization of that material, a resource opportunity that would provide economic and ecological benefits to the state's forests and forest products community. Debarking is one primary process that could enhance the value of these small-diameter-stem materials for secondary markets. The wood products community in Pennsylvania was surveyed as to their perceptions of the status and value of economical small-diameter-stem debarking. The largest perceived current market for debarked, small-diameter-stem material identified by respondents is for chips for pulp and paper, and anticipated future demand is expected to be highest for chips for pulp and paper, chips for energy, and small-dimension lumber. Respondents who currently supply a given market tend to be more optimistic about that market than respondents who do not serve that particular market. Shredded wood/hog fuel and mulch are the two markets with the lowest overall scores for anticipated benefit of additional processing by debarking. Seventy-six percent of all respondents indicated that economical small-diameter-stem debarking would benefit their operation.
... Natural products, including compounds derived from plants, have been used for the development of new drugs, one of the main examples being acetylsalicylic acid (Aspirin), extracted from the bark of the plant Salix alba L. Antioxidant substances based on natural compounds play a preventive role in protecting against the generation of free radicals and, therefore, are one of the most valuable therapeutic agents for reducing the various associated in ammatory diseases (Shara and Stohs 2015). For example, in addition to having antioxidant activities, avonoids and phenolic compounds also play an effective role as antiin ammatory factors, blocking two main signaling pathways, such as NF-κB and MAPKs, which have the main role in the production of several mediators proin ammatory (Arulselvan et al. 2016). ...
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Myrciaria plinioides D. Legrand (Myrtaceae) is a native plant of Southern Brazil, which have potential in the food industry due to its edible fruits. Many plants belonging to this genus have been used for a variety of illnesses, including inflammatory disorders due to antioxidant properties. However, therapeutic uses of M. plinioides have been poorly studied. The aim of study was to assess the anti-inflammatory and anticoagulant activities of the ethanol leaf extract of M. plinioides . In M. plinioides extract-treated RAW 264.7 cells, assessments of cell viability, TNF-α release and p38 MAPK pathway-dependent protein expression were detected. In addition, rat paw edema models were used to analyze the anti-inflammatory effect of the extract. Macrophages cell line treated with M. plinioides extract showed a slight decrease in cell viability. In LPS-stimulated macrophages treated with different concentrations of the extract for 24 h, TNF-α release was inhibited, while modulation of p38 signaling pathway and inhibition of NF-κB p65 protein expression were dose-dependent. In rats, the extract inhibited the formation of paw edema, while an inhibitory effect on trypsin-like enzymes derived from mast cells was seen. Furthermore, the extract presented anticoagulant activity via extrinsic pathway, being able to block specifically factor Xa and thrombin. The study suggests that extract possess potent anti-inflammatory and anticoagulant effects. M. plinioides present great biological potential as a source for the development of anti-inflammatory and anticoagulant drugs. Additional studies can be proposed to better elucidate the mechanism by which M. plinioides exerts its effects.
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Benzyl amines were deaminated for the olefination of methyl N ‐heteroarenes such as quinolines, benzothiazoles, and quinoxalines catalyzed by 4,6‐dihydroxysalicylic acid with only 1 mol % catalyst loading. A wide range of N ‐heteroaryl stilbenoids were synthesized in yields of 42 to 96 % using oxygen (1 atm) as the sole oxidant. 4,6‐dihydroxysalicylic acid not only behaves as an organocatalyst for the oxidation of benzyl amines to the imine intermediates, but also provides an acidic reaction condition for the olefinations. Gram scale reaction and the synthesis of two pharmaceutically relevant conjugated olefins were also successful using this methodology.
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Natural ingredients have many applications in modern medicine and pharmaceutical projects. However, they often have low solubility, poor chemical stability, and low bioavailability in vivo . Spray drying technology can overcome these challenges by enhancing the properties of natural ingredients. Moreover, drug delivery systems can be flexibly designed to optimize the performance of natural ingredients. Among the various drug delivery systems, dry powder inhalation (DPI) has attracted much attention in pharmaceutical research. Therefore, this review will focus on the spray drying of natural ingredients for DPI and discuss their synthesis and application.
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Many traditional Nepalese herbs have been shown to have medicinal, cosmetic, cultural,and nutritional values among different ethnic communities. The extracts, oils, resins,ash or plant parts are used to prepare the medicines, supplements and cosmetics due to their properties for various ailments of the skin, hair, stomach, liver and dental care. The prospect of herbal product development in Nepal in this era is very challenging due to limited technology, policy issues, research funds, experts and market values. But current initiation can generate new opportunities for future directions of international standard product development within the country. The private sectors, particularly the Ayurvedic industries of Nepal, are heavily involved in developing value-added products that claim to be highly effective for daily usage and avoid side effects. Out of the highly traded 300 medicinal plants of Nepal, approximately 85% plants are exported in crude form to more than 50 countries worldwide. Bulk amounts of medicinal plants are mostly exported to India. It is agreed that, improving traditional medicine, standardizing raw materials quality, isolation of active molecules, or new innovations opens the doors to improved financial avenues. Pharmaceutical, agribusiness, cosmetics, personal care, fragrance, botanicals, food and beverage industries are currently doing bio-prospecting of Nepalese medicinal plants. However, there is a significant gap in terms of patenting and sharing the knowledge gained from the specific domain. Most of the academic institutions in Nepal are working on medicinal plant-based research in different perspectives. Only a few are focusing on herbal product development, commercialization, and revenue generation through the finished products. National level trainings, industry-academia linkage, development of Nepalese herbal pharmacopoeia, medicinal plants export policy, biotechnology, research and development (R&D) facility, formulation development, and product standardization are few key components that should be prioritized for promotion of herbal products within the country. To accomplish this target, researchers, scientists, academicians, industry professionals, and students should collectively work on a common platform from the conceptualization of value-addition ideas to detailed revenue collection from both domestic and international markets. Local medicinal plants can be developed into various dosage forms such as tablets, capsules, ointments, creams, gels, microspheres, transdermal patches, and so on using ethno-botany knowledge from Nepal’s indigenous cultures. The phytochemical and common pharmacological strategies such as antimicrobial, antioxidant, wound healing, analgesic, antidiabetic, anticancer, anti-anxiety, anti-inflammatory etc. of plants might lead to the early discovery and commercialization of local herbs. Keywords: Bioprospecting, Ethnobotany, Herbal formulation, Plant biology, Technology
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Background: Inflammatory bowel diseases (IBD) are a worldwide health problem and mainly affect young people, consequently affecting the workforce. Available treatments are often associated with side effects, and new therapeutic options are needed. For centuries, plants have represented important substrates in the field of drug development. Lafoensia pacari (L. pacari) is a plant whose pharmaceutical potential has been described, and may have biological activity relevant to the treatment of IBD symptoms. Aim: To investigate the activity of keto-alcoholic extracts of L. pacari with respect to ameliorating the inflammatory and nociceptive symptoms of acute experimental colitis in mice. Methods: Keto-alcoholic extracts of L. pacari leaves and bark were administered to male and female Swiss mice weighing 25 g to 30 g (n = 8 male mice and n = 8 female mice). The effect of these extracts was observed in an acetic acid-induced acute experimental model of colitis with regard to antinociception/analgesia and inflammatory tissue damage. Recorded macroscopic indices included the Wallace score and the colon weight obtained using a precision scale. Mechanical hyperalgesia was determined using an electronic analgesimeter. Behavior related to overt pain was determined by quantifying the number of writhing instances within 20 min of administration of acetic acid. Molecular docking was performed using human and murine cyclooxygenase-2 (COX-2) with 3 flavonoids (ellagic acid, kaempferol, and quercetin) on the AutoDock Vina software. Analysis of variance followed by Tukey's posttest was used with P < 0.05 indicating significance. Results: In this murine model of colitis, administration of extracts from L. pacari ameliorated acetic acid-induced writhing and colitis-associated inflammatory pain. These improvements may be attributable to the reduction in edema, inflammation (e.g., ulcers, hyperemia, and bowel wall damage), and the intensity of abdominal hyperalgesia. The keto-alcoholic extracts of L. pacari leaves and bark administered at a dose of either 100 mg/kg or 300 mg/kg significantly reduced the number of writhing events when compared to the negative control (P < 0.05). Additionally, extracts of L. pacari bark also performed better than Dipyrone. Leaf extracts administered at 10 mg/kg, 30 mg/kg, and 100 mg/kg and bark extracts administered at 30 mg/kg significantly reduced or prevented the development of edema in the colon of treated mice, while mesalazine did not. Moreover, using molecular docking, we observed that the flavonoids present in L. pacari extracts bind to COX-2, an event not unique to ellagic acid. Conclusion: The results of this study demonstrate a potential novel application of L. pacari extracts for the reduction of inflammation and promotion of antinociception/analgesia as demonstrated by our findings in a murine model of colitis. These findings were also corroborated by in silico analyses, and suggest that L. pacari extracts may be a promising therapeutic agent in the treatment of IBD.
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There is enormous interest in using artificial intelligence (AI) in health care contexts. But before AI can be used in such settings, we need to make sure that AI researchers and organizations follow appropriate ethical frameworks and guidelines when developing these technologies. In recent years, a great number of ethical frameworks for AI have been proposed. However, these frameworks have tended to be abstract and not explain what grounds and justifies their recommendations and how one should use these recommendations in practice. In this paper, I propose an AI ethics framework that is grounded in substantive, human rights theory and one that can help us address these questions.
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Willow bark is highly valuable in medicine, different branches of industry and ecology. In this respect antioxidants and minerals distribution between bark tissues seems to be highly valuable. Using ICP-MS mineral composition of willow bark cambium, phloem and periderm was determined for the first time. Predominance of P, K and Ca was recorded for cambium characterized by intensive metabolism. On the contrary, periderm demonstrated the highest concentrations of all heavy metals, except Ni, Al and As, and the highest coefficients of variation compared to phloem and cambium, especially for Al (107.5%), Pb (112.2%), V (133.3%), and Sn (90.9%). Though trace elements also prevail in periderm, low coefficient of variation between tissues indicates the importance of Fe, Mn, B, Zn, Cu and Mo in plants growth. Among tissues studied cambium recorded the highest antioxidant activity with relatively similar values of polyphenol content compared to periderm and phloem data. The results prove high prospects of willow bark cambium utilization as a valuable source of antioxidants and trace elements and of periderm as a natural adsorbent. KEYWORDS: willow bark, periderm, phloem, cambium, antioxidants, minerals.
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Non-Communicable Diseases (NCDs) have become a major health concern worldwide. The global death percentage caused by NCDs is reported to be 70% of the total deaths. Currently, there is a significant concern about herbal applications in improving people's lifestyles to mitigate the risk of NCDs, and food product development with an herbal context is considered more impactful. Plant/herbal materials have been used in traditional medicine since ancient times due to the nutraceutical properties of secondary plant metabolites. These are known to exert several health-promoting effects such as antioxidant, anti-cancer, anti-lipidemic, anti-hyperglycemic, etc. properties. Therefore, modern society is concerned more about adopting to pharmaceuticals and diet interventions of natural-origin to mitigate health conditions associated with NCDs. Those interventions are, in most cases, termed functional foods and/or nutraceuticals. Thus, a substantial global market opportunity has been relieved for herbal functional foods and nutraceuticals, recently. Therefore, this paper provides a narrative review on the global burden caused by the NCDs, and the deviation of consumer trends towards more natural and herbal oriented functional foods in overcoming those risks. Furthermore, such trends are predicted to rise drastically in upcoming years in the regions around the globe with significant generation of revenue. This review further elaborates on pharmacological and health benefits of herbal materials that could be used in developing functional foods and/or nutraceuticals. In addition, current and prospective functional foods and nutraceuticals that have been developed with herbal origins in recent research across the globe are presented here with their respective health-promoting effects. The food categories currently being developed into functional foods are mostly being, but not limited to, functional beverages, functional teas, functional snacks/starchy foods, and functional confectioneries. The physiological benefits expected by these functional foods and nutraceuticals include, prevention of hyperglycaemia, cardiovascular disease, hypertension, cancers, hypercholesterolemia, etc. This review would provide a brief but informative background for future researchers, who would carry out research on New Product Development (NPD) on functional foods and nutraceuticals of herbal origin.
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Herbal medicines and other complementary & alternative therapies are now a part of the mainstream healthcare system. Adults frequently utilizing herbal remedies to treat pain, which is one of the most prevalent ailments. Although herbal remedies are frequently not the most effective analgesics in the market, they can be very helpful for mild to moderate pain. Herbal bioactive substances may reduce the effectiveness of conventional treatments for pain. Life quality suffers, and excessive medical costs rise as a result of pain. Western medicine may have too many negative effects, such as addiction and tolerance. Alternative pain-management approaches may be offered by herbal medicines. Neuropathic pain is one of the many types of chronic pain that results from damage to the neurological system, including the peripheral nerves. There are few treatments for neuropathic pain now available. Recent studies have also shown the value of dietary bioactive compounds in the management of pain like Ginger, Curcumin, Omega-3 polyunsaturated fatty acids, soy isoflavones and Lycopene. The goal of this review paper is to determine the function of various bioactive and some traditional alternative therapies in the treatment of pain.
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This paper is typically intended to carefully collect and properly review the antinociceptive activities of medicinal plants. In this review article, by searching keywords of medicinal plants, pain, herbal medicine, antinociceptive, phytotherapy in databases of Web of Science, Scopus, Google Scholar, Springer, Wiley, Proquest, PubMed, Nature, Magiran, Emerald, SID, ISI, and some other indexing cites, or traditional books, desired articles were obtained until 2021. The title of medicinal plants was searched diligently in Persian and English. Ultimately, 270 articles were studied. The findings possibly indicated that several medicinal plants are among the most valuable plants that have antinociceptive activities. There efficiently are various antinociceptive compounds in medicinal plants. The antinociceptive activity of these specific compounds may be through their peculiar effects on the opioid system, cholinergic pathways, and stimulation of GABA receptors, with the peripheral and central antinociceptive mechanism. Antiinflammatory processes, inhibition of the synthesis, and the release of arachidonic acid, prostaglandins, phospholipase, nitric oxide, and cyclooxygenase‐2 have been reported as analgesic mechanisms of some herbs. In a reasonable conclusion, our review thoughtfully provides a comprehensive summary of present data from some scientific studies on the common herbs with antinociceptive and antiinflammatory activities.
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Extracts from Boswellia serrata (Bs) and Salix alba (Sa) are used as supplements in poultry feed. The aims of this research were to study the possible effects of dietary supplementation with Bs and Sa extracts on serum and albumen proteins, zinc and iron, and yolk cholesterol content in Leghorn hens during the critical phase of the onset of laying. A total of 120 pullets, 17 weeks of age, were assigned to two groups (control (C) and treated (T), n = 60 each). The T group received a supplement containing Bs (5%) and Sa (5%) for 12 weeks. The study lasted 19 weeks. Serum proteins were fractionated using agarose gel electrophoresis (AGE) and SDS–polyacrylamide gel electrophoresis (SDS–PAGE). Trace elements were determined in serum using atomic absorption spectrometry, and yolk cholesterol was determined using a colorimetric test. No significant differences were observed between control and supplemented hens for the analyzed biochemical indices. Moreover, the supplementation with phytoextracts did not negatively affect the physiological variations in serum proteins; therefore, it can be safely used as a treatment to prevent inflammatory states at onset and during the early laying phase.
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As plantas medicinais e os fitoterápicos são alternativas para o tratamento de diversas doenças. O Sistema Único de Saúde (SUS) possui 12 fitoterápicos padronizados na Relação Nacional de Medicamentos Essenciais (RENAME): alcachofra, aroeira, babosa, cáscara-sagrada, espinheira-santa, garra-do-diabo, guaco, hortelã, isoflavona-de-soja, plantago, salgueiro e unha-de-gato. O objetivo deste trabalho foi avaliar os eventos adversos destes fitoterápicos e as possíveis interações medicamentosas resultantes do seu uso concomitante com medicamentos convencionais. O trabalho foi realizado por meio de uma revisão narrativa da literatura no período entre 1995 e 2020. As plantas medicinais e/ou os medicamentos fitoterápicos são constituídos de compostos químicos, que em sua maioria são responsáveis pelas suas variadas ações farmacológicas. A composição química complexa aumenta a possibilidade de interações quando medicamentos convencionais são utilizados concomitantemente. As interações podem ser benéficas ou desfavoráveis, podendo potencializar o efeito de fármacos, reduzir a eficácia, resultar em reações adversas ou não alterar o efeito esperado do fármaco. Ressaltou-se a importância de considerar os fitoterápicos/plantas medicinais com a mesma importância que os medicamentos sintéticos, baseando a conduta clínica em evidências científicas confiáveis, reconhecendo sua eficácia, mas também seus efeitos adversos e a possibilidade de interações medicamentosas tornando, assim, seu uso mais seguro e eficaz.
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The environment is being continuously deteriorated by air pollution and global warming, increased pressure of work or family on life, and changes in lifestyle; these factors have contributed to an increase in the proportion of both females and males with sensitive skin. To this end, the cosmetics market has focused on developing hypoallergenic or skin-soothing and make-up products. Here, we summarize the definition and causes of sensitive skin, list the mechanisms underlying the development of this condition, and review the natural plant products and purified active components that have potential for use in anti-allergic cosmetics. A review of studies that evaluated the anti-allergic properties of natural products was conducted. There has been a progressive increase in the number of natural products identified as potential anti-allergic raw materials in cosmetics. Finally, we suggest strategies for developing anti-allergic cosmetics in the future.
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Amaç: Kanser, hücrelerin kontrolsüz çoğalması sonucu ortaya çıkan ve her geçen yıl daha da yaygınlaşan hastalıkların başında gelir. Mevcut tedavi yöntemlerinin yetersizliği, seçici etkiye sahip ve nispeten daha az yan etkili yeni yöntem arayışı her geçen gün artmıştır. Son yıllarda kanser tedavi yöntemlerinden biri olarak yaygınlaşan fitoterapi, en dikkat çekici aday ve hızla gelişen bir alan oluşturmuştur. Bu çalışmada fitoterapi yönteminden yola çıkarak, pican cevizinin (Carya illinoinensis) yeşil-dış kabuğunun antikanser aktivitesi araştırılmıştır. Materyal ve Metod: Pican cevizi yeşil kabuğunun çeşitli kanser hücre hatları üzerindeki antikanser aktivitesi hücre kültürü yöntemi kullanılarak test edilmiştir. Bu kapsamda PC-3, DU-145, PNT1-A, HT-29, HCT-116 ve HUVEC hücre hatları, pikan cevizi yeşil-dış kabuğu hekzan ekstraktı ile tedavi edilerek sitotoksik değeri (MTT boyaması) belirlenmiştir. Belirlenen doz ve hücreler kullanılarak Annexin V/PI boyaması ile apoptotik hücre yüzdesi ve PI boyaması ile ise hücre döngüsü üzerine etkileri araştırılmıştır. Bulgular: Elde edilen deney sonuçlarına göre pican cevizi yeşil-dış kabuk hekzan ekstraktı seçici etki göstererek en yüksek sitotoksik etkiyi prostat kanseri hücre hattı olan PC-3 üzerine gösterdiği tespit edilmiştir (IC50: 40.32µg/ml). Belirlenen IC50’unda apoptotik hücre yüzdesi %94 ve G0/G1 fazında tutulan hücre miktarı ise %59.2 olduğu bulunmuştur. Sonuç: Bu çalışma sonucunda PC-3 hücrelerin, hücre bölünmesini yavaşlattığı ve hücrelerde apoptozisi tetiklediği tespit edildi. Bu sonuçlara göre, farmakolojik alanda pican cevizi yeşil-dış kabuğunun kanser tedavisinde kullanılabilecek alternatif bir bitki adayı olduğu ve bu alanda yapılacak çalışmalara yol gösterici olacağı öngörülmektedir.
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Objectives Colorectal cancer continues to have one of the highest incidents of occurrence with a rising rate of diagnosis among people under the age of 50. Chemotherapy with irinotecan results in severe gastrointestinal dose-limiting toxicity that is caused by the glucuronidated form of the active metabolite (SN-38G). This study evaluates herbal compounds and analogs to biomodulate the metabolism of IR to decrease dose-limiting toxicity while increasing the amount of the active metabolite. Methods In vitro metabolism using human liver microsomes was conducted with white willow bark (WWB) extract, select specific components of WWB, and analogues to evaluate biomodulation of the IR metabolism. Samples were analyzed using liquid chromatography-tandem mass spectrometry to measure metabolites between reactions with and without herbals components. Results WWB showed an optimal decrease (>80%) in SN-38G and a corresponding increase in SN-38 levels (128%) at a concentration of near 200 μg/mL. Tannic acid produced a 75% decrease in SN-38G with a 130% increase in SN-38 at 10 μg/mL, whereas the treatment with beta-pentagalloyl glucose and various analogues decreased SN-38G by 70% and increased SN-38 by 20% at 10 μg/mL. Conclusions These results suggest naturally occurring compounds from WWB may have the potential to increase potency by increasing the conversion of IR to SN-38 and decrease dose-limiting toxicity of IR chemotherapy by reducing glucuronidation of SN-38.
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Salix alba (white willow) bark extract is widely used for conditions associated with inflammation, fever, microbial infection or pain. Exposure of human cultured leukocytes to S. alba in vitro noted a genotoxic response. However, data regarding the influence of this bark extract on DNA damage in vivo are lacking. The main goal of this study was to examine the potential of S.alba bark extract to induce DNA damage and chromosome aberrations in an in vivo model using cells obtained from male Swiss albino mice administered the compound orally. The extract was administered by oral gavage daily for 7 days at doses of 500, 1000, or 2000 mg/kg b.w. Genotoxicity analysis was performed using the comet assay on peripheral blood leukocytes, as well as liver, bone marrow, heart, and testicular cells collected 4 hr after the last treatment and the micronucleus (MN) test on bone marrow cells. In essence cells were collected 28 hr after the penultimate treatment Data demonstrated that S. alba bark extract did not induce significant DNA damage in any cell types examined, or clastogenic/aneugenic effects as detected by the MN test at the three tested doses. Under these experimental conditions, evidence indicates that S.alba bark extract did not initiate genotoxic or chromosome aberrations in various mouse cells investigated.
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Coffee and willow are known as valuable sources of biologically active phytochemicals such as chlorogenic acid, caffeine, and salicin. The aim of the study was to determine the interactions between the active compounds contained in water extracts from coffee and bark of willow (Salix purpurea and Salix myrsinifolia). Raw materials and their mixtures were characterized by multidirectional antioxidant activities; however, bioactive constituents interacted with each other. Synergism was observed for ability of inhibition of lipid peroxidation and reducing power, whereas compounds able to scavenge ABTS radical cation acted antagonistically. Additionally, phytochemicals from willow bark possessed hydrophilic character and thermostability which justifies their potential use as an ingredient in coffee beverages. Proposed mixtures may be used in the prophylaxis or treatment of some civilization diseases linked with oxidative stress. Most importantly, strong synergism observed for phytochemicals able to prevent lipids against oxidation may suggest protective effect for cell membrane phospholipids. Obtained results indicate that extracts from bark tested Salix genotypes as an ingredient in coffee beverages can provide health promoting benefits to the consumers; however, this issue requires further study.
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The purpose of this study was to assess the effect of 8-weeks ingestion of a commercialized joint pain dietary supplement (InstaflexTM Joint Support, Direct Digital, Charlotte, NC) compared to placebo on joint pain, stiffness, and function in adults with self-reported joint pain. InstaflexTM is a joint pain supplement containing glucosamine sulfate, methylsufonlylmethane (MSM), white willow bark extract (15% salicin), ginger root concentrate, boswella serrata extract (65% boswellic acid), turmeric root extract, cayenne, and hyaluronic acid. Subjects included 100 men and women, ages 50-75 years, with a history (>3 months) of joint pain, and were randomized to InstaflexTM or placebo (3 colored gel capsules per day for 8 weeks, double-blind administration). Subjects agreed to avoid the use of non-steroidal anti-inflammatory drugs (NSAID) and all other medications and supplements targeted for joint pain. Primary outcome measures were obtained pre- and post-study and included joint pain severity, stiffness, and function (Western Ontario and McMaster Universities [WOMAC]), and secondary outcome measures included health-related quality of life (Short Form 36 or SF-36), systemic inflammation (serum C-reactive protein and 9 plasma cytokines), and physical function (6-minute walk test). Joint pain symptom severity was assessed bi-weekly using a 12-point Likert visual scale (12-VS). Joint pain severity was significantly reduced in InstaflexTM compared to placebo (8-week WOMAC, [downwards arrow]37% versus [downwards arrow]16%, respectively, interaction effect P = 0.025), with group differences using the 12-VS emerging by week 4 of the study (interaction effect, P = 0.0125). Improvements in ability to perform daily activities and stiffness scores in InstaflexTM compared to placebo were most evident for the 74% of subjects reporting knee pain (8-week WOMAC function score, [downwards arrow]39% versus [downwards arrow]14%, respectively, interaction effect P = 0.027; stiffness score, [downwards arrow]30% versus [downwards arrow]12%, respectively, interaction effect P = 0.081). Patterns of change in SF-36, systemic inflammation biomarkers, and the 6-minute walk test did not differ significantly between groups during the 8-week study CONCLUSIONS: Results from this randomized, double blind, placebo-controlled community trial support the use of the InstaflexTM dietary supplement in alleviating joint pain severity in middle-aged and older adults, with mitigation of difficulty performing daily activities most apparent in subjects with knee pain.Trial registration: ClinicalTrials.gov Identifier: NCT01956500.
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Objective: This study was undertaken to determine the effects of an ephedrine- and synephrine-based compound on body mass, body composition, metabolic variables, and mood states in healthy overweight adults.Methods: Thirty subjects with a body mass index > 27 kg/m2 were assigned randomly to the experimental group or the placebo group. The experimental group received a capsule containing ephedrine alkaloids 20 mg, synephrine 5 mg, caffeine 200 mg, and salicin 15 mg twice daily for 8 weeks, whereas the other group received a matching placebo. A registered dietitian instructed all patients about a 22-kcal/kg National Cholesterol Education Program Step One diet. In addition, all patients performed a cross-training exercise program 3 days per week under the guidance of an exercise physiologist. During the exercise sessions, patients achieved ∼70% of age-predicted maximum heart rate.Results: The experimental group had a significantly greater weight loss compared with the placebo group (3.14 kg vs 2.05 kg, respectively; P < 0.05). The experimental group experienced a 16% decrease in body fat compared with a 1% increase for the placebo group. The between-group difference was significant (P = 0.005). Both groups achieved a significant reduction in fat-free mass; however, the reduction in the placebo group was greater than that of the experimental group. This suggests a muscle-sparing effect in the experimental group. No significant changes in blood pressure, serial electrocardiograms, pulse rate, serum chemistry, or caloric intake were noted.Conclusions: These findings indicate the apparent safety and efficacy of the ephedrine- and synephrine-based compound within the confines of this study.
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Dear Editor, A 61-year-old female with the past medical history of hypertension and osteoarthritis presented to Emergency Department with sudden onset of shortness of breath and non-productive cough 30 min, after taking white willow bark supplement. The patient denied any history of the drug or supplement allergy. Pulse oximetry demonstrated oxygen desaturation; SpO2 of 75% on ambient air and 94% on nasal cannula with the flow of oxygen 20 L/min. Arterial blood gas although on FiO2 of 100% showed severe hypoxemia with the high A-a gradient, metabolic acidosis with respiratory compensation (pH 7.28, PCO2 36 mmHg, PaO2 75 mmHg, and HCO3 19 mmol/L). Blood tests demonstrated evidence of wide anion gap (AG) metabolic acidosis (AG 14 mmol/L) from lactic acidosis (lactic acid 4.9 mmol/L) with the normal gap metabolic acidosis (∆AG/∆Bicarb = 0.4) and the patient had no osmolal gap. Furthermore, serum ketone and salicylate levels were undetectable and her chest X-ray showed bilateral interstitial infiltrates [Figure 1]. Transthoracic echocardiogram revealed normal systolic and diastolic function. The diagnosis of acute hypoxic respiratory failure secondary to severe acute respiratory distress syndrome (ARDS) from reaction to white willow bark was made; the PaO2/FiO2 of 75 mmHg. The patient was promptly started on intravenous venous methylprednisolone and oral antihistamines including diphenhydramine and ranitidine. The patient responded well with our treatment and her oxygen requirement gradually improved from 94% on FiO2 of 100% to 95% on room air. Lactic acidosis also subsided after maintaining adequate oxygenation. Figure 1 Chest X-ray demonstrated bilateral interstitial infiltrates The use of white willow bark supplement was first reported back to the time of Hippocrates (400 BC) when patients were advised to chew on the bark for pain relief and fever reduction. Willow bark is also included in weight-loss products.[1] There have been a remarkably small number of reported cases of adverse reactions to willow bark extract. These adverse drug reactions are usually mild (maculopapular rashes). White willow bark induced anaphylaxis is rare; however, a few cases have been reported.[2,3] To our knowledge, this is the first report of white willow bark induced ARDS. People who are allergic or sensitive to salicylates (such as aspirin) should not use willow bark.
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Diabetic retinopathy is a complex condition where inflammation and oxidative stress represent crucial pathways in the pathogenesis of the disease. Aim of the study was to investigate the effects of a fortified extract of red berries, Ginkgo biloba and white willow bark containing carnosine and α-lipoic acid in early retinal and plasma changes of streptozotocin-induced diabetic rats. Diabetes was induced by a single streptozotocin injection in Sprague Dawley rats. Diabetics and nondiabetic (control) rats were treated daily with the fortified extract for the ten days. Retina samples were collected and analyzed for their TNF-α and VEGF content. Moreover, plasma oxidative stress was evaluated by thiobarbituric acid reacting substances (TBARS). Increased TNF-α and VEGF levels were observed in the retina of diabetic rats. Treatment with the fortified extract significantly lowered retinal cytokine levels and suppressed diabetes-related lipid peroxidation. These data demonstrate that the fortified extract attenuates the degree of retinal inflammation and plasma lipid peroxidation preserving the retina in early diabetic rats.
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JEPonline. 2001;4(2):28-34. The purpose was to determine the effects of an herbal preparation containing ma huang, bitter orange and guarana on resting energy expenditure (REE), blood chemistries, and body composition in obese adults. Five males and 15 females (age=31±6.6 yr, height=168.1 ±8.4 cm, weight=93.4±17.1 kg, %fat=43.8 ±6.5%) were matched, randomly assigned to either the supplement (N=12) or placebo (N=8) group, and participated in a 44 d aerobic exercise program (3 d/wk). REE was determined by open-circuit spirometry, and serum samples were analyzed for glucose, cholesterol, triglycerides, HDL, and LDL. Changes in body mass (BM), %fat, fat mass (FM), and fat-free mass (FFM) were determined using DEXA. Due to limited compliance, pre-and post-treatment diet recalls were analyzed for only 14 subjects (supplement=9, placebo=5). Analysis included doubly MANOVA repeated measures (diet recalls and blood chemistries) and independent t-tests (REE and body composition) at á<0.05. The only significant difference was in FM (p=0.033). When a more liberal alpha (á<0.10) is considered, %fat and BM were significant (p=0.096 and 0.087). The supplement, thus, may result in reductions in FM, %fat and BM, but has little effect on energy expenditure, diet or blood chemistries following a six-week period of supplementation and training.
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The aim of this study was to characterize the anti-inflammatory mode of action of botanical extracts from rosehip (Rosa canina), willow bark (Salix alba), and nettle leaf (Urtica dioica) in an in vitro model of primary canine articular chondrocytes. Methods. The biological effects of the botanical extracts were studied in chondrocytes treated with IL-1β for up to 72 h. Expression of collagen type II, cartilage-specific proteoglycan (CSPG), β1-integrin, SOX-9, COX-2, and MMP-9 and MMP-13 was examined by western blotting. Results. The botanical extracts suppressed IL-1β-induced NF-κB activation by inhibition of IκBα phosphorylation, IκBα degradation, p65 phosphorylation, and p65 nuclear translocation. These events correlated with downregulation of NF-κB targets including COX-2 and MMPs. The extracts also reversed the IL-1β-induced downregulation of collagen type II, CSPG, β1-integrin, and cartilage-specific transcription factor SOX-9 protein expression. In high-density cultures botanical extracts stimulated new cartilage formation even in the presence of IL-1β. Conclusions. Botanical extracts exerted anti-inflammatory and anabolic effects on chondrocytes. The observed reduction of IL-1β-induced NF-κB activation suggests that further studies are warranted to demonstrate the effectiveness of plant extracts in the treatment of OA and other conditions in which NF-κB plays pathophysiological roles.
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To establish whether acetaminophen improves performance of self-paced exercise through the reduction of perceived pain, 13 trained male cyclists performed a self-paced 10-mile (16.1 km) cycle time trial (TT) following the ingestion of either acetaminophen (ACT) or a placebo (PLA), administered in randomized double-blind design. TT were completed in a significantly faster time (t(12) = 2.55, P < 0.05) under the ACT condition (26 min 15 s +/- 1 min 36 s vs. 26 min 45 s +/- 2 min 2 s). Power output (PO) was higher during the middle section of the TT in the ACT condition, resulting in a higher mean PO (P < 0.05) (265 +/- 12 vs. 255 +/- 15 W). Blood lactate concentration (B[La]) and heart rate (HR) were higher in the ACT condition (B[La] = 6.1 +/- 2.9 mmol/l; HR = 87 +/- 7%max) than in the PLA condition (B[La] = 5.1 +/- 2.6 mmol/l; HR = 84 +/- 9%max) (P < 0.05). No significant difference in rating of perceived exertion (ACT = 15.5 +/- 0.2; PLA = 15.7 +/- 0.2) or perceived pain (ACT = 5.6 +/- 0.2; PLA = 5.5 +/- 0.2) (P > 0.05) was observed. Using acetaminophen, participants cycled at a higher mean PO, with an increased HR and B[La], but without changes in perceived pain or exertion. Consequently, completion time was significantly faster. These findings support the notion that exercise is regulated by pain perception, and increased pain tolerance can improve exercise capacity.
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This study compared independent effects of caffeine and aspirin on muscular endurance (repetitions), heart rate (HR), perceived exertion (RPE), and perceived pain index (PPI) during light resistance training bouts performed to volitional failure. It was hypothesized that the hypoalgesic properties of these ergogenic aids would decrease pain perception and potentially result in enhanced performance. College-aged men (n = 15) participated in a within-subjects, double-blind study with three independent, counterbalanced sessions wherein aspirin (10 mg x kg(-1)), caffeine (6 mg x kg(-1)), or matched placebo were ingested 1 hour before exercise, and RPE, HR, PPI, and repetitions (per set and total per exercise) were recorded at 100% of individual, predetermined, 12-repetition maximum for leg extensions (LE) and seated arm curls (AC). Repeated-measures analyses of variance were used for between-trial comparisons. Caffeine resulted in significantly greater (p < 0.05) HR (LE and AC), total repetitions (LE), and repetitions in set 1 (LE and AC) compared with aspirin and placebo. Aspirin resulted in significantly higher PPI in set 1 (LE). In LE, 47% of participants' performance exceeded the predetermined effect size (>or= 5 repetitions) for total repetitions, with 53% exceeding the effect size (>or= 2 repetitions) for repetitions in set 1 with caffeine (vs. placebo). In AC, 53% (total repetitions) and 47% (set 1 repetitions) of participants exceeded effect sizes with caffeine (vs. placebo), with only 13% experiencing decrements in performance (total repetitions). Aspirin also produced a higher PPI and RPE overall and in set 1 (vs. placebo). This study demonstrates that caffeine significantly enhanced resistance training performance in LE and AC, whereas aspirin did not. Athletes may improve their resistance training performance by acute ingestion of caffeine. As with most ergogenic aids, our analyses indicate that individual responses vary greatly.
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To investigate the efficacy and safety of a standardized willow bark extract in patients with osteoarthritis (OA) and rheumatoid arthritis (RA). We studied 127 outpatients with hip or knee OA and a WOMAC pain score of at least 30 mm and 26 outpatients with active RA in 2 randomized, controlled, double-blind trials with followup for 6 weeks. OA trial: Patients were randomized to receive willow bark extract, corresponding to 240 mg of salicin/day, diclofenac 100 mg/day, or placebo (n = 43, 43, and 41, respectively). Main outcome measure was the pain subscore of the WOMAC OA Index. RA trial: Patients were randomized to receive willow bark extract, corresponding to 240 mg salicin/day (n = 13) or placebo (n = 13). Main outcome measure was the patient's assessment of pain rated on a 100 mm visual analog scale (VAS). OA trial: WOMAC pain scores decreased by 8 mm (17%) in the willow bark group and by 23 mm (47%) in the diclofenac group, compared with 5 mm (10%) in the placebo group. The difference between willow bark extract and placebo was not statistically significant (-2.8 mm; 95% CI -12.1 to 6.4 mm; p = 0.55, ANCOVA), but the difference between diclofenac and placebo was highly significant (-18.0 mm; 95% CI -27.2 to -8.8 mm; p = 0.0002, ANCOVA). RA trial: The mean reduction of pain on the VAS was -8 mm (15%) in the willow bark group compared with -2 mm (4%) in the placebo group. The difference was not statistically significant (estimated difference -0.8 mm; 95% CI -20.9 to 19.3 mm; p = 0.93, ANCOVA). The OA study suggested that the willow bark extract showed no relevant efficacy in patients with OA. Similarly, the RA trial did not indicate efficacy of this extract in patients with RA.
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To report a case of anaphylaxis resulting from the use of a willow bark-containing dietary supplement in a patient with a history of an aspirin allergy. A 25-year-old white woman presented to the emergency department of a community teaching hospital with anaphylaxis requiring epinephrine, diphenhydramine, methylprednisolone, and volume resuscitation to which she responded favorably. Medication history revealed that she had ingested 2 capsules of Stacker 2 (NVE Pharmaceuticals, Newton, NJ), a dietary supplement promoted for weight loss, prior to experiencing her initial symptoms. Among other active ingredients, this product contains willow bark. Of significance is that this patient also reported a history of allergy to acetylsalicylic acid. No other causes for anaphylaxis were identified. She continued to receive routine supportive care and the remaining hospital course was uncomplicated. Dietary supplements, including herbal products, are used by many individuals who consider them to be inherently safe despite limited regulatory oversight by the Food and Drug Administration. While there may be value to specific botanical ingredients, a potential for adverse effects also exists. The popular product consumed by our patient is used for weight loss and contains willow bark, a source of salicylates. Based on the Naranjo probability scale, it is probable that this case of anaphylaxis was due to this dietary supplement. The use of any willow bark-containing dietary supplement may present a risk of anaphylactic reaction to patients with a history of allergy to salicylates. Clinicians need to recognize the potential for adverse effects from dietary supplements.
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Many higher plants contain novel metabolites with antimicrobial, antifungal and antiviral properties. However, in the developed world almost all clinically used chemotherapeutics have been produced by in vitro chemical synthesis. Exceptions, like taxol and vincristine, were structurally complex metabolites that were difficult to synthesize in vitro. Many non-natural, synthetic drugs cause severe side effects that were not acceptable except as treatments of last resort for terminal diseases such as cancer. The metabolites discovered in medicinal plants may avoid the side effect of synthetic drugs, because they must accumulate within living cells. The aim here was to test an aqueous extract from the young developing leaves of willow (Salix safsaf, Salicaceae) trees for activity against human carcinoma cells in vivo and in vitro. In vivo Ehrlich Ascites Carcinoma Cells (EACC) were injected into the intraperitoneal cavity of mice. The willow extract was fed via stomach tube. The (EACC) derived tumor growth was reduced by the willow extract and death was delayed (for 35 days). In vitro the willow extract could kill the majority (75%-80%) of abnormal cells among primary cells harvested from seven patients with acute lymphoblastic leukemia (ALL) and 13 with AML (acute myeloid leukemia). DNA fragmentation patterns within treated cells inferred targeted cell death by apoptosis had occurred. The metabolites within the willow extract may act as tumor inhibitors that promote apoptosis, cause DNA damage, and affect cell membranes and/or denature proteins.
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The efficacy of willow bark extract in the treatment of painful mobility disorders, such as back pain and arthritis, has been attributed to the content of salicin and its derivatives as pro-drugs of salicylates. However, based on clinical experience and the evidence of experimental pharmacological studies, the fraction of total salicin cannot satisfactorily explain the clinical efficacy of willow bark. In addition, salicins and their metabolites lack the acetylating potential of ASA and must therefore possess a different mechanism of action. A detailed pharmacological screening of the aqueous willow bark extract STW 33-I addressed the question of the identification of fractions contributing to the overall effect. All in vivo and in vitro models studied pointed to relevant contributions of the fraction of polyphenols and flavonoids. The single compounds or their combinations responsible for the effect remain to be elucidated.
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What is already known about this subject: Performance-enhancing dietary supplements have not been clinically tested for safety or efficacy. In clinical trials performed under resting conditions, performance-enhancing supplements raise blood pressure and affect glucose homeostasis. The effect of exercise on the pharmacokinetics and pharmacodynamics of stimulant herbals is unknown. What this study adds: Supplement-induced effects on blood pressure and glucose levels are not ameliorated by exercise. Exercise does not affect the kinetics of stimulant ingredients, caffeine and synephrine. Performance-enhancing supplement use modestly improves exercise tolerance. AIMS Dietary supplements (DS) promoted to enhance athletic performance often contain herbal sympathomimetics such as Citrus aurantium (synephrine) and caffeine. We aimed to characterize the pharmacology of a performance-enhancing DS in the setting of exercise. Methods: Ten healthy adults (three women) aged 20-31 years participated in a three-arm, double-blind, placebo-controlled, crossover study. Subjects ingested one dose of DS (Ripped Fuel Extreme Cut(R) with 21 mg synephrine and 304 mg caffeine by analysis) under resting conditions and 1 h prior to moderately intense exercise (30 min on cycle ergometer at 75-80% HR(max)), with a placebo (PLC)/exercise control. Plasma synephrine and caffeine concentrations were measured over 12 h, and vital signs, serum electrolytes, oxygen consumption and perceived exercise exertion were monitored. Results: No significant adverse events occurred. Synephrine and caffeine pharmacokinetics were unaffected by exercise. Post-exercise diastolic blood pressure was higher after DS (peak mean 71.7 +/- 8.7 mmHg) than PLC (63.0 +/- 4.9 mmHg) (p = 0.007). There were no substantial treatment-related differences in post-exercise HR, systolic blood pressure, or temperature. Postprandial plasma glucose increased to 121.0 +/- 31.6 mg dl(-1) with DS and exercise vs. 103.7 +/- 25.5 mg dl(-1) with PLC and exercise (P = 0.004). No treatment differences in exercise-related oxygen consumption, serum lactate, or insulin were observed. Exercise was rated less difficult with DS than PLC (P = 0.001). Conclusions: Blood pressure and plasma glucose increased post-exercise with DS use, which could be detrimental in some people. Exercise was perceived as less strenuous after DS, presumably due to the stimulant effects of caffeine.
Article
Objective. To investigate the efficacy and safety of a standardized willow bark extract in patients with osteoarthritis (OA) and rheumatoid arthritis (RA). Methods. We studied 127 outpatients with hip or knee OA and a WOMAC pain score of at least 30 mm and 26 outpatients with active RA in 2 randomized, controlled, double-blind trials with followup for 6 weeks. OA trial: Patients were randomized to receive willow bark extract, corresponding to 240 mg of salicin/day, diclofenac 100 mg/day, or placebo (n = 43, 43, and 41, respectively). Main outcome measure was the pain subscore of the WOMAC OA Index. RA trial: Patients were randomized to receive willow bark extract, corresponding to 240 mg salicin/day (n = 13) or placebo (n = 13). Main outcome measure was the patient's assessment of pain rated on a 100 mm visual analog scale (VAS). Results. OA trial: WOMAC pain scores decreased by 8 mm (17%) in the willow bark group and by 23 turn (47%) in the diclofenac group, compared with 5 mm (10%) in the placebo group. The difference between willow bark extract and placebo was not statistically significant (-2.8 mm; 95% CI -12.1 to 6.4 mm; p = 0.55, ANCOVA), but the difference between diclofenac and placebo was highly significant (-18.0 mm; 95% CI -27.2 to -8.8 mm; p = 0.0002, ANCOVA). RA trial: The mean reduction of pain on the VAS was -8 turn (15%) in the willow bark group compared with -2 mm (4%) in the placebo group. The difference was not statistically significant (estimated difference -0.8 mm; 95% CI -20.9 to 19.3 mm; p = 0.93, ANCOVA). Conclusion. The OA study suggested that the willow bark extract showed no relevant efficacy in patients with OA. Similarly, the RA trial did not indicate efficacy of this extract in patients with RA.
Article
Study objective: Efficacy and safety of willow bark extract for pain reduction in patients suffering from musculoskeletal disorders (MSD) has been shown in clinical short term trials. Therefore this observational study over 6 months should evaluate patterns of treatments like mono- or combinations therapy, dosage and safety during long-term treatment under pragmatic conditions with the aqueous willow bark extract STW 33-I, (Proaktiv(®); drug-extract-ratio 16-23:1). Patients and methods: The patients were treated with STW 33-I; comedication with other NSAIDs and opioids was allowed. An extensive case report form including pain questionnaires and patient diary was used for outcome evaluation. Results: Four hundred and thirty-six patients with rheumatic pain mainly due to osteoarthritis (56.2%) and back pain (59.9%) were included. During the study the mean reductions from baseline value 58.4±22.6-31.8±22.5 after 24 weeks in the pain intensity scale (VAS 0-100mm) were significant even after 3 weeks with a reduction by 26 mm (45.6% of the baseline value) at the end of the study. The relative reductions of the weekly means of the daily patient self-rated scores of the pain (6-point Likert-scales) were between 33% and 44% of the baseline values during the course of the study. We present results of subgroups according their analgetic/antiphlogistic comedication. The distribution and specification of the main adverse events and the ratings of the treatment showed a good tolerability. No relevant drug interactions were reported. Conclusion: These data suggest that STW 33-I can be used as a basic treatment in the long-term therapy of painful musculoskeletal disorders and that it can be combined with NSAIDs and opioids if necessary.
Article
Willow bark extract (WBE) is listed in the European Pharmacopoeia and has been traditionally used for treating fever, pain and inflammation. Recent studies have demonstrated its clinical usefulness. This study investigated the antioxidative effects of WBE in human umbilical vein endothelial cells (HUVECs) and Caenorhabditis elegans. WBE prevented oxidative-stress-induced cytotoxicity of HUVECs and death of C. elegans. WBE dose-dependently increased mRNA and protein expression levels of the nuclear factor erythroid 2-related factor 2 (Nrf2) target genes, heme oxygenase-1, γ-glutamyl-cysteine ligase modifier and catalytic subunits, and p62, and intracellular glutathione (GSH) in HUVECs. In the nematode C. elegans, WBE increased the expression of the gcs-1::green fluorescent protein (GFP) reporter, a well-characterized target of the Nrf2 ortholog SKN-1, in a manner that was SKN-1-dependent. WBE increased intranuclear expression and DNA binding of Nrf2, and activity of an antioxidant response element (ARE) reporter plasmid in HUVECs. WBE-induced expression of Nrf2-regulated genes, and increased GSH levels in HUVECs were reduced by Nrf2 and p38 small interfering (si)RNAs, and by the p38-specific inhibitor SB203580. Nrf2 siRNA reduced the cytoprotective effect of WBE against oxidative stress in HUVECs. Salicin, a major anti-inflammatory ingredient of WBE, failed to activate ARE-luciferase activity, while a salicin-free WBE fraction showed intensive activity. WBE induced antioxidant enzymes and prevented oxidative stress through activation of Nrf2 independently of salicin, providing a new potential explanation for the clinical usefulness of WBE.
Article
Here, proof-of-concept of a new analytical platform used for the comprehensive analysis of a small set of commercial willow bark products is presented, and compared with a traditional standardization solely based on analysis of salicin and salicin derivatives. The platform combines principal component analysis (PCA) of two chemical fingerprints, i.e., HPLC and (1)H NMR data, and a pharmacological fingerprint, i.e., high-resolution 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) radical cation (ABTS(+)) reduction profile, with targeted identification of constituents of interest by hyphenated HPLC-solid-phase extraction-tube transfer NMR, i.e., HPLC-SPE-ttNMR. Score plots from PCA of HPLC and (1)H NMR fingerprints showed the same distinct grouping of preparations formulated as capsules of Salix alba bark and separation of S. alba cortex. Loading plots revealed this to be due to high amount of salicin in capsules and ampelopsin, taxifolin, 7-O-methyltaxifolin-3'-O-glucoside, and 7-O-methyltaxifolin in S. alba cortex, respectively. PCA of high-resolution radical scavenging profiles revealed clear separation of preparations along principal component 1 due to the major radical scavengers (+)-catechin and ampelopsin. The new analytical platform allowed identification of 16 compounds in commercial willow bark extracts, and identification of ampelopsin, taxifolin, 7-O-methyltaxifolin-3'-O-glucoside, and 7-O-methyltaxifolin in S. alba bark extract is reported for the first time. The detection of the novel compound, ethyl 1-hydroxy-6-oxocyclohex-2-enecarboxylate, is also described.
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Antiinflammatory compounds in the diet can alleviate excessive inflammation, a factor in the pathogenesis of common diseases such as rheumatoid arthritis, atherosclerosis and diabetes. This study examined three European herbs, chamomile (Matricaria chamomilla), meadowsweet (Filipendula ulmaria L.) and willow bark (Salix alba L.), which have been traditionally used to treat inflammation and their potential for use as antiinflammatory agents. Aqueous herbal extracts and isolated polyphenolic compounds (apigenin, quercetin and salicylic acid, 0-100 μM) were incubated with THP1 macrophages, and interleukin (IL)-1β, IL-6 and tumour necrosis factor-alpha (TNF-α) were measured. At concentrations of 10 μM, both apigenin and quercetin reduced IL-6 significantly ( p < 0.05). Apigenin at 10 μM and quercetin at 25 μM reduced TNF-α significantly ( p < 0.05). Amongst the herbal extracts, willow bark had the greatest antiinflammatory activity at reducing IL-6 and TNF-α production. This was followed by meadowsweet and then chamomile. The lowest effective antiinflammatory concentrations were noncytotoxic (MTT mitochondrial activity assay). The Comet assay, which was used to study the protective effect of the isolated phenols against oxidative damage, showed positive results for all three polyphenols. These are the first findings that demonstrate the antiinflammatory capacity of these herbal extracts. Copyright © 2012 John Wiley & Sons, Ltd.
Article
A quantified aqueous Willow bark extract (STW 33-I) was tested concerning its inhibitory activity on TNF-α induced ICAM-1 expression in human microvascular endothelial cells (HMEC-1) and further fractionated to isolate the active compounds. At 50 μg/ml the extract, which had been prepared from Salix purpurea L., decreased ICAM-1 expression to 40% compared to control cells without showing cytotoxic effects. Further liquid-liquid partition revealed an ethyl acetate phase with potent reduction of ICAM-1 expression to 40% at 8 μg/ml. This fraction was comprehensively characterised by the isolation of flavanone aglyca and their corresponding glycosides, chalcone glycosides, salicin derivatives, cyclohexane-1,2-diol glycosides, catechol and trans-p-coumaric acid. All compounds were investigated for their activity on TNF-α induced ICAM-1 expression. The flavonoid and chalcone glycosides were not active up to 50 μM, whereas catechol and eriodictyol at the same concentration showed a significant reduction of ICAM-1 expression to 50% of control. Interestingly, other isolated flavanone aglyca like taxifolin, dihydrokaempferol and naringenin showed only weak or moderate inhibitory activity. Eriodictyol was a minor compound in the extract, whereas the catechol content in the extract (without excipients) reached 2.3%, determined by HPLC. One of the isolated cyclohexan-1,2-diol glucosides, 6'-O-4-hydroxybenzoyl-grandidentin, is a new natural compound. As catechol is quantitatively important in Willow bark extracts it can be concluded from the in vitro data that not only flavonoids and salicin derivatives, but also catechol can probably contribute to the anti-inflammatory activity of Willow bark extracts.
Article
Willow bark extract is frequently used in the treatment of painful rheumatological diseases, such as arthritis and back pain. Its effect has been attributed to its main component salicin, but pharmacological studies have shown that the clinical efficacy of the willow bark extract cannot be explained by its salicin content alone. Therefore different modes of action have been suggested for the anti-inflammatory effect of willow bark extract. Here, we report in vitro data revelling the effect and mode of action of the aqueous willow bark extract STW 33-I as well as a water-soluble fraction (fraction E [Fr E]) in comparison with well-known non-steroidal anti-inflammatory drugs (NSAIDs) like aspirin (ASA) and diclofenac (Diclo) on pro-inflammatorily activated human monocytes and differentiated macrophages. STW 33-I and the water-soluble Fr E showed concentration-dependent and significant anti-inflammatory effects in lipopolysaccharide-activated monocytes. Both inhibited the intracellular protein expression of tumour necrosis factor-alpha (TNFα) as well as the mRNA expression of TNFα and cyclooxygenase 2 (COX-2), and the release of nitric oxide (NO). In addition, apoptosis of pro-inflammatorily activated monocytes was induced. Furthermore, treatment of activated macrophages with STW 33-I inhibited the nuclear translocation of the p65 subunit of the nuclear transcription factor-kappa B (NF-κB p65). The present in vitro investigations suggest a significant anti-inflammatory activity of willow bark water extract STW 33-1 and of its water-soluble fraction by inhibiting pro-inflammatory cytokines (TNFα), COX-2 and nuclear translocation of the transcription factor NF-κB in pro-inflammatorily activated monocytes. Our results provide further evidence for the therapeutic use of STW 33-I in inflammation-related disorders.
Article
The present study examined the skeletal muscle expression of several genes related to the inflammatory process before and after a bout of downhill running. Twenty-nine males between the ages of 18 and 35 years performed a 45-min downhill (-17.5%) treadmill protocol at 60% of maximal oxygen consumption. Venous bloods samples and muscle biopsy samples from the vastus lateralis were donated prior to and at 3-h and 24-h postexercise, along with ratings of perceived muscle soreness. Serum creatine kinase (CK) was determined, as was skeletal muscle gene expression of interleukin (IL)-6, IL-8, IL-12 (p35), tumor necrosis factor-alpha (TNF-alpha), IL-1beta, cyclooxygenase 2 (COX2), and nuclear factor kappa B (NFkB) (p105/p50). Gene expression was analyzed using RT-PCR and compared with a standard housekeeping gene (beta-actin). Data were analyzed for statistical differences using multivariate analysis of variance with univariate follow-up. In addition, Pearson correlations were conducted to determine if any significant relationship exists between any of these transcripts and both CK and muscle soreness. Significant (p < 0.05) up-regulations in IL-6, IL-8, and COX2 mRNA expression were observed compared with baseline, whereas no significant changes for IL-12, IL-1beta, TNF-alpha, or NFkB were noted. Significant increases in IL-6 mRNA were observed at 3 h (p < 0.001) and 24 h (p = 0.043), whereas significant increases in IL-8 (p = 0.001) and COX2 (p = 0.046) mRNA were observed at 3-h postexercise. In addition, muscle soreness was significantly correlated with IL-8 at 24 h (r = -0.370; p = 0.048), whereas CK was significantly related to NFkB at baseline (r = -0.460; p = 0.012). These data indicate that increases in the mRNA expression of IL-6, IL-8, and COX2 occur in the vastus lateralis as a result of damaging eccentric exercise in young, recreationally trained males. Further, it appears that IL-8 transcription may play some role in inhibiting postexercise muscle soreness, possibly through regulation of angiogenesis.
Article
Since ancient times preparations from Salix species have been used to alleviate pain. The aim of this study was to update the evidence of the effectiveness of willow bark products in the treatment of musculoskeletal pain. OVID(MEDLINE), PUBMED, Silverplatter, and CENTRAL and manual searches were used to identify clinical trials investigating Salix preparations. Authors SC and JEV extracted the data independently and discussed disagreements. Seven manuscripts were identified, reporting four trials with confirmatory and four with exploratory study designs. Three manuscripts presented the same trial data: repetitious reports were excluded. One confirmatory and two exploratory studies indicate a dose-dependent analgesic effect not inferior to rofecoxib in patients with low back pain. In one exploratory and one confirmatory study conflicting results were achieved in participants with osteoarthritis. No significant effect was seen in a confirmatory study in patients with rheumatoid arthritis, but this study was grossly underpowered. All studies investigated ethanolic extracts with daily doses up to 240 mg salicin over periods of up to six weeks. Minor adverse events occurred during treatment. The review provides moderate evidence of effectiveness for the use of ethanolic willow bark extract in low back pain. Further studies are required to find out if treatment of osteoarthritis and rheumatoid arthritis requires extract with higher doses than 240 mg salicin per day. Copyright
Article
The enzymatic catalysis of the decomposition of Salicaceae phenolic glucosides was tested using almond beta-glucosidase and rabbit and porcine liver esterases. The beta-glucosidase catalyzed the complete hydrolysis of salicin and salicortin, yielding saligenin and glucose. Salicortin also produced (+)-6-hydroxycyclohexen-2-one (6-HCH). The acylglucosides were not decomposed by the beta-glucosidase. Both esterases catalyzed the decomposition of tremulacin, salicortin, and 2'-O-acetylsalicortin, releasing tremuloidin, salicin, and 2'-O-acetylsalicin as the main products, accompanied by 6-HCH and catechol. Tremuloidin and 2'-O-acetylsalicin were quite stable under the esterase hydrolysis, and salicin was not decomposed at all.
Article
Leiocarposide (1; 3-beta-D-glucopyranosyloxy-2-methoxy-6-hydroxy-benzoic acid -2'-beta-D-glucopyranosyloxybenzyl ester) is a phenolic glycoside from Solidago virgaurea L. After oral administration to rats it will be only poorly absorbed and mostly unchanged fecaly excreted. In the urine were found less than 10% as metabolites: leiocarpic acid (3; 3,6-dihydroxy-2-methoxy-benzoic acid, 2% of the administered dose), 3-conjugates (2%), salicylic acid (5; 0.5%), 5-conjugates (0.1%) and salicyluric acid (6; 0.5%). On the other hand salicin (2), structural part of 1, is good absorbed. In the urine were excreted 15% of the unchanged drug and the following metabolites: 0.1% saligenin (4), 30% 5, 5% 5-conjugates, 0.1% 6, 2% gentisic acid (7) and 0.1% 2,3-dihydroxy-benzoic acid (8). The different metabolic rates are explicable by the high stability of the ester bond of 1. It is hydrolyzed in artificial intestinal fluid only very slowly (t1/2 = 41.7 h).
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Herbal medicines are widely used for the treatment of pain, although there is not much information on their effectiveness. This study was designed to evaluate the effectiveness of willow (Salix) bark extract, which is widely used in Europe, for the treatment of low back pain. We enrolled 210 patients with an exacerbation of chronic low back pain who reported current pain of 5 or more (out of 10) on a visual analog scale. They were randomly assigned to receive an oral willow bark extract with either 120 mg (low dose) or 240 mg (high dose) of salicin, or placebo, with tramadol as the sole rescue medication, in a 4-week blinded trial. The principal outcome measure was the proportion of patients who were pain-free without tramadol for at least 5 days during the final week of the study. The treatment and placebo groups were similar at baseline in 114 of 120 clinical features. A total of 191 patients completed the study. The numbers of pain-free patients in the last week of treatment were 27 (39%) of 65 in the group receiving high-dose extract, 15 (21%) of 67 in the group receiving low-dose extract, and 4 (6%) of 59 in the placebo group (P <0.001). The response in the high-dose group was evident after only 1 week of treatment. Significantly more patients in the placebo group required tramadol (P <0.001) during each week of the study. One patient suffered a severe allergic reaction, perhaps to the extract. Willow bark extract may be a useful and safe treatment for low back pain.
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This study assessed the clinical efficacy of a chemically standardized willow bark extract in the treatment of osteoarthritis. Willow bark extract, in a dose corresponding to 240 mg salicin/day, was compared with placebo in a 2-week, double-blind, randomized controlled trial. The primary outcome measure was the pain dimension of the WOMAC Osteoarthritis Index. Secondary outcome measures included the stiffness and physical function dimensions of the WOMAC, daily visual analogue scales (VAS) on pain and physical function, and final overall assessments by both patients and investigators. A total of 78 patients (39 willow bark extract, 39 placebo) participated in the trial. A statistically significant difference between the active treatment and the placebo group was observed in the WOMAC pain dimension (d = 6.5 mm, 95% C.I. = 0.2-12.7 mm, p = 0.047); the WOMAC pain score was reduced by 14% from the baseline level after 2 weeks of active treatment, compared with an increase of 2% in the placebo group. The patient diary VAS confirmed this result, and likewise the final overall assessments showed superiority of the willow bark extract over the placebo (patients' assessment, p = 0.0002; investigators' assessment, p = 0.0073). It is concluded that the willow bark extract showed a moderate analgesic effect in osteoarthritis and appeared to be well tolerated.
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We show that high doses of salicylates reverse hyperglycemia, hyperinsulinemia, and dyslipidemia in obese rodents by sensitizing insulin signaling. Activation or overexpression of the IκB kinase β (IKKβ) attenuated insulin signaling in cultured cells, whereas IKKβ inhibition reversed insulin resistance. Thus, IKKβ, rather than the cyclooxygenases, appears to be the relevant molecular target. Heterozygous deletion (Ikkβ +/−) protected against the development of insulin resistance during high-fat feeding and in obese Lepob/ob mice. These findings implicate an inflammatory process in the pathogenesis of insulin resistance in obesity and type 2 diabetes mellitus and identify the IKKβ pathway as a target for insulin sensitization.