Article

Anti-inflammatory and antimicrobial activity of Sideritis scardica extracts

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  • Institute for Medicinal Plant Research "Dr. Josif Pancic"
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... Des Weiteren wurde über Mineralstoffe (Na, K, Ca, Mg, Fe, Zn, Mn) im ppm-Bereich und Spuren von toxischen Inhaltsstoffen wie z. B. Blei, Cadmium und Arsen berichtet, welche jedoch in den traditionellen Zubereitungen, wie Tee oder Tinkturen, nicht nachweisbar sind (Karapandzova et al., 2013;Zarkovic, 1993 (Kostadinova et al., 2008;Mihaylova et al., 2014;Proestos et al., 2013;Tadic et al., 2007;2012). ...
... In vivo erreichten Ether-und n-Butanol-Fraktionen eines 70 % ethanolischen Extraktes in Dosen von 200 bzw. 100 mg/kg den gleichen Effekt wie 4 mg/kg Indometacin (Carrageenaninduziertes Rattenpfoten-Ödem) (Tadic et al., 2007;2012). ...
... kommt also nicht in Frage. Eine Beteiligung von antiinflammatorischen Eigenschaften des Griechischen Bergtees (Tadic et al., 2007;2012) ist prinzipiell denkbar und wurde nicht direkt getestet, ist aber im Fadenwurmmodell sehr fragwürdig, da C. elegans zwar über ein paar innate Infektionsabwehrmechanismen wie Lysozym verfügt, aber durch das Fehlen von Makrophagen, Astrozyten, einer Mikroglia und einem adaptiven Immunsystem die Komplexität einer (Neuro)-Inflammation nicht abbilden kann und die in den Säugetieren beobachteten entzündungshemmenden Mechanismen in den Würmern vermutlich gar nicht greifen (Gregory und Devitt, 2004;Mallo et al., 2002;Richardson et al., 2010). Die von Hofrichter et al. (2016) gezeigte erhöhte phagozytotische Aktivität der Mikroglia kommt also bei C. elegans nicht in Betracht, ebensowenig die erhöhte Expression von ADAM10 als Grund für die verringerte Aβ-Last; allgemein scheiden die Inhibition oder Induktion von Sekretasen als Ursache der Neuroprotektion im Wurmmodell aus, da hier humanes Aβ nicht durch Prozessierung von APP, sondern durch das Exprimieren eines eingeschleusten Minigens produziert wird. ...
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Sideritis scardica Griseb., also known as Greek mountain tea, is a plant that belongs to the family of Lamiaceae. It is endemic to the Balkan region, where the herb is traditionally used against a broad range of afflictions, mostly as an infusion. Over the past few years, S. scardica has been scientifically investigated for the pharmacological properties it is said to have, especially focusing on the effects in the central nervous system, such as an improved cognitive performance and the reduction of β-amyloid plaques which are typical in Alzheimer's disease. Following this issue, the main goal of the present study was to examine whether extracts of Greek mountain tea counteract further pathomechanisms of this and other neurodegenerative disorders which are a rising health concern in our ageing society. For this purpose six hydroalcoholic S. scardica extracts of different lipophilicity, that were produced and phytochemically analysed by Finzelberg GmbH & Co. KG, were investigated for their neuroprotective activity in the model organism Caenorhabditis elegans. Additionally, six fractions of one of the most potent extracts, seven isolated pure compounds and extracts of some well-known medicinal plants were tested. The mid-polar extracts of S. scardica in particular, as well as the more lipophilic fractions and the phenylethanoid glycosides, were counteracting the aggregation or toxicity of β-amyloid peptides, α-synuclein, 6-hydroxydopamine, tau- and polyglutamine proteins in vivo, whereas they did not reveal any antioxidant properties in the nematodes. The spectrum of activities of S. scardica was especially comparable with that of Bacopa monnieri (Brahmi), a plant used in ayurvedic medicine. The alleviation of the neurotoxicity of the proteins and compounds make S. scardica extracts interesting for the preventive or therapeutic treatment of Alzheimer's, Parkinson's, Huntington's and other neurodegenerative diseases. The phenylethanoids could be identified as active constituents, although synergistic effects between extractives of different polarity remain probable and have to be taken into consideration. Also, a hypothetical mode of action could be postulated: the bonding of polyphenols to the peptides, directly inhibiting their aggregation to toxic oligomers or plaques and fibrils. In the present study, the activity of hydroalcoholic Sideritis scardica extracts against hallmarks of Alzheimer's disease could be affirmed and for the first time, positive effects on further neurotoxic substances could be shown, expanding the neuropharmacological profile of the Greek mountain tea. As some studies on vertebrates and humans assessing the influence on cognitive performance and proving the harmlessness have already been conducted, high-quality clinical studies investigating the preventive or therapeutic efficacy against Alzheimer's etc. should be performed.
... Tadić et al. [102] showed that ethanol extract of S. scardica and its fractions (ethanol ether, ehylacetate and n-butanol) exhibit antimicrobial activity against seven strains of microorganismssix bacteria and one fungus. The most active fraction appeared to be the one of n-butanol, acting on Staphylococcus epidermidis. ...
... Seven species demonstrated fungicidal activity [31,39,40,102,103]. ...
... A large part of the substances found in Sideritis species possess prononced anti-inflammatory activity. Tadić et al. [102,104,151] proved this activity in ethanolic extract and fractions (diethyl ether, ethyl acetate and n-butanol) of S. scardica. ...
Article
Background: Over the last two decades there has been a substantial increase of the number of studies on the species of genus Sideritis. Species of section Empedoclia, occurring in the Eastern Mediterranean region and in part of Western Asia possess some remarkable characteristics and are known as valuable medicinal plants used by local people in the traditional medicine and for herbal tea. The objective of the review is to make a survey on the recent studies on the ethnopharmacology and biological activity of the species in Southeastern Europe and in Turkey, which is the center of distribution and their main occurrence. Main body: The review focuses to the ethnopharmacological studies and on biological activities of the species of interest. The numerous phytochemical studies were not considered for this review, except in the cases when combined with the target issues. The survey revealed that total 47 species belonging to section Empedoclia have been studied either in ethnopharmacological aspect, or in relation to their biological activities, or both. Most species have been used traditionally by the local people as herbal tea or for treatment various health problems, most frequently flu, cold and respiratory diseases. The species demonstrate numerous biological activities and are promising for use in the therapy of many diseases and health disorders. Antioxidant activity was found in 40 species, antimicrobial and antibacterial activity – in 27 species, anti-inflammatory – in 14 species, antifungal – in 8 species, cytotoxic – in 7 species. There were also some other, more specific biological activities, found in a few species, but considered promising for further studies and application. Short conclusion: The species of genus Sideritis, section Empedoclia have been used by local people as herbal tea and in traditional medicine since long time ago. People are taking advantage of the high species diversity are aware of their useful properties. Much more information is available about the biological activities of the target species than about their traditional uses. Most species demonstrate various biological activities and are of substantial interest for further studies on their pharmacological properties and their potential for pharmacy and medicine.
... The ethanol extract and its ethyl ether, ethyl acetate, and nbutanol fractions were also examined for their antimicrobial activity using the following laboratory strains of microorganisms: Staphylococcus epidermidis, Micrococcus luteus, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and yeast Candida albicans (Tadić et al., 2007). The investigated samples exhibited antimicrobial activity of varying degrees against all the tested strains. ...
... Indometacin was used as a standard. Compared to indomethacine (4 mg/kg) which caused 50% decrease of inflammation, diethyl ether and n-butanol extracts exhibited almost the same effect in doses 200 and 100 mg/kg (53.6 and 48.7%; 48.4 and 49.9%, respectively) (Tadić et al., 2007(Tadić et al., , 2012. ...
... None of the tested extracts showed significant cytotoxicity against rat astrocytes in primary culture. Koleva et al. (2003) 2,2ʹ-Diphenyl-1-picryl hydrazyl (DPPH ) radical scavenging method Koleva et al. (2003), Tadić et al. (2008Tadić et al. ( , 2012, and Karapandzova et al. (2013) ABTS (2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)) method Ivanova et al. (2005) Anti-inflammatory Carrageenan-induced rat's paw oedema test Tadić et al. (2007Tadić et al. ( , 2012 (2012) Influence on memory Morris water maze Bjoern et al. (2013) ...
Article
Ethnopharmacological relevance: Sideritis scardica Griseb. is an endemic species in the Balkan Peninsula. It is used in traditional medicine as a loosening agent in bronchitis and bronchial asthma; against the common cold and lung emphysema; in the treatment of inflammation, gastrointestinal disorders and coughs; and as an active constituent of dietary supplements for the prevention of anemia. This review aims to provide a comprehensive overview of the traditional use, phytochemistry, biological activity, cultivation, and extraction of Sideritis scardica and to highlight the gaps in our knowledge which deserves further research. Materials and methods: The present review is based on information collected from scientific journals, books, and electronic search. These sources include Scopus, Pubmed, Web of Science, and Google scholar as well as local books on ethnopharmacology and botany of this plant. Results: The reported data on phytochemical studies, biological activity, cultivation, extraction, and traditional uses have been reviewed. Variability in essential oil composition of wild growing and cultivated taxa depending on ecological conditions was discussed. Flavonoids, phenylethanoids, diterpenoids, aliphatic compounds, etc. identified so far have been summarized. A comparative study on the effectiveness of different methods, solvents, and parameters of extraction has also been discussed. A broad range of activities of plant extracts and fractions as antimicrobial, anti-inflammatory, cytotoxic, antioxidant, gastroprotective, antiglioma, and triple monoamine reuptake inhibition as well as cultivation of the species as an approach for conservation of the natural habitats and provision of herb with high and permanent quality has also been presented. Conclusions: Sideritis scardica has become very popular and widely advertised herb in Europe. Although some of ethnobotanical uses have been proved through in vitro experiments, further studies of the individual compounds or chemical class of compounds responsible for the pharmacological effects and the mechanisms of action are necessary. In addition, the toxicity and the side effects from the use of Sideritis scardica as well as clinical trails need attention. The variability in the chemical composition of this medicinal plant depending on the origin requires development of a protocol for its standardization. For the practice it is important to improve cultivation conditions in order to increase the accumulation of biologically active compounds and to obtain herb with permanent and good quality.
... The plant is rich in polyphenols, such as flavonoids, hydroxycinnamic acid derivatives, and phenylethanoid glycosides (Evstatieva, 2002;Petreska et al., 2011). Pharmacological activities like antimicrobial, gastroprotective and antiinflammatory activity are mostly accredited to this class of secondary metabolites (Tadic et al., 2007;Tadic et al., 2012a;Tadic et al., 2012b). Recently the effects of S. scardica extracts on the central nervous system were addressed in a number of studies. ...
... Other possible mechanisms of action against Aβ toxicity involve antiinflammatory and antioxidant activities (Gilgun-Sherki et al., 2001;Heneka et al., 2015;Kadowaki et al., 2005;Shelat et al., 2008). As S. scardica has already shown anti-inflammatory properties (Tadic et al., 2007), the inhibition of neuroinflammation is a possible mechanism in vertebrates. But as the nematodes are lacking important structures and mediators which promote inflammation, this is not applicable in the chosen model. ...
Preprint
Full-text available
Background. Beyond its traditional uses in the Balkan area, Sideritis scardica (known as Greek mountain tea, Lamiaceae) is currently extensively investigated for its pharmacological activity in the central nervous system. Antidepressant, psychostimulating, cognition-enhancing and neuroprotective properties have been described. In this study, we tested hydroalcoholic extracts of S. scardica for their potential to counteract amyloid-β toxicity and aggregation, which plays a crucial role in the pathogenesis of Alzheimer's disease. Methods. For this purpose, we have chosen the nematode Caenorhabditis elegans , which is used as a model organism for neurodegenerative diseases. The concentration of different polyphenols in extracts prepared from water, 20, 40, 50, and 70 % ethanol was analysed by HPLC. Additionally, polar and unpolar fractions were prepared from the 40 % ethanolic extract and phytochemically analysed. Results. Essentially, the contents of all measured constituents increased with the lipophilicity of the extraction solvents. Treatment of transgenic C. elegans strains expressing amyloid-β with the extracts resulted in a reduced number of peptide aggregates in the head region of the worms and alleviated toxicity of amyloid-β, observable through the degree of paralysed animals. The mid-polar extracts (40 and 50 % ethanol) turned out be the most active, decreasing the plaque number by 21 % and delaying the amyloid-β-induced paralysis by up to 3.5 h. The more lipophilic extract fractions exhibited higher activity than the hydrophilic ones. Discussion. Sideritis scardica extracts demonstrated pharmacological activity against characteristics of Alzheimer's disease also in C. elegans , supporting current efforts to assess its potential for the treatment of cognitive decline. The active principle as well as the mode of action needs to be investigated in more detail.
... The plant is rich in polyphenols, such as flavonoids, hydroxycinnamic acid derivatives, and phenylethanoid glycosides (Evstatieva, 2002;Petreska et al., 2011). Pharmacological activities like antimicrobial, gastroprotective and antiinflammatory activity are mostly accredited to this class of secondary metabolites (Tadic et al., 2007;Tadic et al., 2012a;Tadic et al., 2012b). Recently the effects of S. scardica extracts on the central nervous system were addressed in a number of studies. ...
... Other possible mechanisms of action against Aβ toxicity involve antiinflammatory and antioxidant activities (Gilgun-Sherki et al., 2001;Heneka et al., 2015;Kadowaki et al., 2005;Shelat et al., 2008). As S. scardica has already shown anti-inflammatory properties (Tadic et al., 2007), the inhibition of neuroinflammation is a possible mechanism in vertebrates. But as the nematodes are lacking important structures and mediators which promote inflammation, this is not applicable in the chosen model. ...
Preprint
Full-text available
Background. Beyond its traditional uses in the Balkan area, Sideritis scardica (known as Greek mountain tea, Lamiaceae) is currently extensively investigated for its pharmacological activity in the central nervous system. Antidepressant, psychostimulating, cognition-enhancing and neuroprotective properties have been described. In this study, we tested hydroalcoholic extracts of S. scardica for their potential to counteract amyloid-β toxicity and aggregation, which plays a crucial role in the pathogenesis of Alzheimer's disease. Methods. For this purpose, we have chosen the nematode Caenorhabditis elegans , which is used as a model organism for neurodegenerative diseases. The concentration of different polyphenols in extracts prepared from water, 20, 40, 50, and 70 % ethanol was analysed by HPLC. Additionally, polar and unpolar fractions were prepared from the 40 % ethanolic extract and phytochemically analysed. Results. Essentially, the contents of all measured constituents increased with the lipophilicity of the extraction solvents. Treatment of transgenic C. elegans strains expressing amyloid-β with the extracts resulted in a reduced number of peptide aggregates in the head region of the worms and alleviated toxicity of amyloid-β, observable through the degree of paralysed animals. The mid-polar extracts (40 and 50 % ethanol) turned out be the most active, decreasing the plaque number by 21 % and delaying the amyloid-β-induced paralysis by up to 3.5 h. The more lipophilic extract fractions exhibited higher activity than the hydrophilic ones. Discussion. Sideritis scardica extracts demonstrated pharmacological activity against characteristics of Alzheimer's disease also in C. elegans , supporting current efforts to assess its potential for the treatment of cognitive decline. The active principle as well as the mode of action needs to be investigated in more detail.
... In folk medicine it is also known for its anti-inflammatory and antiseptic properties. The study of Tadić et al. [77] confirmed significant anti-inflammatory activity of S. scardica ethanolic extract comparable with a nonsteroidal anti-inflammatory drug indomethacine. In addition, some studies reported the antimicrobial activity of S. scardica extracts against several common Gram-positive (Staphylococcus epidermidis, Micrococcus luteus, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pyogenes, Streptococcus canis, Moraxella catarrhalis, Corynebacterium pseudotuberculosis, and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Pasteurella multocida, and Haemophilus sp.) as well as the yeast Candida albicans [77]. ...
... The study of Tadić et al. [77] confirmed significant anti-inflammatory activity of S. scardica ethanolic extract comparable with a nonsteroidal anti-inflammatory drug indomethacine. In addition, some studies reported the antimicrobial activity of S. scardica extracts against several common Gram-positive (Staphylococcus epidermidis, Micrococcus luteus, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pyogenes, Streptococcus canis, Moraxella catarrhalis, Corynebacterium pseudotuberculosis, and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Pasteurella multocida, and Haemophilus sp.) as well as the yeast Candida albicans [77]. The strongest activity of extracts was determined against S. epidermidis, M. luteus, E. coli, P. aeruginosa, Corynebacterium pseudotuberculosis, Pasteurella multocida, and Haemophilus sp. ...
Article
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Due to the growing problem of obesity associated with type 2 diabetes and cardiovascular diseases, causes of obesity are extensively investigated. In addition to a high caloric diet and low physical activity, gut microbiota disturbance may have a potential impact on excessive weight gain. Some reports indicate differences in the composition of the intestinal microflora of obese people in comparison to lean. Bioactive compounds of natural origin with beneficial and multifaceted effects on the body are more frequently used in prevention and treatment of many metabolic diseases including obesity. Sideritis scardica is traditionally consumed as mountain tea in the Balkans to strengthen the body and improve mood. Many reports indicate a positive effect on digestive system, weight loss, and prevention of insulin resistance. Additionally, it exhibits antioxidant activity and anti-inflammatory effects. The positive effect of Sideritis scardica extracts on memory and general cognitive abilities is indicated as well. The multilevel positive effect on the body appears to originate from the abundant occurrence of phenolic compounds, especially phenolic acids in Sideritis scardica extracts. However, mechanisms underlying their action require careful discussion and further research. Therefore, the objective of this review is to summarize the available knowledge on the role and mechanism of action of biologically active compounds of Sideritis scardica and other related species from the genus Sideritis.
... The plant is rich in polyphenols, such as flavonoids, hydroxycinnamic acid derivatives, and phenylethanoid glycosides (Evstatieva, 2002;Petreska et al., 2011). Pharmacological activities like antimicrobial, gastroprotective and anti-inflammatory activity are mostly accredited to this class of secondary metabolites (Tadic et al., 2007;Tadic et al., 2012a;Tadic et al., 2012b). Recently the effects of S. scardica extracts on the central nervous system were addressed in a number of studies. ...
... Other possible mechanisms of action against Aβ toxicity involve anti-inflammatory and antioxidant activities (GilgunSherki, Melamed & Offen, 2001;Heneka et al., 2015;Kadowaki et al., 2005;Shelat et al., 2008). As S. scardica has already shown anti-inflammatory properties (Tadic et al., 2007), the inhibition of neuroinflammation is a possible mechanism in vertebrates. But as the nematodes are lacking important structures and mediators which promote inflammation, this is not applicable in the chosen model. ...
Article
Full-text available
Background Beyond its traditional uses in the Balkan area, Sideritis scardica (known as Greek mountain tea, Lamiaceae) is currently extensively investigated for its pharmacological activity in the central nervous system. Antidepressant, psychostimulating, cognition-enhancing and neuroprotective properties have been described. In this study, we tested hydroalcoholic extracts of S. scardica for their potential to counteract amyloid-β toxicity and aggregation, which plays a crucial role in the pathogenesis of Alzheimer’s disease. Methods For this purpose, we have chosen the nematode Caenorhabditis elegans , which is used as a model organism for neurodegenerative diseases. The concentration of different polyphenols in extracts prepared from water, 20, 40, 50, and 70% ethanol was analysed by HPLC. Additionally, polar and unpolar fractions were prepared from the 40% ethanolic extract and phytochemically analysed. Results Essentially, the contents of all measured constituents increased with the lipophilicity of the extraction solvents. Treatment of transgenic C. elegans strains expressing amyloid-β with the extracts resulted in a reduced number of peptide aggregates in the head region of the worms and alleviated toxicity of amyloid-β, observable through the degree of paralysed animals. The mid-polar extracts (40 and 50% ethanol) turned out be the most active, decreasing the plaque number by 21% and delaying the amyloid-β-induced paralysis by up to 3.5 h. The more lipophilic extract fractions exhibited higher activity than the hydrophilic ones. Discussion Sideritis scardica extracts demonstrated pharmacological activity against characteristics of Alzheimer’s disease also in C. elegans , supporting current efforts to assess its potential for the treatment of cognitive decline. The active principle as well as the mode of action needs to be investigated in more detail.
... In addition, activity studies conducted on Sideritis perfoliata, Sideritis scardica Griseb. revealed the antiinflammatory effects of the taxa (Tadić et al., 2007;Charami et al., 2008). ...
Article
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Medicinal plants have been used by humans for the treatment of various diseases for thousands of years from past to present. Members of the Lamiaceae family are among the most preferred medicinal plants due to the wide variety of secondary components they contain, particularly essential oils. In this review, Master’s and PhD theses and books based on ethnobotanical studies investigated between 1960 and 2021 as well as internationally recognized databases (PubMed, Scopus, Google Scholar, Web of Science, SciFinder, Springer and Elsevier) were used to determine the medicinal uses of Lamiaceae taxa among the people in Turkey. As a result of the study, it was found that a total of 221 taxa (192 species) belonging to 29 genera, 51 of which are endemic, have medicinal/therapeutic uses. The local names of these taxa, the usage which are used among the people, the diseases in which they are used, and the geographical regions given in the present study. The genera of taxa most commonly used for medicinal purposes by the local people are Salvia (37 taxa), Sideritis (25 taxa), Stachys (22 taxa), Thymus (16 taxa) and Origanum (13 taxa). It was observed that the most frequently used two methods while preparing these plants for use was infusion (61%), and decoction (24%). Studies conducted on National (TURK, BHP), Regional (EU) and International Pharmacopoeias (WHO) and various monographs (AHP, COMISSION E, EMA, ESCOP, PDR) have revealed that there are 29 taxa included in these pharmacopoeias and monographs whose purpose of use are similar to the diseases that local people are trying to treat. Diseases that people use plants for therapeutic purposes are grouped into 12 categories. It was determined that these plants were widely used for therapeutic purposes in gastric disorders as well as otolaryngology and respiratory system diseases. This review briefly discusses whether some taxa commonly used by the local people in the treatment of diseases can be useful in the treatment of the disease in question, in the light of scientific studies.
... In addition, 1,2-dichloroethane and nhexane extracts of the plant was reported to show a potent fungicidal activity. In another study, antimicrobial effects of Sideritis scardica extracts were determined by Tadić et al. (14). According to the results of their study, ethanolic extract of the plant showed various level of antimicrobial activity all tested strains which were Micrococcus luteus, Candida albicans, Staphylococcus epidermidis, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumonia. ...
Data
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Hagers monograph of Sideritis scardica
Data
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Hagers monograph of Sideritidis scardicae herba
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Adams, R. P. 2007. Identification of essential oil components by gas chromatography/ mass spectrometry, 4th Edition. Allured Publ., Carol Stream, IL Is out of print, but you can obtain a free pdf of it at www.juniperus.org
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The antioxidant properties and phenolic composition of 27 Sideritis species were studied. Plant samples were extracted with petroleum ether using a Soxhlet apparatus. The defatted plant materials were extracted with 70% methanol. Antioxidant activities of the extracts were measured using Fe+2 induced linoleic acid peroxidation, as indicated by thiobarbituric acid reactive substance (TBARS) production. Free radical scavenging activities were determined based on 1,1-diphenyl-2-picrylhydrazyl radical (DPPH). Results were compared with standard BHT. Total phenol concentration of the extracts was estimated with Folin-Ciocalteu reagent using gallic acid as standard, and phenolic components were quantified by HPLC-DAD.
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The antioxidant activities and total phenolics of 28 plant products, including sunflower seeds, flaxseeds, wheat germ, buckwheat, and several fruits, vegetables, and medicinal plants were determined. The total phenolic content, determined according to the Folin−Ciocalteu method, varied from 169 to 10548 mg/100 g of dry product. Antioxidant activity of methanolic extract evaluated according to the β-carotene bleaching method expressed as AOX (Δ log A470/min), AA (percent inhibition relative to control), ORR (oxidation rate ratio), and AAC (antioxidant activity coefficient) ranged from 0.05, 53.7, 0.009, and 51.7 to 0.26, 99.1, 0.46, and 969.3, respectively. The correlation coefficient between total phenolics and antioxidative activities was statistically significant. Keywords: Antioxidant activity; phenolics; medicinal plants; oilseeds; buckwheat; vegetables; fruits; wheat products
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The effect of aloe emodin (AE), a herbal anthraquinone derivative, on the rat C6 glioma cell line was investigated. In addition to cell cycle block and caspasedependent apoptosis, AE led to the formation of intracytoplasmic acidic vesicles indicative for autophagic cell death. Moreover, differentiation of surviving cells toward the astrocytic lineage was confirmed by typical morphological changes and increased expression of glial fibrillary acidic protein (GFAP). AE did not affect the activation of mitogen-activated protein kinase p38, Jun-N-terminal kinase, or transcription factor NF-kappaB, but markedly inhibited the activation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) in C6 cells. A selective inhibitor of ERK activation, PD98059, mimicked the effects of AE on glioma cell morphology and GFAP expression, but failed to induce either apoptosis or autophagy. Taken together, these results indicate that the anti-glioma action of AE involves ERK-independent induction of both apoptosis and autophagy, as well as ERK inhibition-mediated differentiation of glioma cells.
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Diet high in vegetables and fruits has been associated with reduced cancer risk. However, the involved mechanisms are unknown. Previously, we reported that the dietary flavonoid apigenin could inhibit the proteasome activity and induce apoptosis in tumor cells. To further investigate the structure-proteasome-inhibitory activity relationships, we chose and tested five dietary flavonoids, including luteolin, apigenin, chrysin, naringenin and eriodictyol. We found that the order of inhibitory potencies and apoptosis-inducing potencies of these five compounds in 20S purified proteasome and tumor cells was: (1) luteolin > apigenin > chrysin, and (2) apigenin > naringenin, and luteolin > eriodictyol. Therefore, flavonoids with hydroxylized B ring and/or unsaturated C ring are natural potent proteasome inhibitors and tumor cell apoptosis inducers. Furthermore, neither apigenin nor luteolin could inhibit the proteasome and induce apoptosis in non-transformed human natural killer cells. This finding may provide a molecular basis for the clinically observed cancer-preventive effects of fruits and vegetables.
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Cancer protection associated with the consumption of olive products is well established, but not for leukemia. The protective effects of olive (Olea europaea L.) leaves were investigated by incubating human promyelocytic leukemia HL-60 cells with olive leaf extracts (OLEs) from seven principal Tunisian olive varieties, namely, Chemchali, Chemlali, Chétoui, Gerboui, Sayali, Zalmati and Zarrazi. The results showed significant growth inhibition of HL-60 cells incubated for 48 h with a 100-fold dilution of each OLE which had been obtained by incubating 10 g of dried leaves in 100 ml of 70% ethanol for one week with subsequent ultrafiltration. DNA fragmentation was observed in the cells incubated for 19 h with a 100-fold dilution of the Chemchali, Chemlali and Zalmati extracts. The results of a nitroblue tetrazolium (NBT) assay revealed NBT reduction, a differentiation marker, by the OLE-treated cells after an overnight incubation. The Gerboui extract showed the highest NBT reduction ability at more than 90%. An HPLC analysis revealed the presence of apigenin 7-glucoside in the extract, which was found in subsequent experiments to be responsible for the Gerboui extract-mediated cell differentiation.
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Nine known and one new ent-kaurene diterpenoid were isolated from the acetone extract of Sideritis stricta Boiss & Heldr. The new compound, identified as ent-1 beta-hydroxy-7 alpha-acetyl-15 beta,16 beta-epoxykaurane (1) by IR, 1D and 2D NMR techniques and mass spectra, was isolated along with sideroxol (2), 7-acetyl sideroxol (3), 7-epicandicandiol (4), linearol (5), ent-7 alpha,15 beta,18-trihydroxy-kaur-16-ene (6), ent-7 alpha-acetyl,15,18-dihydroxy-kaur-16-ene (7), foliol (8), sideridiol (9) and siderol (10). The antibacterial and antifungal activities of these compounds and the whole crude acetone extract were evaluated against E. coli, S. aureus, K. pneumeonia and C. albicans.
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In the framework of the detailed phytochemical analysis of the aerial parts of Sideritis syriaca, two novel acylflavones were isolated together with three acetylated flavone glycosides and acylated flavone glycosides. The novel acylflavones were identified as isoscutellarein 7-trans-p-coumarate and apigenin 7-,4′-bis(trans-p-coumarate). Their structures were elucidated by means of UV, 1D and 2D NMR, LC–DAD–MS and confirmed by HR-MS spectroscopy.
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METHODS for measuring antioxidants and appraising antioxidant activity appear to be of two general types. If the chemical nature of the antioxidant is known, one may strive for a test specific for the compound or group of interest; for example, the nitroprusside test for sulphydryl groups. Alternatively one may observe the inhibition of some natural oxidative process such as the β-oxidation of fats, as a function of the added antioxidant.
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The Sideritis species are widely used in the treatment of gastrointestinal disorders, rheumatism, cough, the common cold and as a diuretic, and they are commonly used as an herbal tea in folk medicine in Turkey. The teas of Sideritis have unique tastes, pleasant aromas and a transparent yellow colour, and are preferred as a hot beverage. In order to evaluate this information, the crude methanolic extract and the water soluble part of the methanolic extract after partition with chloroform and n-butanol were investigated for their anti-inflammatory and antinociceptive activities. Phytochemical studies performed on the n-butanol extract of the overground parts of Sideritis brevibracteata, which is rich in phenolic compounds with promising activities, resulted in the isolation of six acetylated allose containing 8-hydroxyflavone glycosides and a phenylethanoid glycoside. The structures of the compounds were established by spectroscopic evidence (UV, IR, NMR, MS). Furthermore, these phenolic compounds of S. brevibracteata were studied for anti-inflammatory, antinociceptive, antioxidant and aldose reductase inhibitory activities. The experimental data demonstrated that S. brevibracteata displayed remarkable anti-inflammatory, antinociceptive and antioxidant activities.
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Twenty four phenolic compounds have been characterised in medicinal Sideritis species (aerial parts) from Macedonia by liquid chromatography-UV diode array coupled to ion-trap mass spectrometry with electrospray ionisation interface (negative mode). Three new phenylethanoid glycosides, alyssonoside, echinacoside, and forsythoside were detected for the first time in the genus of Sideritis, along with two known phenylethanoid glycoside verbascoside and leucoseptoside A. Three hydroxycinnamic acids, such as, 3-caffeoylquinic acid, 5-caffeoylquinic acid and feruloylquinic acid, five flavonoid 7-O-diglycosides of apigenin, hypolaetin, 3'-O-methylhypolaetin, isoscutellarein and 4'-O-methylisoscutellarein and 11 acetylated flavonoid 7-O-diglycosides. The phenolic profile of different parts of two wild and cultivated grown Sideritis species from Macedonia has been analysed using water and methanol extracts to give an insight of the nature of the flavonoids in their glycosylated forms and combinations with phenolic acids present in the plants. The structures of flavonoid glycosides were analysed before and after alkaline hydrolysis. The effect of sugar substitution and acetylation on the flavonoids and ESI ionisation and fragmentation are discussed.
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Plant samples from several species and populations of the genus Sideritis (Labiatae) grown in Bulgaria (S scardica, S syriaca and S montana) were extracted with different solvents. Their antioxidant activities were determined by the -carotene bleaching test (BCBT), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and static headspace gas chromatography (HS-GC) and compared with the antioxidant activity of two reference compounds of different polarity, viz butylated hydroxytoluene (BHT) and rosmarinic acid. The pure reference compounds were applied in a ten-times lower concentration than the plant extracts. The highest antioxidant activity in the BCBT, close to that of BHT, was observed for the more apolar extracts. The inhibitory effect on -carotene bleaching of the polar extracts and rosmarinic acid was much lower than that of BHT. The inhibition of hexanal formation in bulk safflower oil by most of S syriaca and S scardica extracts was as effective as BHT but less so than rosmarinic acid. S montana extracts showed weak antioxidant or even pro-oxidant properties. Extracts from butanol and from ethyl acetate and the total methanol extracts from all Sideritis plants studied showed a strong radical scavenging activity against DPPH, close to that of rosmarinic acid. S montana extracts were, as a whole, slightly weaker radical inhibitors than the extracts from the other two species. The antioxidant activity of Sideritis extracts was attributed to the presence of flavonoid and phenylpropanoid glycosides
Article
The petroleum ether and acetone extracts of the aerial parts of Sideritis arguta afforded two new and six known diterpenoids with the ent-kaurane skeleton. The structures of the new diterpenoids were determined as ent-7alpha,18-diacetoxy-16beta-hydroxykaurane (diacetyldistanol) (1) and ent-7alpha-acetoxy,15alpha,18-dihydroxykaur-16-ene (15-epi-eubol) (2) by spectroscopic data interpretation. Antioxidant potential was investigated for the ent-kauranes and the plant extracts by three methods (beta-carotene bleaching, free-radical scavenging, and superoxide-anion scavenging activity). Acetylcholinesterase and butyrylcholinesterase inhibitory activity were also evaluated, and the ent-kauranes eubol (3), sideroxol (5), and 7-epi-candicandiol (6) exhibited moderate butyrylcholinesterase inhibitory activity.
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A new iridoid diglucoside, 10-O-(E)-p-coumaroylmelittoside (1) and a new flavone glucoside, O-(6''-O-Acetyl-)-beta-glucopyranosylchrysoeriol (2), together with four known flavone glycosides, were isolated from the aerial parts of Sideritis lanata. The structures of the new compounds were elucidated by spectroscopic methods, 2D NMR and MS.
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Five flavonoid glycosides, 4'-O-methylisoscutellarein 7-O-[6"'-acetylallopyranosyl(1----2)glucopyranoside], 4'-O-methylisoscutellarein 7-O-allopyranosyl(1----2)glucopyranoside, 3'-hydroxy-4'-O-methylisoscutellarein 7-O-[6"'-acetylallopyranosyl(1----2) glucopyranoside], and hypolaetin-8-glucoside have been isolated from Sideritis javalambrensis aerial parts and identified by standard methods. These glycosides have been tested for their antioxidant properties alongside other 7,8-substituted flavonoids using FeSO4/cysteine-induced microsomal lipid peroxidation. Superoxide scavenging activity was assessed in the nitroblue tetrazolium test. Among this series of flavonoids, hypolaetin-8-glucoside is the most potent inhibitor of nonenzymic lipid peroxidation. The antiperoxidative activity of these flavonoids may be related to their superoxide scavenging ability.
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The effect of the radical removing agents, allopurinol and dimethyl sulphoxide (DMSO), on the healing rate of ethanol (1 ml of 40% solution) induced gastric mucosal injury was studied in the rat. One millilitre of 1, 2 or 5% allopurinol or DMSO were instilled into the stomach 1, 24 and 48 h after giving ethanol by gavage. One hour after administration of ethanol, gastric mucosal injury was produced in all animals (20.4 +/- 1.2 mm2, mean +/- SEM, n = 10). Treatment for 24 h with 2% allopurinol or DMSO significantly (p less than 0.01) reduced the extent of the ethanol injury (11.1 +/- 0.8 and 11.9 +/- 0.9 mm2, respectively, vs. 19.2 +/- 1.1 mm2, n = 10) and this was similarly achieved by the 5% solutions (10.4 +/- 0.9 and 10.2 +/- 0.8 mm2, respectively, vs. 19.2 +/- 1.1 mm2, n = 10). After treatment for 48 h, 30% of animals having 1% allopurinol or DMSO remained with injury significantly (p less than 0.001) less than that seen with ethanol alone (4.1 +/- 0.4 and 3.9 +/- 0.5 mm2, respectively, vs. 12.1 +/- 0.9 mm2, n = 10); however, none treated with 2 or 5% solutions remained with any injury. Healing of this injury was confirmed microscopically and was achieved by regeneration. Thus, removing oxygen-derived free radicals stimulates the healing of ethanol-induced acute gastric mucosal injury in the rat.
Article
Fifty-one essential oils extracted from plants of known origin were tested for their antimicrobial activity against three bacteria, Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli and four yeasts, Torulopsis utilis, Schizosaccharomyces pombe, Candida albicans and Saccharomyces cerevisiae using the drop diffusion method. All showed antimicrobial activity against at least one of the micro-organisms. Following this preliminary screening, 13 essential oils showing antimicrobial activity against at least five of the micro-organisms were tested in the range 50 micrograms ml-1 to 500 micrograms ml-1 using broth micro dilution techniques with dimethylsulphoxide (DMSO) as a dispersing solvent. The concentration of most of the oils required for total inhibition of growth was > 500 micrograms ml-1. Further studies on the antimicrobial action of cinnamon oil in the range 10-150 micrograms ml-1 showed that 50-fold higher activity was found when no dispersing solvent was used.
Article
Andalusol, ent-6α,8α,18-trihydroxy-13(16),14-labdadiene, is a naturally occurring diterpene, isolated from Sideritis foetens (Lamiaceae). This compound exhibited therapeutic activity when evaluated in in vivo models of paw and ear inflammation (Navarro et al., 1997: Z. Naturforsch., 52, 844-849). The pharmacological effects of this diterpene have been analysed on the activation of the macrophage cell line J774 with lipopolysaccharide (LPS) and interferon-γ (IFN-γ). Incubation of J774 macrophages with andalusol (0.1–100 μM) inhibited the synthesis of nitrite caused by LPS (1 μg ml−1) in concentration and time-dependent manners. The maximal inhibition was observed when andalusol was added 30 min before LPS stimulation and decreased progressively as the interval between andalusol and LPS challenge increased up to 14 h. Incubation of J774 cells with LPS resulted in the expression of NOS-2 protein (130 kDa) as identified by Western blot analysis. The levels of this enzyme decreased significantly in the presence of andalusol (IC50=10.5 μM), suggesting that this diterpene inhibited NOS-2 expression. Andalusol inhibited nuclear factor κB activation, a transcription factor necessary for NOS-2 expression in response to LPS and IFN-γ. This compound also inhibited the degradation of IκBα favouring the retention of the inactive NF-κB complexes in the cytosol. Related compounds to andalusol but lacking the polyol groups were less effective inhibiting NOS-2 expression in LPS-activated macrophages. The present findings provide a mechanism by which the anti-inflammatory properties of this diterpene could be mediated. British Journal of Pharmacology (1999) 128, 605–612; doi:10.1038/sj.bjp.0702844
Article
The effect of nitric oxide (NO) on growth and major histocompatibility complex(MHC)-unrestricted cytotoxicity of interleukin(IL)-2-cultivated rat spleen nonadherent mononuclear cells was examined. NO donor sodium nitroprusside (SNP) at relatively low concentrations increased magnitude, as well as duration of IL-2-induced proliferative response of nonadherent splenocytes. SNP effect depended completely on released NO, because it was prevented by NO scavenger haemoglobin, but not mimicked by expired SNP solution, unable to generate NO, or ferricyanide, a second breakdown product of SNP. Other NO donors - SIN-1, SNAP and GSNO failed to exert SNP-like growth-enhancing action, probably as a consequence of rapid NO generation, compared to sustained NO release by SNP. All NO-releasing chemicals at high concentration blocked IL-2-induced proliferation. Growth-promoting effect of SNP-derived NO was independent of guanilat cyclase activation, because dibutyryl cGMP did not affect IL-2-triggered splenocyte proliferation. Macrophage NO acted in a manner similar to SNP; at low concentrations it promoted IL-2-induced splenocyte growth, however higher amounts were suppressive. Cytotoxicity of IL-2-activated splenocytes against NK-sensitive K562 cell line was significantly increased when SNP was present during cultivation with IL-2. Proportion of NKR-P1+ and CD25+ cells, as well as per cell expression of these important activation molecules were increased upon SNP treatment, suggesting possible mechanism for the observed NO action.
Article
Flavonoids are a class of polyphenolic compounds widely distributed in the plant kingdom, which display a variety of biological activities, including chemoprevention and tumor growth inhibition. Our aim was to investigate the effects of several polyphenols on the growth and metastatic potential of B16-BL6 melanoma cells in vivo. Intraperitoneal administration of quercetin, apigenin, (-)-epigallocathechin-3-gallate (EGCG), resveratrol, and the anti-estrogen tamoxifen, at the time of i.m. injection of B16-BL6 cells into syngeneic mice, resulted in a significant, dose-dependent delay of tumor growth, without toxicity. The relative descending order of potency was EGCG > apigenin = quercetin = tamoxifen > resveratrol > control. Furthermore, polyphenols significantly potentiated the inhibitory effect of a non-toxic dose of cisplatin. When tested for the ability to inhibit lung colonization, quercetin, apigenin, and tamoxifen (but not EGCG or resveratrol) significantly decreased the number of B16-BL6 colonies in the lungs in a dose-dependent manner, with quercetin and apigenin being more effective than tamoxifen. Interestingly, quercetin, apigenin, and tamoxifen (but not EGCG or resveratrol) significantly decreased the invasion of B16-BL6 cells in vitro, with quercetin and apigenin being more effective than tamoxifen. This suggests that anti-invasive activity is one of the mechanisms underlying inhibition of lung colonization by quercetin and apigenin. In conclusion, quercetin and apigenin inhibit melanoma growth and invasive and metastatic potential; therefore, they may constitute a valuable tool in the combination therapy of metastatic melanoma.
Article
Extracts obtained from aerial parts of Stachys inflata have been used in Iranian folk medicine in infective, rheumatic and other inflammatory disorders. In the present study, the anti-inflammatory properties of total methanol extract isolated from aerial parts of Stachys inflata were investigated in two well-characterised inflammatory models in rats, carrageenan-induced paw oedema and formalin-induced paw licking. Intraperitoneal injection of the extract, 60 min before induction of inflammation, revealed a dose-related inhibition of carrageenan-induced rat paw oedema over the dose range 50-200 mg/kg. In the formalin test, the extract (50, 100 and 200 mg/kg) had no effect against the first phase (0-5 min) of the formalin-induced pain, but all three doses produced a significant blockade of the second phase (P < 0.001). Myeloperoxidase (MPO) activity was determined, and a histopathological study was carried out in paw tissue 4 h after induction of inflammation. The hydroalcoholic extract (200 mg/kg) substantially reduced MPO activity (P < 0.05), which was increased in the control group. Histological examination showed a marked reduction in tissue injury and inhibition in neutrophil infiltration in rats treated with the extract (200 mg/kg).
Article
A sterol fraction composed of campesterol (7.6%), stigmasterol (28.4%) and beta-sitosterol (61.1%) was obtained by activity-guided fractionation of the acetone extract of Sideritis foetens Clem. This sterol fraction showed anti-inflammatory activity in in vivo murine models of inflammation. It decreased carrageenan paw oedema in mice after oral administration of 30 and 60 mg/kg and inhibited mouse ear oedema induced by 12-O-tetradecanoylphorbol acetate (TPA) after topical application. Quantitation of the neutrophil specific marker myeloperoxidase (MPO) demonstrated that its topical anti-inflammatory activity was associated with reduction in neutrophil infiltration into inflamed tissues. Non-cytotoxic concentrations of the sterol fraction inhibited leukocyte granular enzyme release (beta-glucuronidase) and superoxide generation. However, it did not shown any significant inhibitory effect on histamine release from mast cells. In vitro modulatory activity towards the classical pathway of the complement system shown by this fraction would correlate with the anti-inflammatory profile shown in vivo.
Article
A previous chemical study of Sideritis canariensis var. pannosa demonstrated the presence of some important classes of related organic compounds with anti-inflammatory activities. In the present study, the crude ethanol extract and the chloroformic and aqueous fractions of S. canariensis have been examined for their antimicrobial actions through the disk-diffusion method and for their anti-inflammatory and analgesic effects in several animal models. No relevant antimicrobial activity against the tested microorganisms was found. The chloroformic fraction was the most interesting, exhibiting a good analgesic and anti-inflammatory activity.
Article
Fatty acids (FA), hydrocarbons, alpha-amyrin, stigmasterol and beta-sitosterol were identified in the n-hexane extract of the aerial parts of Sideritis taurica Stephan ex Wild. Xanthotoxin, as well as 2-acetyl-3-hydroxy-5,6,8-trimethoxy-1,4-naphthoquinone were isolated from the methylene chloride extract of the plant. In addition to apigenin 7-O-beta-D-glucopyranoside and apigenin, previously reported from the plant, hypolaetin 7-O-beta-D-allopyranosyl-O-beta-D-glucopyranoside was isolated from the ethyl acetate extract. From the methanol extract, isoscutellarein 7-O-beta-D-allopyranosyl-O-beta-D-glucopyranoside was also isolated. Toxicity study of petroleum ether extract (f(1)), ethanolic extract (f(2)), dichloromethane fraction of f(2) (f(3)) and n-butanolic fraction of f(2) (f(4)) of the plant proved that it is relatively nontoxic. The tested extracts and fractions exhibited significant analgesic, anti-inflammatory, anti-ulcerogenic and antihyperglycaemic activities, but no anticonvulsant and antipyretic effects, as compared with control groups and reference drugs.
Article
Flavonoids have been proposed to act as beneficial agents in a multitude of disease states, including cancer, cardiovascular disease, and neurodegenerative disorders. The biological effect of these polyphenols and their in vivo circulating metabolites will ultimately depend on the extent to which they associate with cells, either by interactions at the membrane or more importantly their uptake. This review summarises the current knowledge on the cellular uptake of flavonoids and their metabolites with particular relevance to further intracellular metabolism and the generation of potential new bioactive forms. Uptake and metabolism of the circulating forms of flavanols, flavonols, and flavanones into cells of the skin, the brain, and cancer cells is reviewed and potential biological relevance to intracellular formed metabolites is discussed.
Article
Nine 7-o-allosyl glucosides of 5,8-dihydroxy substituted flavones were isolated from a fraction of the methanol extract of the aerial parts of Sideritis raeseri Boiss et Heldr. subsp. raeseri. The structures were identified by spectroscopic methods. The antioxidant activity of this fraction, evaluated by the Co(II) EDTA-induced luminol chemiluminescence and by the DPPH scavenging activity, was found to be moderate. The activity can be related with the presence of 5- and 8-o-disubstituted flavones.
Article
Reactive oxygen species are believed to play a very significant role in the pathogenesis of several diseases including Alzheimer's disease and Parkinson's disease. It is reported that the crucial balance between reactive oxygen species generation and antioxidant defense is regarded as a force in a wide variety of chronic diseases. In this paper, PC12 cells were used to study the antioxidative effect of hyperoside. The results indicated that hyperoside could effectively protect PC12 cells against cytotoxicity induced by hydrogen peroxide and tert-butyl hydroperoxide at 160 microg/ml and 100 microg/ml, respectively. The study also showed that hyperoside was no harmful within the tested concentration range and could easily enter into the PC12 cells. With the increasing concentration of hyperoside, cytotoxicity induced by hydrogen peroxide and tert-butyl hydroperoxide was significantly attenuated and the corresponding extracellular lactate dehydrogenase levels decreased concurrently by pretreatment with hyperoside. The results were proved by flow cytometric detection of apoptotic cells. All the above results showed hyperoside could efficiently prevent the PC12 cells from shrinking and turning against apoptosis induced by hydrogen peroxide and tert-butyl hydroperoxide.
Article
Sideritis italica (Miller) Greuter et Burdet is a widespread Lamiacea in the Mediterranean region used in traditional medicine. Essential oils were antibacterial against nine ATCC and as many clinically isolated Gram-positive and Gram-negative bacterial strains. Antibacterial activity was also found against Helicobacter pylori: a dose-dependant inhibition was shown between 5 and 25 μg/ml. The antibacterial activity of the oils was expressed as MICs (minimum inhibitory concentrations) and MBCs (minimum bactericidal concentrations). At a concentration between 3.9 and 250 μg/ml the oils showed a significant antibacterial effect against both Gram-negative and Gram-positive bacteria. In particular the ATCC strains Pseudomonas aeruginosa (MIC = 3.9 μg/ml and 7.8 for flowerheads and leaves, respectively), Proteus mirabilis (MIC = 15.6 and 7.8 μg/ml), Salmonella typhi (MIC = 7.8 μg/ml) and Proteus vulgaris (MIC = 15.6 μg/ml) were the most inhibited. Only Pseudomonas aeruginosa showed MBC at a concentration between 62.6 and 125 μg/ml. The antioxidant activity of the essential oils was evaluated by two cell free colorimetric methods: ABTS and DMPD; leaf oil is more active (4.29 ± 0.02 trolox equivalents and 4.53 ± 0.67 ascorbic acid equivalents by ABTS and DMPD, respectively). Finally the antioxidant activity of the essential oils was also evaluated by their effects on human whole blood leukocytes (WB) and on isolated polymorphonucleate (PMN) chemiluminescence. Comparing the effects of the oils from leaves and flowerheads on both PMN and WB chemiluminescence emission, we found no significant differences. Essential oils showed a dose-dependent and linear inhibitory activity on isolated PMN as well as on WB CL emission when PMA-stimulated. On the contrary, the inhibitory activity on resting cells was nonlinear.
Article
The in vitro antimicrobial and antioxidant activities of the essential oil and methanol extracts of Achillea millefolium subsp. millefolium Afan. (Asteraceae) were investigated. GC-MS analysis of the essential oil resulted in the identification of 36 compounds constituting 90.8% of the total oil. Eucalyptol, camphor, alpha-terpineol, beta-pinene, and borneol were the principal components comprising 60.7% of the oil. The oil strongly reduced the diphenylpicrylhydrazyl radical (IC(50)=1.56 micro g/ml) and exhibited hydroxyl radical scavenging effect in the Fe(3+)-EDTA-H(2)O(2) deoxyribose system (IC(50)=2.7 micro g/ml). It also inhibited the nonenzymatic lipid peroxidation of rat liver homogenate (IC(50)=13.5 micro g/ml). The polar phase of the extract showed antioxidant activity. The oil showed antimicrobial activity against Streptococcus pneumoniae, Clostridium perfringens, Candida albicans, Mycobacterium smegmatis, Acinetobacter lwoffii and Candida krusei while water-insoluble parts of the methanolic extracts exhibited slight or no activity. This study confirms that the essential oil of Achillea millefolium possesses antioxidant and antimicrobial properties in vitro.
Article
Acetone extract from aerial parts of Sideritis ozturkii Aytaç & Aksoy and its fractions were investigated for its in vivo anti-inflammatory and antinociceptive activities. For the anti-inflammatory activity assessment, carrageenan-induced hind paw edema and for the antinociceptive activity, p-benzoquinone-induced abdominal constriction tests were used. Acetone extract of the plant and its phenolic fraction were found to possess significant inhibitory activity on these in vivo models in mice. Ozturkoside A (chrysoeriol 7-O-[2'''-O-caffeoyl-6'''-O-acetyl-beta-d-glucopyranosyl-(1-->2)-beta-d-glucopyranoside]); ozturkoside B (chrysoeriol 7-O-[2'''-O-caffeoyl-beta-d-glucopyranosyl-(1-->2)-beta-d-glucopyranoside]); and ozturkoside C (chrysoeriol 7-O-[2'''-O-p-coumaroyl-6'''-O-acetyl-beta-d-glucopyranosyl-(1-->2)-beta-d-glucopyranoside]) were isolated from the active phenolic fraction. The structures of isolated compounds were elucidated by spectroscopic techniques (UV, IR, 1D- and 2D-NMR, MS). Ozturkoside C showed notable antinociceptive and anti-inflammatory activities without inducing any apparent acute toxicity or gastric damage. Although the activity of ozturkosides A and B were found insignificant in statistical analysis, some inhibitory effect was observed. Accordingly, it is suggested that these components in phenolic fraction might possibly share the antinociceptive and anti-inflammatory activities together.
Article
Sideritis perfoliata L. subsp. perfoliata is a plant widely used in folk medicine in Greece since antiquity because of its antiinflammatory, antirheumatic, antiulcer, digestive and vasoprotective properties. Phytochemical investigations of the polar extracts afforded four flavonoid glycosides, four phenylpropanoic glycosides, caffeic acid and one iridoid, ajugoside. Reactive oxygen species (ROS) are implicated in the aetiology of several inflammatory processes. In the present study polar fractions and isolated compounds from S. perfoliata subsp. perfoliata were evaluated for their antioxidant activity using DPPH spectrophotometric and TBA lipid peroxidation assays, as well as for their antiinflammatory activity using the soybean lipoxygenase bioassay. All extracts and isolated compounds showed significant antioxidant and inhibitory activity against soybean lipoxygenase. These findings give support to the ethnopharmacological use of the plant in the treatment of several inflammatory ailments. Copyright
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