Article

Local Anaesthetic Activity of the Essential Oil of Lavandula angustifolia

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Abstract

In this work we studied the local anaesthetic activity of the essential oil obtained from Lavandula angustifolia Mill., a medicinal plant traditionally used as an antispasmodic. We compared its activity to the essential oils obtained from two citrus fruits, Citrus reticulata Blanco and Citrus limon (L.) Burm. f., which have no medical uses. Biological tests were also performed on the major pure components of L. angustifolia Mill. essential oil: linalol and linalyl acetate as determined by GC and confirmed by GC-MS. Anaesthetic activity was evaluated in vivo in the rabbit conjunctival reflex test, and in vitro in a rat phrenic nerve-hemidiaphragm preparation. The essential oil of L. angustifolia, linalyl acetate and linanol (0.01-10 micrograms/ml) but not the oils of Citrus reticulata and Citrus limon were able to drastically reduce, in a dose-dependent manner, the electrically evoked contractions of rat phrenic-hemidiaphragm. In the rabbit conjunctival reflex test treatment with a solution of essential oil of L. angustifolia, as well as linalyl acetate and linalol (30-2500 micrograms/ml administered in the conjunctival sac) allow a dose-dependent increase in the number of stimuli necessary to provoke the reflex, thus confirming in vivo the local anaesthetic activity observed in vitro.

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... Essential oil of L. angustifolia is reported to have anti-bacterial, mast cell degranulation inhibitory, antioxidant, spasmolytic, CNS-depressant, sedative, anti-convulsive, and local anesthetic properties [4,5]. ...
... The various mechanisms of the relaxant effect of the plant on smooth muscle included; muscarinic receptors, potassium channel opening, calcium channel-blocking [5,11], histamine (H 1 ) receptor inhibition [4], ß 2 -adrenergic receptor stimulation, nitric oxide production, cyclooxygenase pathways, and phosphodiesterase activity. In the present study, the relaxant effect of the plant on tracheal smooth muscle preincubated with atropine, glibenclamide, diltiazem, propranolol, L-NAME, indomethacin, chlorpheniramine, and papaverine was examined to evaluate the possible contribution of the above mechanisms on its relaxation response. ...
... The relaxant effect of L. angustifolia was showed in guinea-pig ileum and rat ilea [9,17] in previous studies and intracellular unknown mechanisms were suggested be involved in the relaxant effects of Lavandula angustifolia [17]. The relaxant effects of the plant may be mediated by reducing the available calcium in the cell [17,18], ACE enzyme inhibition [19][20][21], Na and Ca 2+ channels inhibition [5,11], histamine release inhibition [4], muscarinic and modulation of nicotinic neurotransmitters pathway [22,23]. ...
Article
Background Lavandula angustifolia (L. angustifolia) Mill. (Common name Lavender) is used in traditional and folk medicines for the treatment of various diseases including respiratory disorders worldwide. The relaxant effect of the plant on the smooth muscle of some tissues was shown previously. The present study has investigated the role of different receptors and pathways in the relaxant effect of L. angustifolia on tracheal smooth muscle. Methods Cumulative concentrations of the hydro-ethanolic extract of L. angustifolia flowers (0.5, 1, 2 and 4 mg/ml) were added on pre-contracted tracheal smooth muscle by methacholine (10 μM) or KCl (60 mM) on non-preincubated or preincubated tissues with atropine, chlorpheniramine, propranolol, diltiazem, glibenclamide, indomethacin, ω-nitro-L-arginine methyl ester (L-NAME) and papaverine. The results compared with of theophylline (0.2, 0.4, 0.6 and 0.8 mM) as positive control and saline (1 ml) as negative control. Results The extract showed concentration-dependent relaxant effects in non-preincubated tracheal smooth muscle contracted by KCl and methacholine (p < 0.05 to p < 0.001). The relaxant effect ofL. angustifolia was not significantly different between non-preincubated and preincubated tissues with chlorpheniramine, propranolol, diltiazem, glibenclamide, and papaverine. However, two higher concentrations of L. angustifolia in preincubated tissues with L-NAME (p < 0.01), indomethacin (p < 0.05 to p < 0.001) and atropine (p < 0.05) showed significantly lower relaxant effects than non-preincubated tissues. The EC50 values of L. angustifolia in tissues preincubated with indomethacin was significantly higher than non-preincubated trachea (p < 0.05). The effects of three first concentrations of the extract on KCl and methacholine-induced muscle contraction were significantly lower than those of theophylline (p < 0.05 to p < 0.001). Conclusions These results indicated a relatively potent relaxant effect ofL. angustifolia that was lower than the effect of theophylline. The possible mechanisms of relaxant effect of this plant on tracheal smooth muscle are muscarinic receptors blockade, inhibition of cyclooxygenase pathways and/or involvement of nitric oxide production. Its clinical applications should be investigated in further studies.
... While, the presence of -3-carene represented by spathulenol (0.6%). Spathulenol was (12.6 %) as the chief compound in group B could increase reported recently to possess an immunomodulatory, its medicinal importance in the treatment of metabolic antitumor and antimicrobial activity [53,54,55]. The bone disorders and for the maintenance of bone health as presence of other medicinal important monoterpenes it have been recently reported to stimulate significantly hydrocarbon, such as tricyclene (0.7%) and myrtenal the activity and expression of alkaline phosphatase, that (0.5%) have extensively increased the medicinal promote osteoblastic differentiation [39]. ...
... chemical composition between the studied groups. This While, tricyclene [53] is reported to be one of the main result was consistent with an earlier study obtained from constituents responsible for the antimicrobial activity of ...
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Essential oils isolated from the aerial parts of Haplophyllum tuberculatum (Forsskal) A. Juss collected from five different locations of Egypt showed significant differences in their yield and chemical composition among the different locations. Estragole, Myrtenal, Spathulenol and a homologous series of medicinally important monoterpene and sesquiterpenes are succinctly viewed in the analyzed essential oils. The extensive disparity in the abundance and existence of both the major and minor detected bio active compounds reflects a considerable chemo-diversity that can favor the medicinal use of each group towards certain medical conditions the fact that could explain its wide range of different traditional uses reported in literature.
... Depending on the different types of lavandin, variations in the chemical composition were found. Ghelardini et al. (1999) [30] [33]. The essential lavender oil grown in India consisted of linalool (28.06%) and linalyl acetate (47.5%) [34]. ...
... Depending on the different types of lavandin, variations in the chemical composition were found. Ghelardini et al. (1999) [30] [33]. The essential lavender oil grown in India consisted of linalool (28.06%) and linalyl acetate (47.5%) [34]. ...
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Essential oils from Lavandula genus and the obtained hybrids are widely used for different purposes such as perfume production in the cosmetic field and for its biological properties. This is the first study on the liquid and vapour phase of Lavandula × intermedia “Grosso” essential oil grown in the Lazio Region, Italy, investigated using headspace coupled to gas chromatography and mass spectrometry (HS-GC/MS). The results showed the most abundant components were linalool and linalyl acetate, followed by 1,8-cineole and terpinen-4-ol, while lavandulyl acetate and borneol were identified as minor compounds, maintaining the same proportion in both the liquid and vapour phase. Furthermore, we tested lavandin liquid and vapour phase essential oil on gram-negative bacteria (Escherichia coli, Acinetobacter bohemicus, and Pseudomonas fluorescens) and gram-positive bacteria (Bacillus cereus and Kocuria marina).
... In animal studies, lavender oily essence had sedative [17] and analgesic [18] effects. Lavender contains linalool alcohol ketone esterzoaldehyde. ...
... Lavender contains linalool alcohol ketone esterzoaldehyde. Ketones in lavender effectively reduce pain and inflammatory and help falling asleep [18]. Esters prevent muscular spasm, reducing stress and depression [19,20]. ...
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Background: Labor pain is one of the most severe pains, which most of women experience. By using novel supportive methods, the labor pain can be reduced, which makes this event pleasant and delightful. Several original studies have been conducted in regard to the effect of lavender on reducing labor pain, whose results are controversial. One of the applications of meta-analysis studies is to respond to these hypotheses and remove controversies; therefore, this study aimed to determine the effect of lavender on labor pain in Iran by using meta-analysis. Methods: In this study, to find published articles electronically from 2006 to 2019, the published articles in national and international databases of SID, MagIran, IranMedex, IranDoc, Google Scholar, Cochrane Library, Embase, ScienceDirect, Scopus, PubMed, and Web of Science (ISI) were used. Heterogenic index between studies was determined by Cochrane test (Q)c and I2. Due to heterogeneity, the random effects model was used to estimate standardize difference of the mean score of lavender test in order to assess the labor pain between intervention and control group. Results: In this meta-analysis and systematic review, finally 13 eligible articles met the inclusion criteria of the study. The sample size from original studies enrolled in the meta-analysis entered in the intervention group was 794 individuals and in the control group was 795 individuals. Mean score for pain in the control group was 7.2 ± 0.42 and in the intervention group was 5.4 ± 0.58 and this difference was statistically significant (p ≤ 0.001). Conclusion: The results of this study showed that lavender can reduce labor pain, which can be considered by health policy makers and gynecologists.
... Moreover, lavender essential oil has anti-inflammatory and analgesic properties [9,10] as well as antimicrobial activity [11]. Lusby et al. [12] compared the treatment effects of Lavandula x allardii honey and essential oil and a standard therapeutic honey (Medihoney) for wound healing in rats. ...
... Electronic reprint for personal use ▶ (32) Mammaliicoccus lentus (16) Staphylococcus spp. b (9) Jeotgalicoccus psychrophilus (6) Macrococcus caseolyticus (2) Bacillaceae (58) Bacillus licheniformis (41) Lysinibacillus fusiformis (14) Bacillus pumilus (2) Bacillus pseudomycoides (1) Planococcaceae ( Klebsiella oxytoca (4) Salmonella enterica (2) Escherichia fergusonii (1) Enterobacter ludwigii (1) Enterobacter absuriae (1) Klebsiella pneumoniae (1) ...
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This study aimed to evaluate the efficacy of Norway spruce ointments on wound healing of castration wounds in piglets. This study included 95 male pigs randomly divided into five treatment groups: Norway spruce balm (Vulpuran), Norway spruce resin (Abilar), pork lard (ointment base of Vulpuran), no treatment (negative control) and antibiotic blue spray (Cyclo spray, positive control). Wound healing parameters (such as healing time, wound size, reddening of wound edges and surrounding, swelling, secretion and wound contamination), microbiological status and the haptoglobin level as an inflammation parameter were investigated. In the Norway spruce groups, some positive effects on wound healing parameters were found. In the first 6 days of treatment, Abilar or Vulpuran showed the smallest means of wound areas, and at the end of the study (day 15 + 17), the highest rates of completely closed wounds compared to the other groups. Vulpuran treatment led to significantly lower wound secretion (p = 0.003) and wound contamination (p = 0.015) than the untreated control did. Furthermore, the microbiological status was determined using MALDI-TOF-MS and partial 16S rRNA gene sequencing at different days of treatment. A comparison of the five treatment groups on day 3 revealed that Norway spruce led to the lowest rate of wounds colonised with fungi, mainly classified into genus Candida, (Abilar 77%, Vulpuran 70%) in comparison with blue spray (89%), lard (100%) and untreated control (100%). Fungi could only be detected in one of the 13 samples treated with Vulpuran on day 8, which nearly reached significance (p = 0.055).
... L. angustifolia was shown to have a pain inhibitory effect similar to morphine, dexamethasone, and indomethacin (Uritu et al., 2018). In addition, Ghelardini et al., (1999) compared EOs of citrus to L. angustifolia , and determined the constituents linalyl acetate and linalool to have drastic reduction of pain in vivo of the localized area, whereas the citrus oils showed no effect. Numerous in vivo studies confirm internal and external analgesic properties (Rusinowska & Śmigielski, 2014). ...
... ranj Boya ( N. ruderalis ) have been reported to have similar effects. M. vulgare possesses the antispasmodic, analgesicand anti-inflammatory compound, marribium(Uritu et al., 2018). M. vulgare has been shown to have significant antispasmodic effects on proinflammatory antagonists in animal tissues during in vivo experimentation(Souza et al, 1998).Ghelardini et al., (1999) indicates strong evidence supporting L. angustifolia as a powerful antispasmodic herb. According to Rusinowska & Śmigielski (2014), L. angustifolia was able to increase levels of cMAP which is attributed to the antispasmodic properties. M. piperita contains cineol and menthol shown to have highly antispasmodic and anti-inflammatory acti ...
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The musculoskeletal system consists of the bones, muscles, joints, cartilage and connective tissues. These areas can cause pain and stiffness due to stress and overuse through strenuous physical activity or injuries. More serious and potentially immobilizing, chronic conditions such as osteoarthritis, rheumatoid arthritis, fibromyalgia, bursitis, and tendinitis can cause severe musculoskeletal pain. Research suggests that many species of the Lamiaceae (mint) family have analgesic, anti-inflammatory, nervine, antispasmodic, rubefacient, and circulatory benefits; particularly useful for musculoskeletal pain. The Lamiaceae family is one of the largest and most distinguished families of flowering plants with over 3,500 species, this study only investigates 10 of those species most suitable for relief of musculoskeletal dysfunction; catnip (Nepeta cataria), horehound (Marrubium vulgare), hyssop (Hyssopus officinalis), lavender (Lavandula angustifolia), peppermint (Mentha piperita), rosemary (Rosmarinus officinalis), lemon balm (Melissa officinalis), motherwort (Leonurus cardiaca), skullcap (Scutellaria lateriflora), and thyme (Thymus vulgaris) are investigated. These species of the Lamiaceae family offer symptomatic relief from temporary and chronic musculoskeletal pain. While these herbs have been listed as safe for consumption, using members of this family should be avoided during pregnancy. Essential oils of these herbs should be used topically, while herbal forms such as infusions, capsules, and teas should be used internally. These species should be avoided during pregnancy.
... Another study exhibited that it modulates the expression of glutamate activation in vitro (competitive antagonism of L-[ 3 H] glutamate binding) and in vivo (delayed subcutaneous N-methyl D-aspartate-induced convulsions and blockade of intracerebroventricular quinolinic acid-induced convulsions) Silva Brum et al., 2001). Anesthetic activity related to its effects on the nicotinic receptor-ion channel (Ghelardini et al., 2000), spasmolytic effect (Lis-Balchin and Hart, 1999), and antimicrobial activity against several bacteria and fungi (Carson and Riley, 1995;Pattnaik et al., 1997) are the most vital outcomes related to linalool's pharmacological effects. Moreover, linalool, as well as other terpenes and terpenoids, could enhance the permeability of a number of drugs through skin or mucus membranes (Kunta et al., 1997;Ceschel et al., 1998;Kommuru et al., 1998). ...
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Introduction: Psoriasis is a chronic inflammatory skin disorder characterized by keratinocyte hyperproliferation and differentiation with increased immune cell infiltration. The anti-psoriatic effect of lavender oil has been reported. However, its phytoconstituents, linalool (L) and linalyl acetate (LA), showed a distinctive affinity with psoriasis targets. Objectives: This investigation was aimed to determine the combined effect of L and LA in ameliorating psoriasis-like skin inflammation and its safety in long-term topical uses. Methods: The combined effect of L and LA was compared with their individual effects. The anti-psoriatic activity was performed using imiquimod (IMQ)-induced psoriasis in BALB/c mice and evaluated to reduce PASI and CosCam scores and Th-1 and Th-17 cell-specific cytokine levels. The acute and repeated dose dermal toxicities were investigated as per the OECD guidelines. Results: L and LA combination (LLA) in the 1:1 w/w ratio at 2% concentration showed a synergistic effect. The combination showed 76.31% and 71.29% recovery in PASI and CosCam Scores; however, L2% and LA2% showed 64.28% and 47.61% recovery in PASI and 64.75 and 56.76% recovery in CosCam scores, respectively. It showed >90% and >100% recovery in Th-17 and Th-1 cell-specific cytokines, respectively, and restored epidermal hyperplasia and parakeratosis toward normal compared with psoriatic mice. A marked reduction in NF-κB, cck6, and the IL-17 expression was also observed in the LLA-treated group. This combination was safe in a therapeutically effective dose for 28 days as no significant changes were observed in organ and body weights, liver and kidney parameters, and differential leukocyte counts. Conclusion: This study proves the synergy between L and LA in a 1:1 w/w ratio at 2% in the treatment of psoriasis-like skin inflammation and provides strong scientific evidence for its safe topical use.
... -. -. , [18,19]. ISSN 2310ISSN -4902 , 2'2018 , -, ' -, [22,23]. ...
Article
In Ukraine there is a complicated epizootic situation caused by the spread of serious viral diseases, in particular in the pig breeding of African swine fever (ACS) and epidemic swine diarrhea (EDS). In such conditions, the market for disinfectants is actively developing, but often drugs do not prevent the spread of viral diseases. This is due to the discrepancy in methods and doses of application, the weak effect on certain viruses and bacteria, and also the wrong organization of disinfection. The veterinary well-being of livestock farms, complexes and poultry farms largely depends on the regular and thorough carrying out of veterinary and sanitary measures. Disinfection is an important part of the measures aimed at preventing and controlling infectious animal diseases. In most cases, existing disinfectants and recommendations for their use were designed for large commodity and industrial complexes that do not fully meet the requirements of small farms. Most commonly used disposables are toxic to humans and animals (sodium or potassium hydroxide solution, bleach, phenol and others), so they should be carefully used to prevent poisoning. In veterinary practice there are practically no ecologically clean and safe disinfection means that can be used for sanitation of various objects of veterinary supervision, including in the presence of animals and poultry. The practice of using disinfectants in agriculture for persistent chemicals such as bleach, hydrogen peroxide, formaldehyde and several others have proved to be unserviceable in many ways. Before all it is biological harmfulness, impossibility to carry out disinfection in the presence of animals and poultry, adaptation of pathogenic microflora, high cost, high complexity of treatment of objects, clogging of the external environment, etc. Most modern low-toxic disinfectants are used in the form of solutions by irrigation or aerosols, but it is not possible to rehabilitate their premises in the presence of animals. The use of these agents is also relatively labor-intensive, greatly increases the humidity in the room, and there is a likelihood of accumulation of their residual amounts in meat. Therefore, as an option - it is worth considering the current disinfection of premises with dry biocidal preparations, for example: Stalosan F (Vitfoss, Denmark), Dezosan Vigor (JHJ, Poland), Advais draj (NutriConcept, France), Lyubisan-eko, Lyubisan pyglet (LLC Ekodisan-Ukraine), Clinosan "ZVK" (Ukraine), Mecadzade (NPC "Globus", Ukraine) and others. These disinfectants, in their properties, are environmentally friendly, represent an amorphous powder of pleasant smell, which can absorb moisture. They are effective in the destruction and control of many bacteria, viruses, fungi, parasites, and fly larvae. In addition, they improve the quality of the litter, reduce the ammonia content and moisture in livestock buildings. The main properties of the above-mentioned disinfectants include: use without restrictions in any livestock and poultry facilities (at doses of 30-50 g / m2, depending on the means), once a day during the first three days, then once a week at the indicated dose). In case of an increased risk of infection, use should be increased up to 2-3 times a week; urea bindings - prophylaxis of ammonia formation; prevention of manifestations of diseases associated with excessive moisture (dermatitis, coccidiosis, etc.); destruction and delay of the development of pathogenic and saprophytic molds, many bacteria (staphylococci, streptococcus, salmonella, pasteurens, emerios, coronaviruses), etc. When the disinfectant enters into or on the skin and mucous membranes, it does not exert an irritating effect on the organism of animals and birds. Has aseptic properties (healing of scratches and wounds of the skin). In the gastrointestinal tract, they destroy the pathogenic microflora; improves digestion and general physiological state. Activates indicators of humoral and cellular immunity. Improves animal survival and productivity. However, there are certain difficulties for dry disinfectants. First, imported disinfestations are relatively expensive (Stalosan F - up to 40 UAH, Dezosan Vigor - 30-35 UAH, Advice dry - 18-20, Mijsedas and Klinosan - 15-20 UAH / kg, depending on the seller price and the region. Secondly, the lack of domestic technical means for their sawing. Third, the use of the staff to certain means, and the transition to cheaper causes unpleasant organoleptic feelings during application. Thus, to date, both imported and domestic disinfectants have been developed and widely used, which are sufficiently effective. However, the range of preparations presented on the market of veterinary disinfectants does not fully meet the requirements that are being put forward to them. The means that would meet all the requirements for the quality and safety of disinfection is not enough today. Therefore, the development of new domestic disinfectants, especially dry forms, on time. Key words: veterinary well-being, veterinary-sanitary measures, sources of infection, pathogens transfer factors, susceptibility of the organism, complex of measures, disinfection tasks, disinfectant, animals, safe and high-quality products.
... Thus, the present study was focused on exploring the anti-biofilm and antivirulence properties of linalool (3,7-dimethyl-1,6-octadien-3-ol), a monoterpene alcohol found in the essential oils of many floral aromatic and spice plants (Peana et al. 2008). Several studies have reported the antibacterial, antifungal and antiviral (Mazzanti et al. 1998;Chiang et al. 2005;Hsu et al. 2013), anti-inflammatory and local anaesthetic effects of linalool (Ghelardini et al. 1999;Peana et al. 2002). However, the current study demonstrated the inhibitory efficacy of linalool against P. mirabilis crystalline biofilm formation as well as virulence factor production through in vitro bioassays and transcriptomic analysis. ...
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Proteus mirabilis is one of the leading causes of catheter-associated UTIs (CAUTI) in individuals with prolonged urinary catheterization. Since, biofilm assisted antibiotic resistance is reported to complicate the treatment strategies of P. mirabilis infections, the present study was aimed to attenuate biofilm and virulence factor production in P. mirabilis. Linalool is a naturally occurring monoterpene alcohol found in a wide range of flowers and spice plants and has many biological applications. In this study, linalool exhibited concentration dependent anti-biofilm activity against crystalline biofilm of P. mirabilis through reduced production of the virulence enzyme urease that raises the urinary pH and drives the formation of crystals (struvite) in the biofilm. The results of q-PCR analysis unveiled the down regulation of biofilm/virulence associated genes upon linalool treatment, which was in correspondence with the in vitro bioassays. Thus, this study reports the feasibility of linalool acting as a promising anti-biofilm agent against P. mirabilis mediated CAUTI.
... It is used in traditional and folk medicines in various parts of the world for treating gastrointestinal, nervous and rheumatic ailments (Duke, 1989;Evans, 1989;Leung and Foster, 1996). Pharmacological and biological studies of lavender (extracts, fractions, and essential oil) reported that it has anti-convulsive, sedative, spasmolytic, local anaesthetic, antioxidant, anti-bacterial and mast cell degranulation inhibitory effects ( Ghelardini et al., 1999;Gilani et al., 2000;Hohmann et al., 1999;Kim and Cho, 1999;Leung and Foster, 1996;Lis-Balchin and Hart, 1999;Maruyama et al., 2005;Yang et al., 2010). Phytochemical researches showed that linalool, linalyl acetate and additional mono and sesquiterpenes, flavonoids such as luteolin, triterpenoids like ursolic acid and coumarins such as umbelliferone and coumarin were the primary constituents of the aerial parts and flowers of lavender plant (Duke, 1989;Leung and Foster, 1996;Omidbaigi, 2000;Renaud et al., 2001). ...
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Asthma is an inflammatory disease of the lungs, and it causes oxidative stress. Lavandula dentata is an aromatic herb with anti-oxidative and anti-inflammatory activities. This study examined the activity of L. dentata extract on a guinea pig model of asthma. Adult males were divided into five groups: First group was control, second was asthma model induced by OVA, third was treated with L. dentata extract orally (300 mg/kg) for 21 days; the fourth was an asthma model with L. dentata extract (300 mg/kg) and fifth was treated with Tween 80 for 21 days. OVA treatment increased IgE, triglycerides, total cholesterol, glucose levels in serum, WBC count in blood and MDA in lungs. Also, OVA reduced SOD activity, GSH content in lungs, and GGT activity in serum (p<0.05). L. dentata extract treatment in asthma model reduced elevated IgE, triglycerides, total cholesterol, glucose levels in serum, and MDA in lungs (p<0.05), while it increased GSH content in lungs (p<0.05). These results suggest the possibility that L . dentata extract can exert suppressive effects on asthma, and may provide evidence that it is a useful agent for the treatment of allergic airway disease, it also limits oxidative stress induced by OVA. L. dentata extract appears to have hypolipidemic and hypoglycemic activities.
... β-Caryophyllene is widely used as a flavoring agent and additive in food and cosmetics applications [3,4]. The pharmaceutical industry uses the β-caryophyllene due to its potentialized effect as anesthetic, antifungal, antiviral, spasmolytic and anti-inflammatory [5][6][7][8]. ...
Article
Molecularly imprinted polymers provide an excellent platform for the modification of selective electrodes for sensing applications. Herein, we present a novel modified carbon paste electrode (CPE) with a selective molecularly imprinted polymer (MIP) for recognition of sesquiterpene β-caryophyllene, constituted of important plants oil-resins and extracts. The non-covalent MIP was synthesized using AA, EGDMA, and AIBN as a functional monomer, cross-linker and initiator agent, respectively. Structural and chemical characterization of the synthesized MIP was conducted through scanning electron microscopy (SEM), Fourier-transform infrared (FT-IR) spectroscopy, Raman spectroscopy and X-ray photoelectron spectroscopy (XPS). It was possible to verify the functional features of the synthesized MIP related to the extraction process of the template molecule. The CPE modified with MIP for sesquiterpene β-caryophyllene recognition was characterized by electrochemical techniques as cyclic voltammetry (CV) and square wave voltammetry (SWV). The highest selective recognition electrode enables to detect concentrations in the range between 1.5 × 10 ⁻⁷ and 7.5 × 10 ⁻⁷ M, showing great potential for applications in monitoring content of sesquiterpene β-caryophyllene in technological processes and for predicting the quality of extracts, oils, and resins of plants.
... Lavender infusion removes headaches and insomnia. Externally it can be used for muscular pain, oral hygiene, herpetic lesions, insect bites, antiseptic and healing for surface wounds and burns by direct application of volatile oil, even undiluted, quickly absorbed by the skin, etc. ( Konstantia et al., 1998;Ghelardini et al., 1999;Valiollah et al., 2003;Koulivand et al., 2013;Kutlu et al., 2013). ...
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Lavender (or French lavender) is a plant that has gained a lot of popularity in Romania in recent years, both for aromatic and medicinal use, as well as for ornamental purposes. Volatile oil consists of numerous monoterpenic compounds, predominantly linalool (freely or esterified-especially as acetate) and esters, triterpene acids, coumarins, flavones, resins, a bitter principle, polyphenols (eg rosmarinic acid). The production and quality of volatile oil are greatly influenced by pedoclimatic conditions. For therapeutic purposes, inflorescences or volatile oil can be used in aromatherapy, inhalation or massage, with beneficial action in neurological diseases (including migraines, insomnia, epilepsy)-relaxing, antispasmodic, anticonvulsant and neuroprotective action (anticonvulsive and neuroprotective); carminative, analgesic, sedative, hypotensive, antimicrobial, antifungal, antitussive, collagogue, choleretic, diuretic, general tonic, cardiotonic and tonic aperitif, deodorant and many others.
... In pharmacological and biological researches, L. angustifolia extracts, fractions and essential oils are reported to have relaxant, hypnotic, anti-convulsive, spasmolytic, antioxidant, local anesthetic, antibacterial and anti-inflammatory effects (17)(18)(19)(20)(21). Recent pharmacological studies confirm the traditional use of lavender for the treatment of painful and inflammatory conditions (10). ...
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Introduction: Lavender (Lavandula angustifolia Mill) is a herbal medicine widely used for gastrointestinal (GI) disorders. However, its pharmacological action on isolated ileum has not been studied. In this research effect of hydroalcoholic extract of L. angustifolia on isolate ileum contractions was studies and compared with loperamide. Methods: Hydroalcoholic extract of the plant was prepared by percolation method. The total flavonoid contents were assessed by colorimetric technique. A portion of rat ileum was suspended in an organ bath containing Tyrode's solution. The tissue was kept under 1 g tension at 37°C and continuously gassed with O2. The tissue was stimulated with KCl (80 mM), acetylcholine (ACh, 2 µM) and electrical field stimulation (EFS). Effect of the L. angustifoliaextract was studied on ileum contractions and compared with that of loperamide. Results: The yield of hydroalcoholic extract was 17% with total flavonoid content of 185 µg/ mL in the stock solution. Loperamide in concentration dependent manner inhibited ileum contractile response to KCl, ACh and EFS. Hydroalcoholic extract of L. angustifolia (8-512 µg/mL) concentration dependently inhibited ileum contraction induced by KCl (IC50 = 88±21 µg/mL), ACh (IC50 = 119±251 µg/mL) and EFS (IC50=87±33 µg/mL). The vehicle had no significant effect on ileum contractions. Conclusion: From this study it was concluded that L. angustifolia extract at microgram concentration shows an inhibitory effect on rat ileum smooth muscle. Therefore, isolation and identification of active ingredients are recommended.
... This sensation is stimulated by the effect of menthol on heat-detecting nerve ends. EOs like eugenol, linalool, linalyl acetate, benzoin and thyme were also used for hundreds of years as local anaesthetics and in dentistry as antiseptics [39]. Thymol has been found to have prominent antiseptic effects [40]. ...
Background - At present, 'pharmaco-epigenomics' constitutes the hope in cancer treatment owing to epigenetic deregulation- a reversible process and playing a role in malignancy. Objective: Chemotherapy has many limitations like host-tissue toxicity, drug resistance. Hence, it is imperative to unearth targets to better treat cancer. Here, we intend to repurpose a set of our previously synthesized difluorinated propanediones (PR) as histone lysine methyltransferase inhibitors (HMTi). Methods: The cell lines of leukemic origin viz. histiocytic lymphoma (U937) and acute T-cell leukemia (JURKAT) were treated with PR-1 to 7 after docking studies with active pocket of HMT. The cell cycle analysis, in vitro methylation and cell proliferation assays were carried out to delineate their physiological role. Results - A small molecule PR-4, at 1 and 10μM, has shown to alter the methylation of histone H3 and H4 in both cell lines. Also, treatment shows an increase in G2/M population and a subsequent decrease in the G0/G1 population in U937. In JURKAT, an increase in both G2/M and S phase population was observed. The sub-G1 population showed a steady rise with increase in dose and prolonged time intervals in U937 and JURKAT cell lines. In SRB assay, the PR showed a cell growth of 42.6 and 53.4% comparable to adriamycin; 44.5 and 53.2% in U937 and JURKAT, respectively. The study suggests that PR-4 could emerge as a potential HMT inhibitor. Conclusion - The molecule PR-4 could be a lead in developing more histone lysine methyltransferases inhibitors with potential to be pro-apoptotic agents.
... ) . Koulivand et al., 2013;Ghelardini et al., 1999 ...
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This study was conducted to compare the effect of two anesthetizers Topped lavender essential oil (Lavandula angustifolia) and clove oil on some hematological and serum biochemical parameters in common carp (Cyprinus carpio) juveniles. Common carp juveniles exposed to three treatments including optimum concentration of Topped lavender essential oil (170 mg l-1), clove oil (35 mg l-1) and control and hematological, serum biochemical and stress parameters were determined at different times including 0, 3 and 24 h after anesthetizing. The results showed the effect of treatment (anesthetizing agent) on all hematological parameters, the effect of time on WBC, Hb, MCH and MCHC, the interaction effect of treatment and time on Hct and RBC and the effect of treatment, time and the interaction effect of them on all serum biochemical parameters were significant (p0.05), but in clove oil at the start of anesthetizing time (0) was significantly higher than other sampling times (p
... According to the literature, LEO has antibacterial, antifungal, antioxidant, analgesic, anti-inflammatory, and antispasmodic properties (Yang et al., 2010;Prusinowska andŚmigielski, 2014;Carrasco et al., 2016;Giovannini et al., 2016). Studies on animal and human models alike have shown that lavender has potential immunostimulatory, anxiolytic, sedative, hypnotic, analgesic, and anticonvulsant effects, and may also improve one's mood (Ghelardini et al., 1999;Sasannejad et al., 2012;Prusinowska andŚmigielski, 2014). ...
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The aim of this study was to evaluate growth performance, selected biochemical blood parameters, and the microbiota of ileal digesta in broiler chickens provided with drinking water containing an addition of natural lavender essential oil (LEO). The experiment was carried out on a commercial farm using n = 300 unsexed Ross-308 broiler chickens. One-day-old chicks were randomly assigned to three groups of 100 chickens each (five replications, 20 individuals each). The control group broilers were provided with drinking water without the addition of LEO. Groups LEO1–42 and LEO22–42 had access to water containing 0.4 ml/L LEO (for 6 h/day) from days 1 to 42 (LEO1–42) and 22 to 42 (LEO22–42). Body weight, feed intake, water intake, and mortality were recorded throughout the experiment. The analyses reveal that the addition of LEO has a positive effect on body weight in the second period of rearing (d 22–24). Treatment broilers (LEO1–42 and LEO22–42) weighed on average 6.35% more compared to the control (P < 0.01). LEO addition positively affected weight gains and feed conversion ratio (P < 0.01) in the second period of rearing (d 22–24). No differences were found between the groups feed intake, water intake, survival rate, and blood biochemical parameters (P > 0.05). The addition of LEO to drinking water had a positive impact on the gut microflora of the ileum: the numbers of pathogenic microorganisms decreased (Escherichia coli and coliform) while the number of probiotic bacteria increased (P < 0.01).
... 754 Its local anesthetic effects 755 were equal to procaine and menthol. 756 Analgesic effects have also been attributed to adenosine A 2A activity 757 and by ionotropic glutamate receptors including AMPA, NMDA, and kainate. 758 Linalool significantly decreased morphine opioid usage in gastric banding surgical patients following lavender inhalation vs placebo. ...
Article
Background.—Comprehensive literature reviews of historical perspectives and evidence supporting cannabis/ cannabinoids in the treatment of pain, including migraine and headache, with associated neurobiological mechanisms of pain modulation have been well described. Most of the existing literature reports on the cannabinoids Δ9 -tetrahydrocannabinol (THC) and cannabidiol (CBD), or cannabis in general. There are many cannabis strains that vary widely in the composition of cannabinoids, terpenes, flavonoids, and other compounds. These components work synergistically to produce wide variations in benefits, side effects, and strain characteristics. Knowledge of the individual medicinal properties of the cannabinoids, terpenes, and flavonoids is necessary to cross-breed strains to obtain optimal standardized synergistic compositions. This will enable targeting individual symptoms and/or diseases, including migraine, headache, and pain. Objective.—Review the medical literature for the use of cannabis/cannabinoids in the treatment of migraine, headache, facial pain, and other chronic pain syndromes, and for supporting evidence of a potential role in combatting the opioid epidemic. Review the medical literature involving major and minor cannabinoids, primary and secondary terpenes, and flavonoids that underlie the synergistic entourage effects of cannabis. Summarize the individual medicinal benefits of these substances, including analgesic and anti-inflammatory properties. Conclusion.—There is accumulating evidence for various therapeutic benefits of cannabis/cannabinoids, especially in the treatment of pain, which may also apply to the treatment of migraine and headache. There is also supporting evidence that cannabis may assist in opioid detoxification and weaning, thus making it a potential weapon in battling the opioid epidemic. Cannabis science is a rapidly evolving medical sector and industry with increasingly regulated production standards. Further research is anticipated to optimize breeding of strain-specific synergistic ratios of cannabinoids, terpenes, and other phytochemicals for predictable user effects, characteristics, and improved symptom and diseasetargeted therapies.
... In addition to anxiolytic and anti-depressant properties, LNL (single dose of 5, 10 or 20 mg/kg, i. p.) shows anti-nociceptive effects, as evidenced by the reversal of PAC-induced allodynia and hyperalgesia via the involvement of the peripheral opioid system [112]. Accordingly, LNL (50 mg/kg) (as well as linalyl acetate) evoked local anesthesia in vivo [113]. With various models of chronic inflammatory and neuropathic pain, LNL treatment significantly reduced mechanical hypersensitivity and edema in mice [114]. ...
Article
Cannabaceae plants Cannabis sativa L. and Humulus lupulus L. are rich in terpenes-both are typically comprised of terpenes as up to 3-5% of the dry-mass of the female inflorescence. Terpenes of cannabis and hops are typically simple mono-and sesquiterpenes derived from two and three isoprene units, respectively. Some terpenes are relatively well known for their potential in biomedicine and have been used in traditional medicine for centuries, while others are yet to be studied in detail. The current, comprehensive review presents terpenes found in cannabis and hops. Terpenes' medicinal properties are supported by numerous in vitro, animal and clinical trials and show anti-inflammatory, antioxidant, analgesic, anticonvulsive, antidepressant, anxiolytic, anticancer, antitumor, neuroprotective, anti-mutagenic, anti-allergic, antibiotic and anti-diabetic attributes, among others. Because of the very low toxicity, these terpenes are already widely used as food additives and in cosmetic products. Thus, they have been proven safe and well-tolerated.
... It exhibits anti-inflammatory and analgesic activity [333][334][335] as well as anti-nociception via activation of opioidergic and cholinergic systems [333], anticonvulsant via antiglutamatergic and GABA neurotransmitter systems [336][337][338][339][340], anti-anxiety/stress [341][342][343][344], sedation [343,[345][346][347], and anti-insomnia properties [100]. Its local anesthetic effects [348] were equivalent to procaine and menthol [349], and analgesic effects have been attributed to adenosine A 2A activity [350] and ionotropic glutamate receptors including AMPA, NMDA and kainate [351]. Morphine opioid usage in gastric banding surgical patients was significantly decreased following lavender inhalation vs. placebo, and this was attributed to the linalool concentration [352]. ...
Article
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Background Medicinal cannabis registries typically report pain as the most common reason for use. It would be clinically useful to identify patterns of cannabis treatment in migraine and headache, as compared to arthritis and chronic pain, and to analyze preferred cannabis strains, biochemical profiles, and prescription medication substitutions with cannabis. Methods Via electronic survey in medicinal cannabis patients with headache, arthritis, and chronic pain, demographics and patterns of cannabis use including methods, frequency, quantity, preferred strains, cannabinoid and terpene profiles, and prescription substitutions were recorded. Cannabis use for migraine among headache patients was assessed via the ID Migraine™ questionnaire, a validated screen used to predict the probability of migraine. Results Of 2032 patients, 21 illnesses were treated with cannabis. Pain syndromes accounted for 42.4% (n = 861) overall; chronic pain 29.4% (n = 598;), arthritis 9.3% (n = 188), and headache 3.7% (n = 75;). Across all 21 illnesses, headache was a symptom treated with cannabis in 24.9% (n = 505). These patients were given the ID Migraine™ questionnaire, with 68% (n = 343) giving 3 “Yes” responses, 20% (n = 102) giving 2 “Yes” responses (97% and 93% probability of migraine, respectively). Therefore, 88% (n = 445) of headache patients were treating probable migraine with cannabis. Hybrid strains were most preferred across all pain subtypes, with “OG Shark” the most preferred strain in the ID Migraine™ and headache groups. Many pain patients substituted prescription medications with cannabis (41.2–59.5%), most commonly opiates/opioids (40.5–72.8%). Prescription substitution in headache patients included opiates/opioids (43.4%), anti-depressant/anti-anxiety (39%), NSAIDs (21%), triptans (8.1%), anti-convulsants (7.7%), muscle relaxers (7%), ergots (0.4%). Conclusions Chronic pain was the most common reason for cannabis use, consistent with most registries. The majority of headache patients treating with cannabis were positive for migraine. Hybrid strains were preferred in ID Migraine™, headache, and most pain groups, with “OG Shark”, a high THC (Δ9-tetrahydrocannabinol)/THCA (tetrahydrocannabinolic acid), low CBD (cannabidiol)/CBDA (cannabidiolic acid), strain with predominant terpenes β-caryophyllene and β-myrcene, most preferred in the headache and ID Migraine™ groups. This could reflect the potent analgesic, anti-inflammatory, and anti-emetic properties of THC, with anti-inflammatory and analgesic properties of β-caryophyllene and β-myrcene. Opiates/opioids were most commonly substituted with cannabis. Prospective studies are needed, but results may provide early insight into optimizing crossbred cannabis strains, synergistic biochemical profiles, dosing, and patterns of use in the treatment of headache, migraine, and chronic pain syndromes.
... Terpenoids demonstrate effects on the brain at very low ambient air levels in animal studies [13]. Generally speaking terpenoids contribute a sedative and anxiolytic effect to cannabis with more specific pharmacological effects attributed to individual terpenoids; such as, pinene exhibiting antibiotic activity [14] or β-caryophyllene providing gastric cytoprotective activity [15] or the anticonvulsive effects of β-myrcene [16]. ...
... Some other studies reported that L. Stoechas exhibit Local anaesthetic effects, both in-vivo and in-vitro animal experiments. [36] Clinical studies ...
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Ustukhuddoos has been used as a healing agent since ancient times. Renowned Unani physicians Jalinus and Desquredus discovered varied medicinal properties of this plant origin drug. They recommended using this drug, especially in cerebral disorders. Lavandula stoechas Linn. belongs to Lamiaceae / Labiatae family. This is an evergreen shrub usually grows to 30-100 cm in height. The leaves are 1-4 cm long, greyish and tomentose. The flowers are pink to purple in color appear in late spring and early summer season. In Unani Medicine, it is commonly known as Ustukhuddoos. Unani literatures has mentioned many pharmacological actions of this drug such as Jaroob-e-Dimagh (brain scavenger), Daf-e-Sauda (evacuation of black bile), Da-fe-Tashannuj (anti-convulsant), Mufarrah-e-Qalb-Wa-Dimagh (exhilarant of heart and brain), Muqaww-i-Aasab (nervine tonic) etc, and it is used in several ailments such as Zof-e-Dimagh, Nisyan (dementia), Malankholia (malancholia), Waja al qalb (angina pectoris), Suda-e-Muzmin (a chronic headache), Falij (paralysis), Laqwa (facial paralysis) etc. Many scientific studies have been proved that Ustukhuddoos is significantly useful in several neurological disorders such as anxiety, depression, convulsions and cerebral ischemia etc. The present review is an attempt to portray this wonder drug Ustukhuddoos in the light of scientific studies carried out pertaining to brain and nerves which is rightly coined as the "broom of the brain".
... Lavender oil (Lavandulae aetheroleum) is known for its antibacterial, antifungal, carminative, antiflatulence, antiholic, sedative and antidepressive activities [12]. Lavender oil is used in phytotherapy to relief cough, neuralgia, insomnia but also for bath and compress [13][14][15]. According to World Health Organization, medicinal plants would be the best source to obtain a variety of drugs. ...
Article
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Foodborne pathogens are microorganisms as well as a number of parasites, which are capable of infecting humans via contaminated food or water. In recent years, diseases caused by foodborne pathogens have become an important public health problem in the world, producing a significant rate of morbidity and mortality. In traditional medicine, numerous plants and their extracts have used for thousands of years to treat health disorders. Although many studies were made on natural herbs, those involving the antimicrobial, antioxidant and antimutagenic activity of the herb species are rather rare. This study researches the biological activities of ethanol and methanol extracts of Lavandula stoechas L., which are prevalent in Turkey. In this study, 8 food pathogens were used for antimicrobial activity studies. Antimicrobial activity studies were done by disk diffusion assay and MIC (minimum inhibitory concentration). DPPH method was used for non-enzymatic antioxidant activity. The Lavandula extracts were screened for their antimutagenic activity against sodium azide by Ames test in absence of rat microsomal liver enzyme (-S9). The ethanol and methanol extracts of Lavandula stoechas showed antibacterial activity (7 mm) against most of bacteria. The antifungal activity of L. stoechas was not determined against C. albicans RSKK02029. The lowest MIC value was determined as 3250 μg/mL. The highest radical inhibition was determined as 79 % by Lavandula stoechas flower methanol extract. The flower extract of L. stoechas (12500 μg/plate) was found to have its highest antimutagenic activity for Salmonella Typhimurium TA98. This inhibition value is 42 %. L. stoechas leaves extracts (6250 and 3125 μg/plate) showed a moderate positive inhibitory effect for Salmonella Typhimurium TA98, and TA100. L. stoechas flower extracts (12500 and 6250 μg/plate) showed a moderate positive inhibitory effect (respectively 31 and 30 %) for Salmonella Typhimurium TA100. The extracts of L. stoechas have antimicrobial, antioxidant and antimutagenic activities.
... Lavender oil (Lavandulae aetheroleum) is known for its antibacterial, antifungal, carminative, antiflatulence, antiholic, sedative and antidepressive activities [12]. Lavender oil is used in phytotherapy to relief cough, neuralgia, insomnia but also for bath and compress [13][14][15]. According to World Health Organization, medicinal plants would be the best source to obtain a variety of drugs. ...
... This monoterpenic ester has also been linked to anti-inflammatory and peripheral analgesic properties (Moretti et al., 1997). Tests on rabbit conjunctiva and rat phrenic nerve-hemidiaphragm preparations were conducted to determine L. angustifolia EO's local anesthetic activity on rabbit conjunctiva (Ghelardini et al., 1999). The EO, as well as its main constituent's linalool and linalyl acetate, were found to reduce electrically evoked contractions of the rat phrenic-hemidiaphragm in a dose-dependent manner. ...
Article
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Lavender is a very old herb that has been used for centuries as an antiseptic and relaxant. The demand for its essential oil continues to grow on a global scale. The fact remains that harvesting at the right time of growth is critical to maximizing the rate of active ingredients found in the plant. Thus, in the current study, L. angustifolia plants were collected at various growth stages (pre-flowering, mid-flowering, and post-flowering) from Adana, Turkey in order to determine the most suitable harvest time for the highest amount of essential oils and its important compounds. The highest flower essential oil content (7.50 mL 100 g-1) was obtained at mid-flowering of the third year of plantation. The major compounds for L. angustifolia were linalyl acetate (25.63-31.63%), linalool (16.33-24.79%), nerol (8.83-13.43%), beta-farnesene (3.67-5.70%), β-cis-ocimene (1.76-8.14%), respectively. The obtained data have been inquired by principal components analysis (PCA), allowing differentiation of plantation ages and growth stages. Compared to the plantation ages, essential oil content and linalool content increased significantly in the third year of cultivation. As a result, the most suitable harvest time may be considered as mid-flowering in terms of essential oil content and in terms of high linalyl acetate and linalool content.
... De plus, le lavandin a démontré des propriétés anticarcinogènes, principalement du au constituent perillyl alcool (Bellanger, 1998). L'HE de lavande a également montré par des tests cliniques une nette amélioration du cycle de sommeil Graham et al., 2003 une activité anesthésique locale (Ghelardini et al., 1999). De plus, un effet spasmolytique sur les muscles lisses a été démontré in vitro (Lis-Balchin and Hart, 1997). ...
Research
For several years, the genus Lavandula has known a considerable interest by the scientific community, through the discovery of these many therapeutic applications, especially those related to the central nervous system. This document reviews these different characteristics, including the overall chemical composition of essential oils and its relationship to biological properties (antioxidant, anti-inflammatory and antimicrobial activity).
... Lavender is a typical aromatic plant of the Labiatae family used as a folk medicine, which is mainly distributed in the south of France and Xinjiang in China (Xie et al. 2002). The essential oil of this plant has been popular all over the world, which has been reported for various medical efficacies in terms of as sedative hypnotic, anaesthetic activity, anti-inflammatory, anti-bacterial, anti-oxidation and anti-mutation (Ghelardini et al. 1999;Cavanagh and Wilkinson 2002;Yadikar 2017). However, the content of essential oil in dried lavender flowers is only about 1.5% (Huang et al. 2018), and a considerable amount of the remaining materials after the essential oil being previously removed have merely been used as livestock feed and crop fertilizer (Yadikar et al. 2018a), that causes squander of resources. ...
Article
A phytochemical investigations on the n-butanol fraction of Lavandula angustifolia Mill. residues resulted in the isolation of ten compounds, including two new ones, 4,40dimethoxy-2,20di-Ob-D-glucopyranosyl-truxinate (1) and 2-(b-D-glucosyloxy)-trans-cinnamic acid butyl ester (2), along with eight known compounds. The structures of compounds were confirmed by NMR and HRESI-MS techniques and comparison with published data. The NMR data for 3 were attributed for the first time. Compound 2 was proofed to be a natural compound in plant rather than a butyl ester artifact formed by esterification reaction with butanol by comparative HPLC-DAD analysis with the ethanol extract which was obtained prior to the application of butanol. All isolated compounds were evaluated for their antioxidant and anti-hypoglycaemic activities. Among them, compounds 4 and 5 showed strong anti-oxidant activities against DPPH with IC50 values of 12.99 and 31.74 lM, respectively. Compound 5 exhibited moderate inhibitory activity against PTP1B with an IC50 value of 31.28 lM.
... It is worth mentioning that, amongst Lavandula species, which are all rich in linalyl acetate and linalool, lavandin (Lavandula × intermedia) has the highest content of 1,8-cineole, accounting for up to the 13% of its composition (Renaud et al., 2001), but with far less camphor (between 5% and 11%) (Blumenthal et al., 1999;Council of Europe, n.d.;Health Canada, 2004;Millqvist et al., 2013;Nair, 2001;Tisserand and Young, 2013) when compared to L. latifolia, thus making lavandin a safer and easier alternative to L. latifolia. Beyond the action of eucalyptol, linalyl acetate and linalool, which are derived from lavender essential oil, showed some in vivo anesthetic activity when tested on rabbits (Ghelardini et al., 1999). Additionally, linalyl acetate demonstrated spasmolytic properties on smooth muscles in a laboratory experiment (de Sousa et al., 2011). ...
Article
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Introduction The involvement of the upper respiratory tract is common in COVID-19, and the majority of patients are treated at home with a mild-to-moderate form of the disease. Many approaches based on essential oils have been proposed for the symptomatic treatment of COVID-19. This work aims to outline the potential and safe evidence-based uses of essential oils and their major components for the clinical management of mild respiratory symptoms caused by uncomplicated coronavirus infections, including SARS-CoV-2. Due to their wide use, a focus on the constituents eucalyptol and menthol has been provided. Methods An overview of the scientific literature with a critical discussion of retrieved evidence and clinical recommendations. Results In general, eucalyptol and essential oils or blends whose content is rich in it, may be used as an integrative remedy for the symptomatic improvement of patients with mild and uncomplicated infections caused by coronaviruses. Menthol is not recommended in patients with COVID-19, due to a potential reduction of the self-perception of dyspnea, which can lead infected patients to underestimate the actual disease severity and to delay medical attention. Discussion Based on available evidence, symptomatic remedies for COVID-19, such as essential oils and their isolated compounds, can be useful, but are not an alternative to standard medical therapy and do not exempt patients from following precautionary measures issued by health authorities. Clinical recommendations on the appropriate use of essential oils for the management of upper airway symptoms of COVID-19 are provided. Further studies on the topic are advised.
... Several agarwood compounds function as medicines: guaiacol (anticancer, antiimflammatory, antiseptic, antioxidants) [22,23]; linalool (antiimflammatory, peripheral analgesic activities) [24][25][26]; benzylacetone (antiepileptic, antiseptic, antihypertension) [27,28]; cumene (antibacterial, antioxidants) [29,30]; globulol (antioxidants, antimutagenic) [31][32][33]; aromadendrene (anticancer, antitumor, antimicrobial) [34,35]; hydrocinnamic acid (antityrosinase, anticolagenase) [36]; humulane (antioxidants, antiimflammatory) [37], etc. ...
Article
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This research aimed to study about chemical composition and anti-cancer activities of natural agarwood and cultivated agarwood ( Gyrinops vertegii [Gilg.] Domke). Agarwood used in the research was of lowest qualities, which comprised agarwood with natural kemedangan type (A), with cultivated kemedangan-I type (B1), and with cultivated kemedangan-II type (B2), all after methanol extraction. Chemical composition was examined using GC-MS instrument, meanwhile tests on lungs associated anticancer activities (A549’s cancer cells) were performed using MTT method. Chemical composition in low-quality agarwoods was predominantly sesquiterpene compounds, comprising among others guaiacol, cumene, aromadendrene, aplha-humulene, velleral, etc; and conservely did not contain chromone derivative compounds which are compounds characterizing quality agarwood. Low-quality agarwood extracts afforded efficacious potency as anticancer actions against A549’s lungs-attacking cancer cells with IC 50 values at 144.92 µgmL ⁻¹ (A); IC 50 at 206.88 µgmL ⁻¹ (B1), and IC 50 187.97 µgmL ⁻¹ (B2).
... It may be effective in treatments of several neurological disorders since it has neuroprotective features [39,40]. Furthermore, it possesses anaesthetic activity [41] as well as antifungal [42] and antibacterial activities [43,44]. The anti-inflammatory effect of LEO was tested in acute inflammation models of pleurisy and ear oedema [45,46]. ...
Article
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Background Pseudomonas aeruginosa is the most common Gram-negative bacterium associated with nosocomial respiratory infections. Lavender essential oil is mainly used in aromatherapy, but it has several pharmacological and therapeutic properties. Furthermore, it possesses antifungal and antibacterial activities. The anti-inflammatory activity of essential oils may depend on the composition and the ratio of the compounds. The constitution of the essential oils extracted from the different stages of flowering period varies, which makes it plausible that the collection time of the flowers influences the anti-inflammatory effects. Different types of essential oils reduce inflammation acting similarly by modulating the activity and action of the NFκB signalling pathway, which is the major regulator of the transcription of pro-inflammatory cytokines. Methods Lavender essential oils were distilled from lavender plant cultivated in Hungary and the flowers were harvested at the beginning and at the end of flowering period. The experiments were carried out on THP-1 human monocyte/macrophage cell line as in vitro cell culture model for monitoring the effects of lavender essential oils and the main compound linalool on P. aeruginosa LPS stimulated inflammation. The mRNA and protein levels of four pro-inflammatory cytokines, IL-6, IL-1β, IL-8 and TNFα were determined by Real Time PCR and ELISA measurements. The effects of essential oils were compared to the response to two NFκB inhibitors, luteolin and ACHP. Results Linalool and lavender essential oil extracted from plants at the beginning of flowering period were successful in decreasing pro-inflammatory cytokine production following LPS pretreatment. In case of IL-8 and IL-1β lavender oil showed stronger effect compared to linalool and both of them acted similarly to NFκB inhibitors. Pretreatments with linalool and lavender essential oil/beginning of flowering period prevented pro-inflammatory cytokine production compared to LPS treatment alone. Although lavender essential oil/end of flowering period decreased IL-6, IL-1β and IL-8 mRNA expression in case of LPS pretreatment, it was not capable to reduce cytokine secretion. Conclusion Based on our results it has been proven that lavender essential oil extracted at the beginning of flowering period is a potent inhibitor of the synthesis of four pro-inflammatory cytokines IL-6, IL-8, IL-β and TNFα of THP-1 cells. This supports the relevance of the collection of the lavender flowers from early blooming period for essential oil production and for the utilization as an anti-inflammatory treatment.
... Uleiul de lavandă modulează starea de excitabilitate a unor receptori interni, crescând pragul de excitabilitate al miocardului (efect antiaritmic). S-a observat de asemenea și o activitate de favorizare a normalizării nivelului plasmatic al lipidelor totale [62]. ...
... Research in rats suggests that 24 may protect the immune system from undesirable changes caused by stress (Nakamura et al. 2009). The local anaesthetic effects of 24 are comparable to procaine (Ghelardini et al. 1999). Evidence shows that administering 24 by inhalation can significantly reduce opioid consumption in postoperative conditions (Kim et al. 2007). ...
Article
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Cannabis spp. are some of the most controversial medicinal plants in the world. They contain great amounts of biologically active secondary metabolites, including the typical phenolic compounds called cannabinoids. Because of their low toxicity and complex biological activities, cannabinoids can be useful in the therapy of various diseases, but adverse psychological effects (of Δ9-THC in particular) raise concerns. This review summarizes the current knowledge of selected active C. indica compounds and their therapeutic potential. We summarize the main compounds contained in cannabis, the mechanisms of their effects, and their potential therapeutic applications. Further, we mention some of the clinical tests used to evaluate the efficacy of cannabinoids in therapy.
... It is also useful for nervous breakdown, nervous tension [26][27][28] , alopecia 29 , enhancing cognitive performance and mood behaviour 30 . It has analgesic, anticonvulsive 9 and local anesthetic effect 31 . On the basis of above descriptions, it is vindicated that this traditional plant is also have very worthy and almost similar medicinal applications, but as per Unani physicians, ambiguous descriptions mentioned in classical Unani literature provide indistinct idea of identification to this plant. ...
Article
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Lavandula stoechas L. (Lamiaceae) is a medicinal plant of traditional Unani, Iranian and Tunisian systems of medicine. It has a unique attribute to expel out and remove all impurities and obstructions and reinvigorate the brain power, honored as broom of brain in classical Unani literatures. To establish clear identification between L. stoechas (LS) and L. officinalis (LO) standard operating parameters, TLC fingerprinting and physicochemical and histo-anatomical studies were done. LS exhibited significantly higher physical values for their standardization and quality parameters with respect to LO. Histo-anatomical disquisition and chemo-microscopic studies of the drug revealed that presence of substantial and marked diagnostic feature to LS having large bract, brown colored flexible peduncle, presence of exorbitant number of uniseriate and multi seriate covering and uniseriate glandular trichomes leading to soft stem and peduncle. It has distinguished and well-developed phloem, centrally filled with parenchymatous cells, with camphoric stench along with bitter in taste while LO has lesser hairs, hard stem and peduncle, greenish color, presence of centrally hollow pith, indiscriminate bract, and flowers are without stalks with pleasant aroma. Seeds of LS are yellowish brown, frivolous weight and very small in size while LO have blackish seeds and are comparatively larger in size and weight.
... It is pertinent to mention that lavender oil (LO) from Lavandula plants (Lavender) shows significant antiviral activity (Alghaith et al., 2021), and LO creams have demonstrated successful treatment against herpes labialis lesions (Altaei & Ahmed, 2012). Moreover, the anesthetic activity of LO can be of immense use in alleviating pain of lesions in herpes labialis (Ghelardini et al., 1999). ...
Article
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Herpes labialis, caused by herpes simplex virus type 1, is usually characterized by painful skin or mucosal lesions. Penciclovir (PV) tablets are found to be effective against herpes labialis but suffer from poor oral bioavailability. This study aimed to combine the benefits of PV and lavender oil (LO), which exhibits anesthetic activity, in the form of a self-nanoemulsifying drug delivery system (SNEDDS) for the treatment of herpes labialis. Toward this purpose, LO (oil), Labrasol:Labrafil M1944 CS in the ratio of 6:4 (surfactant mixture), and Lauroglycol-FCC (co-surfactant, selected based on the solubility of PV) were evaluated as the independent factors using a distance quadratic mixture design. The formulation was optimized for the minimum globule size and maximum stability index and was determined to contain 14% LO, 40.5% Labrasol:Labrafil 1944 (6:4), and 45.5% Lauroglycol-FCC. The optimized PV-LO-SNEDDS was embedded in chitosan hydrogel and the resulting formulations coded by (O3) were prepared and evaluated. The rheological studies demonstrated a combined pseudoplastic and thixotropic behavior with the highest flux of PV permeation across sheep buccal mucosa. Compared to a marketed 1% PV cream, the O3 formulation exhibited a significantly higher and sustained PV release, nearly twice the PV permeability, and a relative bioavailability of 180%. Overall, results confirm that the O3 formulation can provide an efficient delivery system for PV to reach oral mucosa and subsequent prolonged PV release. Thus, the PV-LO-SNEDDS embedded oral gel is promising and can be further evaluated in clinical settings to establish its therapeutic use in herpes labialis.
... Salvia officinalis essential oil has been also reported to possess various properties such as antibacterial (Delamare et al., 2007;Bouaziz et al., 2009), antioxidant (Bozin et al., 2007) and insecticidal (Pavela, 2005). Lavandula angustifolia essential oil exhibits significant potentials such as anaesthetic (Ghelardini et al., 1999), anti-inflammatory and analgesic (Hajhashemi et al., 2003), antifungal (D'auria et al., 2005), antimicrobial (de Rapper et al., 2013), and antimutagenic (Evandri et al., 2005). Various significant roles of Ocimum basilicum essential oil have reported such as antioxidant (Politeo et al., 2007;Hussain et al., 2008), antigiardial (de Almeida et al., 2007 and antimicrobial (Hussain et al., 2008). ...
Article
Drought stress is of the major abiotic stress factors shifting the primary and secondary metabolism of the plants. The mechanisms corresponding to the stress-plant interaction and subsequently impacts on plants have been well-documented. However, there are insufficient documents regarding with drought experience influence on the plant metabolism. Along with the study, the drought experience on the essential oil compounds of rosemary, sage, lavender and basil leaves were for the first time-investigated. Briefly, experimental plants were firstly divided into two groups: irrigated and non-irrigated groups for seven days and then all plants were fully-irrigated as recovery stage. After recovery stage, both plant groups were divided into two more groups as irrigated and non-irrigated for more seven days. For the analysis, leaf samples were collected at Day-0, Day-7 (first cycle), Day-14 (second cycle) and Day-21 (third cycle) for each group. Since the accumulation of the secondary me-tabolites has been considered as an adaptive strategy of the plants in response to the stress that matters, the changes in essential oil compounds in order to investigate the possible influence of drought experience were profiled. Along with the study, specifically, the behaviour of common components including α-pinene, D-li-monene, eucalyptol, and camphor in rosemary, sage, lavandula, and basil were assessed. Of those components, α-pinene decreased with the maturity and drought stress in rosemary but increased in lavender. In sage, it sharply decreased with the stress but recurrent drought increased. In basil, first stress and recurrent stress increased the percentage of the component. D-limonene increased with first and recurrent drought stress in rosemary and basil. On the other hand, the percentage decreased with the first stress but increased with the recurrent drought stress in sage and lavender. Eucalyptol increased by the maturity and drought stress in all plants. Camphor percentage increased with the first stress in all plants but the recurrent drought effects were different for all plants. The present study might be fundamental for the relevant researches and forthcoming studies are required to be addressed on molecular, physiological and biochemical responses associated with essential oil production.
... Natural monoterpenes as well as their synthetic derivatives exert various pharmacological properties (Bardon, Picard, & Martel, 1998;Crowell, 1999;Raphael & Kuttan, 2003;Wagner & Elmadfa, 2003) and have applications in health care products (Ajikumar et al., 2008;Nöldner, Germer, & Koch, 2011). In particular, linalool showed sedative effects at the central nervous system (Buchbauer, Jirovetz, & Jäger, 1991;Re et al., 2000), and various anticonvulsant, anesthetic, analgesic, spasmolytic and antinociception activities (Elisabetsky, Brum, & Souza, 1999;Ghelardini, Galeotti, Salvatore, & Mazzanti, 1999;Lis-Balchin & Hart, 1999;Peana et al., 2002Peana et al., , 2003. Linalool is one of the main constituents of Silexan, an active ingredient approved for treatment of restlessness and mild anxiety in Germany (Nöldner et al., 2011). ...
Article
This study aimed to explore common purslane (Portulaca oleracea L.) as potential raw substrate to develop novel functional preparations through lactic acid fermentation. Different lactic acid bacteria were used as single starter. P. oleracea fermented with Lactobacillus kunkeii B7 and Lactobacillus plantarum POM1 resulted in decreased levels (ca. 30%) of oxalic acid, which is commonly recognized as an anti-nutritional compound. Lactobacillus brevis POM4 enhanced by ca. 400% the concentration of γ-amino butyric acid, a non-protein amino acid with various physiological functions. Fermentation of P. oleracea led to a marked increase of α-linalool, a monoterpene compounds with various pharmacological properties. Bioconversion of oleraceins by L. kunkeii B7 is likely responsible for the increased antioxidant activity. The decrease of polyunsaturated fatty acids potentially underlined the synthesis of various derivatives with potential health or nutritional effects. Hence lactic acid fermentation of P. oleracea is a powerful tool to achieve standardized functional foods.
... essential oil is one of the medicinal herbal products, which contains as main components 1,8-cineole and linalool, having utilization in cosmetics and pharmaceuticals as well. Linalool has sedative [6,7] and local anesthetic effects [8]; antimicrobial [9,10], and insecticidal effects [11,12]; whereas the main component 1,8-cineole has antispasmodic [13] and antimicrobial [10] properties. 1,8-Cineole is also present in L. angustifolia and L. hybrida, although in much lower concentrations [14][15][16]. ...
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Combination of various compounds and essential oils for pharmaceutical formulations withdraw attention. In this present study, it was aimed to evaluate the in vitro potential synergistic antibacterial effect of Lavandula latifolia (spike lavender) essential oil with camphor by using the checkerboard method against the human pathogens; Staphylococcus aureus and Listeria monocytogenes. Pharmacopoeia quality L. latifolia essential oil and racemic camphor were analyzed and verified by GC-FID and GC/MS, simultaneously. In vitro antibacterial activity of essential oil and camphor (MIC range: 0.16-20 mg/mL) and standard antimicrobial clarithromycin (MIC range: 0.125-16 μg/mL) were carried out by broth microdilution against S. aureus and L. monocytogenes standard strains, respectively. Resulting antibacterial effects were evaluated for their fractional inhibitory concentrations (FICs) as antagonistic, additive and synergistic effects. The analytical results showed that the major component of essential oil was linalool (45.2%) and 1,8-cineole (25.6%). Antibacterial effects of essential oil were determined as MIC 1.25-5 mg/mL. As a result of the experiments, L. latifolia essential oil-camphor combinations were identified as "synergistic (FIC ≤ 0.5), and additive (0.5 < FIC ≤ 1)" in the respective combinations, suggesting further evaluation for formulations for potential antimicrobial applications in food and pharmaceuticals.
... μg/ml declined animal diaphragm. Also, the oil or its major constituents (linalyl acetate or linalool) in an in-vivo study at a dose ranged from 30.0-2500.0 μg/ml increased the number of stimuli needed to inflame the reflex [30]. The oil declined senses buried numbers. ...
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Lavandulae aetheroleum, the oil, was obtained by vapor condensation from the flower of Lavandula angustifolia Mill. or Lavandula intermedia Loisel (Lamiaceae) plant. Other names of Lavandulae aetheroleum oil are Al birri, common or English lavender. The Lavandula angustifolia Mill. or Lavandula intermedia Loisel plant is spreading in the Mediterranean, southern Europe, Bulgaria, Russia, and USA. The Lavandula angustifolia Mill. or Lavandula intermedia Loisel plant, is an odor shrub with 1-2 m in height. The oil is a clear, colorless, or pale yellow. The gas chromatography studies reported the following percentage of the major chemical constituents in the oil: linalyl acetate (25-46%), linalool (20-45%), terpinen-4-ol (1.2-6.0%), lavendulyl acetate (> 1.0%), 1,8-cineole (1,8-cineol, cineol, cineole, eucalyptol) (< 2.5%), 3-octanone (< 2.5%), camphor (< 1.2%), limonene (< 1.0%), and α-terpineol (< 2.0%). Medicinal applications of the oil include the treatment of restlessness, anxiety, cardiovascular disorders, insomnia, and gastrointestinal disorders, burns, diarrhea, headache, sore throats, and wounds. Pharmacological effects include experimental and clinical pharmacology. Experimental pharmacology includes anesthetic, anticonvulsant, sedative, anti-inflammatory, antimicrobial, antispasmodic, antispasmodic, central nervous system depressant effects. Clinical pharmacology includes anxiolytic, analgesic, and cardiovascular effects. The oil dose by inhalation = 0.06-0.2 ml/ 3 times/day while oil dose internally = 1-4 drops approximately 20-80 mg on a sugar cube per day. In conclusion, Lavandulae aetheroleum oil had an anesthetic, anticonvulsant, sedative, anti-inflammatory, antimicrobial, antispasmodic, antispasmodic, central nervous system depressant, anxiolytic, analgesic, and cardiovascular effects.
... Linalyl acetate is known to have very low toxicity and skin irritation effect, in addition to high calming and spasmolytic properties (Kim and Lee, 2002). Likely, linalool has low toxicity in addition to antiviral and antibacterial properties (Ghelardini, et al., 1999). Therefore, the three Lavandula species in our study could be evaluated as the highest quality because of its linalool and linalyl acetate content. ...
Article
The present investigation was conducted to study the differences in taxonomic characters, essential oil production and composition as well as the genetic relationship of three different Lavandula species that are widely grown in Egypt, wild type L. pubescens Decne., and two cultivated species, L. angustifolia Miller and Lavandula × heterophylla Viv). The essential oil study showed that the maximum volatile oil percent in the fresh leaves was observed in L. pubescens with 0.8%, while the minimum was observed in L. heterophylla (Lavandula × heterophylla Viv; 0.04%). Despite the noticed fact that the three Lavandula species under investigation were evaluated as the highest quality compared to other Lavandula species because of their content of linalool and linalyl acetate, it was obvious that the L. angustifolia volatile oil was distinctive due to containing unique components, α-fenchene and Camphene, which were absent in the other two species. The anatomical analysis revealed that the upper and lower surfaces of the leaves of L. angustifolia have epidermal hairs, which were absent in the other two species. In addition, the presence of capitates peltate glandular trichomes on upper and lower epidermis distinguished the other two species from L. angustifolia species. Results of the band-based approach came out to support the essential oil and anatomical studies by generating a dendrogram with two separate clusters, the first consists of L. pubescens and L. heterophylla in one clade with 79% bootstrap value, and the second consisted of L. angustifolia Miller in a distant clade. Based on these results, it could be concluded that L. angustifolia is distinguishable species that has distinct genetic composition, which could be due to the widespread and diverse exchange of the plant material during cultivation.
... However, they have advised extended research on a large scale for evaluating the effectiveness of essential oils in reducing dental anxiety [15]. Ghelardini et al. demonstarted L. angustifolia oil, linalyl acetate and linalool to retain anesthetic activity both in pre-clinical and clinical experimental set up [23]. Re et al explained action of linalool, through inhibition of acetylcholine release at neuromuscular junction altering ion channel function [24]. ...
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Background: Though local analgesia is used to alleviate pain and render dental procedures comfortable, its administration using injectable mode of delivery itself induces pain. Chemically derived analgesic agents are frequently used to achieve topical analgesia before or during dental procedures. However, few herbal agents are observed to show anesthetic properties. One such agent described in literature but evaluated minimally in medical and dental field is lavender oil. The present in-vivo study was planned to compare and evaluate efficacy of essential oil (lavender oil) against 20% benzocaine gel as topical analgesic agent in order to minimize pain before or during injecting local anesthesia. Materials and Methods: 50 children between 6-14 years, requiring bilateral extraction of maxillary teeth through local infiltration anesthesia were selected in this study. One side was anesthetized with benzocaine gel (20%) followed by local infiltration and other with lavender oil (100%) followed by local infiltration analgesia. The effectivity of these test agents as topical analgesia was evaluated with the help of Visual Analogue Scale (VAS), Wong-Baker Scale (WBS) & Sound Eye Motor Scale (SEM). Results: The mean score of VAS for benzocaine was 0.48±0.79 (p=0.0001) and lavender oil, 0.04±0.20 (p<0.001) respectively. Mean score of WBS for benzocaine was 0.68±0.93 (p=0.0001) and 0.00±0.00 for lavender oil (p<0.001). Mean score of SEM for benzocaine was 3.48±1.26 (p>0.35) and 3.64±1.11 (p>0.05) for lavender oil. Conclusion: Lavender oil showed better efficacy than benzocaine gel to reduce perception of pain during local infiltration anesthesia. It can be effectively used as substitute to chemically derived anesthetic agents for effective topical analgesia.
... Its linalyl acetate component is known as an analgesic while linalool has a sedative effect. 6,7 When used in traditional treatment, lavender oil is used in diuretic, antiepileptic, antirheumatic, and especially nervous system and migraine pains as well as postoperative pain management. 8 Postoperative pain management is an important component of postoperative care. ...
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This was a randomized, placebo-controlled study. The sample consisted of 3 groups of patients: an experimental group, massage application with lavender oil (n = 15); a placebo group, massage application with ultrasound gel (n = 15); and a control group (n = 15). Massage application was performed 3 hours after analgesic application. Pain levels of the patients in the experiment and placebo groups were evaluated with a Verbal Rating Scale (VRS) at the 30th minute and the 3rd hour after the application. Similarly, the pain level of patients in the control group was also evaluated with the VRS at 3 hours after the initial analgesic administration and following the 30th minute and the 3rd hour. Generally, the VRS scores of the 3 groups did not show a significant difference in terms of group and time interaction (P = .221). However, there was a significant difference in VRS scores between the experimental and control groups at the 30th minute after the massage (P = .036). This difference was caused by the lower pain level of the group, which had massage with lavender (2.66 ± .89) compared with the control group (3.80 ± 1.01). According to the study results, while only hand massage application after gynecologic surgery was effective for a short period in decreasing postoperative pain, it was determined that massage application with lavender had a longer effect in decreasing postoperative pain. The results of this study showed that this inexpensive and easy-to-apply method can be safely performed by nurses on postoperative patients and can support pain management of patients in the first hours after gynecologic surgery.
Chapter
Brassinosteroids (BRs) are a group of naturally occurring endogenous steroidal plant growth regulators (PGRs) which are hydroxylated derivatives of a 5α- cholestane ring structure. Both spectroscopy and X-ray based structural elucidation methods have revealed the structure of the first discovered BR, i.e. Brassinolide (BL) as (22R, 23R, 24S) - 2α,3α,22,23-tetrahydroxy-24-methyl-B-homo-7-oxa-5α- cholestan-6-one. Generally, the natural BRs are hydroxylated at the C-2, C-3, C-22 and C-23 positions. The most biologically active BRs differ from other BRs solely on the basis of either a 6-oxo functional group or a lactone structure at one of its rings. Presently, more than 60 types of BRs have been identified and isolated from a diverse range of plants. Recently, BRs have emerged as important PGRs that are a pre-requisite for growth and various developmental processes along with other PGRs namely auxins, gibberellins, cytokinins, ethylene and abscisic acid. Further, these BRs also provide protection to the plants under both biotic and abiotic stresses. Therefore, the present chapter highlights the structure, occurrence, mode of action, biosynthetic pathway, plant stress ameliorating properties of BRs and their interactions with other PGRs.
Chapter
An essential oil is an extraction of the volatile plant molecules that confer distinctive colors, flavors, and aromas to different plant species (aka the “volatiome” of a plant). This diverse group of molecules are produced by all plants and are considered secondary metabolites. While primary metabolites are those substances created to meet the basic survival needs of the plant, secondary metabolites provide adaptive and protective mechanisms for plants, while also regulating the plant’s development and metabolism, and are classified by nitrogen content. The non-nitrogen containing secondary metabolites include cannabinoids, terpenes, flavonoids, lignans, saponins, and fatty acids (Wink 2010). The volatile molecules of particular interest in cannabis for clinical and therapeutic use are terpenes and flavonoids. These molecules provide each variety of cannabis its distinctive color, aroma, and flavor profile, while potentially conferring therapeutic benefits in their own rights.
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A convenient and easy-moving, modified, headspace solid-phase microextraction (HS-SPME) device was developed for monitoring a living plant’s volatile organic compounds (VOCs). It consisted of a polyethylene terephthalate (PET) bottle as a sampling chamber, and certain variables were considered when using the HS-SPME device, including the material used and the fiber position, the direction of the airstream, and the distance between the sample and the fan. The results from varying those factors, generated by the orthogonal array design (OAD) method, were used to optimize the modified HS-SPME conditions. Based on the current literature regarding extracting fragrances by SPME, we selected polydimethylsiloxane/divinylbenzene (PDMS/DVB) and polydimethylsiloxane (PDMS) as the fiber materials. Using the OAD method, PDMS/DVB was found to be the better fiber material when it was parallel to the fan, and also when the airstream provided positive pressure to the sample with the fan near the sample. The device was used to sample biogenic volatile compounds emitted from fresh Nymphaea caerulea (water lily) flowers, followed by gas chromatography-mass spectrometry (GC-MS) analysis. For the method validation, under the optimum conditions, the calculated detection limit value of the model compound (butyl decanoate) was 0.14 ng on column, which was equal to 1.41 ppm for the injection. The relative standard deviations of the intra-day and inter-day precisions were 1.21% and 3.05%. Thirty-three compounds were separated and identified. The main components in the vapor phase of N. caerulea were benzyl acetate (10.4%), pentadecane (15.5%), 6,9-heptadecadiene (40.1%), and 8-heptadecene (15.3%).
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Introduction Some studies have investigated the effect of Lavender on pain and the healing of wounds. The aim of this systematic review was to investigate the effect of Lavender on pain and wound healing of episiotomy. Methods The Cochrane Library, MEDLINE (PubMed), Scopus, and Web of Science (all databases from inception until February 2020) were searched. Data were extracted from eligible studies by two review authors individually. Our inclusion criteria were full-text interventional studies published in English or any other languages. All data were analyzed using Review Manager 5.3. The protocol of this systematic review was registered in PROSPERO with the reference number CRD42020140623. Results Our search found six trials involving 415 participants. The use of Lavender could significantly reduce pain in women with episiotomy (95 % CI: -1.06 – -0.32). The use of Lavender has significantly improved the healing of episiotomy compared to the placebo (95 % CI: -2.13 – -1.34). In all studies, pain and healing of episiotomy were evaluated with Visual Analog Scale (VAS) and Redness, Edema, Ecchymosis, Discharge, Approximation (REEDA) scale respectively. Conclusion This review showed that the use of Lavender (in any form) in postpartum has a significant effect on pain relief and healing of episiotomy wound. All six studies that were included in this systematic review were from developing countries. A high level of heterogeneity was observed in the effect of Lavender on pain but not the healing of the episiotomy. Therefore, the results should be considered with caution. Using Lavender may be considered for wound healing of episiotomy.
Article
Background : Many of plant-derived compounds inhibiting nerve conduction enhance glutamatergic spontaneous excitatory transmission by activating transient receptor potential (TRP) channels in spinal substantia gelatinosa (SG) neurons that play a crucial role in regulating nociceptive transmission. Although (±)-linalool and its isomer geraniol having antinociceptive effects inhibit nerve conduction, it has not been examined yet how they affect excitatory transmission in SG neurons. We examined the effects of the compounds on action potential-independent spontaneous excitatory transmission with a focus on an involvement of TRP channels. Methods : The whole-cell patch-clamp technique was applied to SG neurons in adult rat spinal cord slices. Results : (±)-Linalool increased the frequency of spontaneous excitatory postsynaptic current (sEPSC) with a small increase in its amplitude. The (±)-linalool activity was sensitive to TRP vanilloid-1 (TRPV1) antagonist capsazepine and TRP ankyrin-1 (TRPA1) antagonist HC-030031 while resistant to BCTC that is antagonist for cloned TRPV1 and TRP melastatin-8 (TRPM8) channels and for TRPM8 channels in the SG, indicating TRPV1 and TRPA1 activation. In 73% of the neurons tested, (±)-linalool produced an outward current at -70 mV. In SG neurons sensitive to (±)-linalool, geraniol produced a quantitatively similar effect to (±)-linalool. Geraniol-induced sEPSC frequency increase was sensitive to BCTC but resistant to capsazepine and HC-030031, indicating TRPM8 activation. Outward currents produced by (±)-linalool and geraniol were unaffected by all of the TRP antagonists. Conclusion : In SG neurons, (±)-linalool and geraniol presynaptically enhanced spontaneous excitatory transmission by activating different types of TRP channel while hyperpolarizing membranes in a manner independent of TRP channels. Such a TRP channel modulation and hyperpolarization could contribute to the antinociceptive effects of (±)-linalool and geraniol.
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Background: Dysmenorrhea is a common problem in women of reproductive age and despite the current treatments, it still remains a common problem in women's health. This study was done to determine the effect of aromatherapy on pain severity in primary dysmenorrhea. Materials and Methods: This randomized clinical trial was done on 108 students with primary dysmenorrhea with pain score of 2 and 3 based on the multidimensional spoken criteria. After random allocation, the participants received massage with almond oil, massage alone, and massage with a mixture of lavender and peppermint essential oil a week before menstrual period until the presence of pain in two continuous cycles. During cycles zero, one, and two, the participants recorded the highest level of pain during the first, second, and third days according to the visual analogue scale. Data were analyzed using SPSS software. Results: There was a significant difference in the total of the most pain in days 1, 2, and 3 among the groups(p=0.038). A reduction was observed in massage and aromatherapy groups(p=0.014). There were significant differences in within group comparisons (p=0.002) for zero and first cycles(p=0.016) and first and second cycles(p=0.002). Conclusion: Aromatherapy reduces menstrual pain and considering the prevalence of dysmenorrheal, the low price, and harmless nature of this essence, its application in relieving menstrual cramping and pain is recommended.
Article
In nature, plants are constantly challenged by an array of drought episodes, which critically affect the distribution of the plants. The drought episodes might occur recurrently, so the plants endure drought by adjusting and shifting their metabolisms. The impacts of subjecting plants to drought stress have been widely investigated, but reports on how reiterated drought stress affects the plants are limited. The present study was designed to investigate the response of lavender, a reputed medicinal and aromatic plant, against single drought, recovery and reiterated drought stress at greenhouse conditions. In this regard, the experimental design was based on three cycles of 11 days of drought by withholding water, followed by subsequent periods of 6 days of recovery, and then double-stressed and single-stressed periods. As expected, the present findings revealed that single stress decreased the fresh and dry weights of the leaf, stem and root. Reiterated drought stress caused critical reductions in the fresh weight of the leaf, stem and root, while the dry weight of stem and root were not significantly affected. Of the estimated traits, only the dry weight of leaf increased with reiterated drought stress. The mineral status of the leaves was adversely affected with single stress, but the effects of recovery and reiterated stress were not in accordance with the improvement in water contents of the leaf and soil. Regarding essential oil compounds, eucalyptol, camphor and endo-borneol were predominant. Single and reiterated drought stress increased camphor percentage, while recovery and full irrigation decreased the percentage. Endo-borneol was decreased under single stress, but reiterated stress increased the percentage of the compound. Considering the phenolic acids, stressed and non-stressed groups were well discriminated and hence, phenolic acids might be useful as good indicators of the stress response in lavender.
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P. racemosa (Mill) J.W. Moore, belongs to the genus Pimenta of the Mirtaceae family, is native to the Lesser Antilles, Puerto Rico and Cuba, being widely cultivated in the American Tropics. The essential oil extracted from the leaves has disinfectant and astringent properties and does not give rise to allergic reactions on people. In this work the pharmacognostic and chemical study of the species that grew in the city of Guayaquil, Guayas province (Ecuador), was carried out, on which it was possible to establish the macro and micromorphological characteristics of the species, that were researched for the first time, The physical-chemical quality parameters of the leaves of the species were also determined, aspects that were previously reported. A comparative study was carried out on the extraction of essential oil from the leaves using the hydrodistillation method and the microwave assisted hydrodistillation (MWHD) method, for which a yield of 1,3% was obtained, which was higher than that of which was reported in the bibliography. The distillation time to reach this yield was lower when MWHD was used and some differences were observed in the physicochemical characteristics of the essential oil. The chemical composition of the essential oil determined by the use of the GC-MS coupled system made it possible to identify methyl eugenol and estragol as the major components, followed by β-pinene, 1,8-cineole, linalool and limonene, which correspond to the information reported for P. racemosa var. racemosa, although modifications in the qualitative-quantitative composition were evident, depending on the extraction method.
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The antimutagenic effects of various tea extracts prepared from nonfermented tea (green tea), semifermented tea (oolong tea and pouchong tea), and fermented tea (black tea) were investigated by Salmonella/microsome assay. No mutagenicity or toxicity in Salmonella typhimurium TA98 and TA100 was observed with any tea extract. The tea extracts markedly inhibited the mutagenicity of 2-amino-3-methylimidazo(4,5-f)quinoline, 3-amino-1,4-dimethyl-5H-pyridol(4,3-b)indole,2-amino-6-methyldipyrido(l,2-a:3′,2′-d)imidazole, benzo[a]pyrene, and aflatoxin B1 toward S. typhimurium TA98 and TA100 in the presence of S9 mixture, especially those of oolong and pouchong teas inhibited over 90% mutagenicity of these five mutagens at the dosage of 1 mg per plate. Among four tea extracts, black tea exhibited the weakest inhibitory effect on mutagenicity of these five mutagens. The mutagenicity of 4-nitroquinoline-N-oxide, a direct mutagen, was not inhibited by black and oolong tea extracts to S. typhimurium TA98 in the absence of S9 mixture but was increased by the tea extracts at the dose of 1 mg per plate to S. typhimurium TA100. As the antimutagenic effect of semifermented tea was stronger than nonfermented and fermented teas, some antimutagenic substances might be formed during manufacturing processes of tea.
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The antimicrobial and toxicological properties of the Australian essential oil, lemon myrtle, (Backhousia citriodora) were investigated. Lemon myrtle oil was shown to possess significant antimicrobial activity against the organisms Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, methicillin-resistant S. aureus (MRSA), Aspergillus niger, Klebsiella pneumoniae and Propionibacterium acnes comparable to its major component-citral. An in vitro toxicological study based on the MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) cytotoxicity assay was performed. In vitro cytotoxicity testing indicated that both lemon myrtle oil and citral had a very toxic effect against human cell lines: HepG2 (a hepatocarcinoma-derived cell line); F1-73 (a fibroblast cell line derived from normal skin) and primary cell cultures of human skin fibroblasts. Cytotoxicity IC50 (50% inhibitory concentration) values ranged from 0.008 to 0.014% (w/v) at 4 h to 0.003-0.012% (w/v) at 24 h of exposure. The no-observed-adverse-effect level (NOAEL) for lemon myrtle oil was calculated as 0.5 mg/l at 24 h exposure and the RfD (reference dose) was determined as 0.01 mg/l. A product containing 1% lemon myrtle oil was found to be low in toxicity and could potentially be used in the formulation of topical antimicrobial products.
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Oral and intra-peritoneal acute toxicity and the sub-chronic intra-peritoneal toxicity of the essential oil of Ocimum gratissimum Linn, Lamiaceae (Ocimum oil), was investigated. The acute toxicity test involved the oral and intra-peritoneal administration of graded doses of Ocimum oil prepared as a 4% v/v emulsion to 2 groups each of 30 rats and mice. LD50 and LD100 were determined for both routes and species. In the sub-chronic toxicity study, 25 male Sprague-Dawley rats were randomized into 4 test groups (treated with three graded sub-lethal doses of Ocimum oil prepared as a 4% v/v emulsion) and a control. Organs and blood samples were taken for analyses after a 30 day treatment period. A dose-dependent sedative effect of Ocimum oil was observed during the acute toxicity study in mice and rats and in the sub-chronic test in rats. Evidence of treatment, route, and dose-dependent toxicity were detected in both studies. Changes in weight of the testes, hearts, kidneys, intestines and lungs of the rats were statistically insignificant (ANOVA P < 0.05). Data analyses of blood biochemical, haematological and histopathological findings showed significant differences between control and treated groups and revealed that Ocimum oil is capable of invoking an inflammatory response that transits from acute to chronic on persistent administration. While the study revealed that Ocimum oil might be better tolerated when administered orally for systemic delivery, the oil has toxic potentialities that should not be overlooked.
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The reducing activity on the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, z.rad;OH radical scavenging potential, in vitro inhibition of lipid peroxidation and modulation of mutagenicity induced by ter-butyl hydroperoxide (TBH) in Escherichia coli were sequentially screened in 45 species of plants used with medicinal purposes in Cuba, in a search for antioxidant agents which protect DNA against oxidative stress.Five species, e.g. Tamarindus indica L., Lippia alba L., Pimenta dioica (L.) Merr, Rheedia aristata Griseb. and Curcuma longa L. displayed IC(50)<30 micro g/ml in the DPPH radical reduction assay and IC(50)<32 micro g/ml in lipid peroxidation inhibition testing. Pimenta dioica and Curcuma longa L. showed also a 20% inhibition of the in vitro induced z.rad;OH attack to deoxyglucose. Further antimutagenesis assay in Escherichia coli IC 188 evidenced that only Pimenta dioica prevents DNA damage by TBH to the test bacteria. A role of antioxidant enzymes is presumed in this case, as judged by a different response in the isogenic Escherichia coli IC 203 deficient in catalase and alkyl hydroperoxide reductase and the discrete inhibition of oxidative mutagenesis also observed when pre-treatment of the extract was assayed. Eugenol, the main constituent of the essential oil of Pimenta dioica, also inhibited oxidative mutagenesis by TBH in Escherichia coli, at concentrations ranging from 150 to 400 micro g/plate.
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There is an increasing awareness at several levels of the need to develop pharmacovigilance practices for herbal medicines. The current model of pharmacovigilance and its associated tools have been developed in relation to synthetic drugs, and applying these methods to monitoring the safety of herbal medicines presents unique challenges in addition to those described for conventional medicines. Several problems relate to the ways in which herbal medicines are named, perceived, sourced, and utilised. Other important challenges arise from the current regulatory framework for herbal medicines in the UK. In the UK at present, the Committee on Safety of Medicines/Medicines and Healthcare products Regulatory Agency’s (CSM/MHRA) ‘yellow card’ scheme for adverse drug reaction (ADR) reporting is the main method of monitoring the safety of herbal medicines. Despite recent initiatives to stimulate reporting of suspected ADRs associated with herbal medicines, such as extending the scheme to unlicensed herbal products, and including community pharmacists as recognised reporters, numbers of herbal ADR reports received by the CSM/MHRA remain relatively low. Under-reporting, an inevitable and important limitation of spontaneous reporting schemes, is likely to be significant for herbal medicines, since users typically do not seek professional advice about their use of such products, or report if they experience adverse effects. The herbal sector in the UK has initiated various spontaneous reporting schemes, based on the yellow card scheme, but targeted mainly at herbal-medicine practitioners. It is important that these schemes have a link with the CSM/MHRA so that potential signals are not missed. Several other tools used in pharmacovigilance of conventional medicines, such as prescription-event monitoring, and the use of computerised health-record databases, currently are of no use for evaluating the safety of herbal and other non-prescription medicines. Proposed European Union legislation for traditional herbal medicinal products will require manufacturers of products registered under new national schemes to comply with regulatory provisions on pharmacovigilance. In the longer term, other improvements in safety monitoring of herbal medicines may include modifications to existing methodology, patient reporting and greater consideration of pharmacogenetics and pharmacogenomics in optimising the safety of herbal medicines.
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Sixteen hydroalcoholic extracts (methanol-water, 50:50 v/v), obtained by plants selected on the basis of medicinal folklore, were studied for their antispasmodic activity using the guinea-pig ileum. Among these, only four plants (Angelica arcangelica roots, Eucalyptus globulus leaves, Aesculus hippocastanum skinned seeds, Lavandula angustifolia flowering tops) reduced significantly (p < 0.05-0.01) the spontaneous contractions of the circular smooth muscle at concentrations ranging from 100 to 800 μg/ml (IC50: 265-738 μg/ml) and inhibited acetylcholine and barium chloride-induced contractions of the longitudinal smooth muscle at concentrations of 50-800 μg/ml (IC50: 137-598). Angelica archangelica was found as the most active plant (IC50: 146-265 μg/ml).
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The essential oils (EOs) obtained from the oregano plants Origanum vulgare subsp. hirtum, Coridothymus capitatus, and Satureja thymbra were examined by a combination of GC and GC−MS and found to be rich in carvacrol, thymol, γ-terpinene, and p-cymene. These EOs and their main constituents, carvacrol and thymol, were tested for insecticidal and genotoxic activities on Drosophila. The EO of S. thymbra was found to be the most effective as an insecticide, while carvacrol was found to be more toxic than thymol. The toxicities of carvacrol and thymol do not correspond to their participation in the EOs, and mixtures of these two phenols in levels resembling their content in the three oils showed that the toxicity of carvacrol was reduced in the presence of thymol, thus suggesting antagonistic phenomena. The somatic mutation and recombination test on Drosophila revealed that, among the five compounds studied, only thymol exhibits genotoxic activity. Keywords: Oregano; Origanum vulgare; Coridothymus capitatus; Satureja thymbra; essential oils; carvacrol; thymol; insecticides; genotoxicity; Drosophila melanogaster
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The spasmolytic activity of Achillea ageratum L. essential oil in isolated rat duodenum has been in estigated. The essential oil was found to present a marked spasmolytic activity against acetylcholine and BaCl2 via a non-competitive type of antagonism.
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The antimicrobial activity of essential oil of Hyssopus officinalis L. var decumbens (Jordan & Fourr.) Briq. from France (Banon) and Hyssopus officinalis L. from Italy (Piedmont) was studied taking account of their chemical composition determined by GC and GC–MS. Pinocamphone and isopinocamphone are present in H. officinalis (4.4% and 43.3%, respectively), according to the ISO 9841 Standard (1991 E) but they are lacking in var. decumbens, where linalol (51.7%), 1,8-cineole (12.3%) and limonene (5.1%) instead are predominant. The disc diffusion tests carried out on Gram-positive (Staphylococcus aureus and Enterococcus spp.) and Gram-negative bacteria (Klebsiella oxytoca, Escherichia coli, Proteus mirabilis, Pseudomonas spp. and two strains of Salmonella spp.) showed an antimicrobial activity generally negligible for H. officinalis, but broader, and in a few cases more evident (Enterococcus spp. and E. coli), for var. decumbens. All yeasts (seven strains of Candida albicans, C. krusei and C. tropicalis) were strongly inhibited by both species. In liquid medium the MIC of H. officialis was always >1.2% v/v for bacteria and between 0.6 and 1.2% v/v for yeasts, while the MIC of var. decumbens was between 0.15 and 0.6% v/v for the Gram-positive bacteria, 0.3 and 1.2% v/v for the Gram-negative bacteria and 0.15 and 0.3% v/v for the yeasts. The effect of var. decumbens was generally bactericidal. Linalol, and in a lesser way, 1,8-cineole, may contribute to the greater antimicrobial activity of var. decumbens in comparison with H. officinalis, while limonene may be responsible for the antimycotic action observed in both oils, as suggested by results of the disc diffusion tests carried out on the pure reference substances. © 1998 John Wiley & Sons, Ltd.
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Dried pomegranate peels were powdered and extracted in a Soxhlet extractor with ethyl acetate (EtOAc), acetone, methanol and water for 4 h each. The dried extracts were used to determine their antioxidant capacity by the formation of phosphomolybdenum complex and antimutagenicity against the mutagenicity of sodium azide by the Ames test. All the peel extracts exhibited marked antioxidant capacity, but the water extract was the lowest. The order of antioxidant capacity varied because of differential responses at four concentrations (25, 50, 75 and 100 μg/ml) in each solvent. All the extracts decreased sodium azide mutagènicity in Salmonella typhimurium strains (TA100 and TA1535), either weakly or strongly. At 2500 μg/plate all the extracts showed strong antimutagenicity. The antimutagenicity of the water extract was followed by acetone, EtOAc and methanol extracts. The overall results showed that the pomegranate peel extracts have both antioxidant and antimutagenic properties and may be exploited as biopreservatives in food applications and neutraceuticals.
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Escherichia coli strain WP2 and its repair-deficient derivatives are suitable strains for mutagen screening. In these strains, agents which cause base substitution mutations can be shown to increase the frequency of Trp+ revertants. In addition, agents causing many types of DNA damage can be detected through increased killing of the repair deficient derivatives. Four ways of performing tests are described: (a) Spot tests in which a small amount of the agent under test is placed directly on a selective agar plate. Trp+ revertants are counted and increased sensitivity of repair-deficient strains determined from the size of the zone of inhibition of cell growth. (b) Treat and plate tests, where a strain is treated with the agent under test and subsequently plated to determine survival or frequency of Trp+ revertants. (c) A simplified fluctuation test which shows exceptional sensitivity in measuring mutation with low levels of mutagens. (d) Use of a liver microsomal fraction in conjunction with treat and plate tests to detect metabolically activated mutagens. The merits and defects of these systems are discussed. Common pitfalls in evaluating tests and procedures for avoiding them are described.
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Genotoxic properties of essential oils from Anthemis nobilis L., Artemisia dracunculus L., Salvia officinalis L., Salvia sclarea L., Satureja hortensis L., Satureja montana L., Thymus capitatus L., Thymus citriodorus Schreb., Thymus vulgaris L., Citrus bergamia Risso, were studied with Bacillus subtilis rec-assay and Salmonella/microsome reversion assay. The essential oil of Artemisia dracunculus L. "Piemontese" turned out to be active in the rec-assay but not in the Salmonella test. DNA-damaging activity was demonstrated to be due to the estragol component of the oil. Advantages of the combined use of these two short-term microbial assays in genotoxic studies are discussed.
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The present study examines postoperative pain experience following 243 gingivectomies in Norwegian patients using possible combinations of 3 local anaesthetics (lidocaine-adrenalin, prilocaine-felypressin or mepivacaine) and 3 periodontal dressings (Coe-pak, Wondrpak or Nobetec). When Coe-pak was used, the mean pain score was higher (P less than 0.05) in the group treated with lidocaine-adrenalin 4 to 6 h after gingivectomy than the groups treated with prilocaine-felypressin or mepivacaine. There was no significant difference between the groups treated with prilocaine-felypressin or mepivacaine. When Wondrpak or Nobetec were used, there was no significant difference between any of the local anaesthetics used. The present finding shows that the local anaesthetic combination of lidocaine-adrenalin (1:80,000) gives rise to a higher mean postoperative pain experience after gingivectomy than prilocaine-felypressin or mepivacaine. However, the relative difference in pain experience seen after gingivectomy when using the present local anaesthetic agents is masked when using an eugenol-containing periodontal dressing. Thus, the higher pain experience reported after lidocaine-adrenalin may only be clinically important when using periodontal dressings without local anaesthetic components such as eugenol.
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Tea-tree oil (an essential oil of the Australian native tree Melaleuca alternifolia) has long been regarded as a useful topical antiseptic agent in Australia and has been shown to have a variety of antimicrobial activities; however, only anecdotal evidence exists for its efficacy in the treatment of various skin conditions. We have performed a single-blind, randomised clinical trial on 124 patients to evaluate the efficacy and skin tolerance of 5% tea-tree oil gel in the treatment of mild to moderate acne when compared with 5% benzoyl peroxide lotion. The results of this study showed that both 5% tea-tree oil and 5% benzoyl peroxide had a significant effect in ameliorating the patients' acne by reducing the number of inflamed and non-inflamed lesions (open and closed comedones), although the onset of action in the case of tea-tree oil was slower. Encouragingly, fewer side effects were experienced by patients treated with tea-tree oil.
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The research group at Research Triangle Institute (RTI) has had many years of experience in the isolation and structural elucidation of antitumor agents. Several of us attended the First International Conference on Antimutagenesis and Anticarcinogenesis Mechanisms (University of Kansas, 1985). Stimulated by papers presented at this meeting and the subsequent book (7), we became interested in the question whether secondary plant metabolites have a role in antimutagenesis mechanisms. There was already considerable evidence that higher plants contain a variety of preformed secondary metabolites which represent a structurally diverse array of antimutagenic and mutagenic compounds (3,5). Since we had on hand thousands of plant extracts from previous antitumor studies and had extensive experience in bioassay-directed isolation of naturally-occurring compounds, along with the availability of an active microbiology laboratory, we believed that we might be able to make a contribution to this interesting field.
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Two different preparations of the rat phrenic nerve-hemidiaphragm (whole nerve-muscle preparation, end-plate preparation) were used for studying synthesis and release of radioactive acetylcholine in the absence and presence of cholinesterase inhibitors. When the whole nerve-muscle preparation (110–180 mg) was incubated with [3H]choline, only small amounts of radioactive acetylcholine were synthesized within the tissue. Electrical nerve stimulation of the whole nerve-muscle preparation produced no increase in tritium outflow. Incubation of the end-plate preparation (16–29 mg) which was obtained after removal of most of the muscle mass led to the formation of large amounts of [3H]acetylcholine. Synthesis depended on nerve activity and increased 13-fold during a high loading stimulation (50 Hz), as compared to the synthesis at rest. In a denervated end-plate preparation the formation of [3H]acetylcholine was reduced to 4% of the control preparation. Electrical nerve stimulation of the end-plate preparation produced a release of tritium that could be attributed entirely to the release of [3H]acetylcholine. The stimulated tritium efflux was completely suppressed in a calcium-free medium or in the presence of tetrodotoxin (300 nM). Release could even be detected during a short train of 50 pulses (5 Hz) with a fractional release of about 0.04% of the [3H]acetylcholine tissue content per pulse. It is concluded that the large muscle mass interferes with nerve labelling by a reduction of the [3H]choline supply to the nerve terminals when the whole nerve-muscle preparation is used. Removal of most of the muscle fibres reduces the possibility for [3H]choline to be captured by them and then more radioactive choline can enter the end-plate region. From this end-plate preparation a calcium-dependent release of radioactive transmitter can be measured in the absence of cholinesterase inhibitors.
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2-Nitrofluorene (NF), a model substance for nitrated polycyclic aromatic hydrocarbons, is present in exhaust from diesel- and petrol-driven vehicles, in exhaust from kerosene heaters, and in urban air and river sediments. Therefore the possible consequences of human exposure are important to elucidate. In the present study the initiating and promoting activity of NF was studied in a liver model for chemical carcinogenesis in the rat. Furthermore, the in vivo metabolism and formation of genotoxic metabolites of NF were investigated. NF was found to be a moderate initiator and a weak promoter when compared to diethylnitrosamine (DEN) and 2-acetylamino-fluorene (AAF) respectively, both of which are potent carcinogens. Animals given NF excreted more urinary mutagenicity when compared to animals given AAF or DEN.
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Lemon oil contains furocoumarin derivatives and is known to cause phototoxicity. In this study, lemon oil was fractionated, and its phototoxic activity was measured by means of a biological assay. The substances producing phototoxicity were identified by high-performance liquid chromatography as being oxypeucedanin and bergapten. The phototoxic potency of oxypeucedanin was only one-quarter of that of bergapten. However, the amounts of these two phototoxic compounds present in lemon oils produced in different regions of the world varied by a factor of more than 20 (bergapten, 4-87 ppm; oxypeucedanin, 26-728 ppm), and their ratio was not constant. The two compounds accounted for essentially all of the phototoxic activity of all lemon-oil samples. Among various other citrus-essential oils investigated, lime oil and bitter-orange oil also contained large amounts of oxypeucedanin. Oxypeucedanin was found to elicit photopigmentation on colored-guinea-pig skin without preceding visible erythema.
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The nitrated polycyclic aromatic hydrocarbons constitute a group of chemicals of environmental concern which display a broad spectrum of mutagenic, genotoxic and carcinogenic properties. Some members of the group are the most potent direct-acting bacterial mutagens while others exhibit low levels of potencies which require metabolic activation mixtures. Bacterial mutagenicity is dependent upon reduction of the nitro function. In mammalian cell systems the genetic and genotoxic effects of these nitrated chemicals include the induction of unscheduled DNA synthesis, sister-chromatid exchanges, chromosomal aberrations, gene mutations and cell transformation. The qualitative as well as quantitative expression of these effects is dependent upon the species and tissue of origin as well as culture history of the cell which in turn determine their enzymic capabilities and the conversion of these nitroarenes to ultimate mutagens and genotoxicants. In eukaryotic cells the following bioactivation pathways have been recognized: (a) reduction of the nitro moiety, (b) ring oxidation (the nature of which is influenced by the nitro function) followed by reduction of the nitro group, and (c) ring oxidation without concomitant reduction of the nitro moiety.
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In addition to the spasmolytic activity of ORIGANUM COMPACTUM, the antagonistic effect of the main components thymol and carvacrol is investigated on the isolated guinea-pig ileum, induced by carbachol, histamine, 1,1-dimethyl-4-phenylpiperazinium iodide and BaCl 2 . The l-noradrenaline contractions on the rat vas deferens are also reduced by both of phenols and the Origanum macerate. pD′ 2 values and relative potency to papaverine illustrate the affinity of the isomers. It is concluded that thymol and carvacrol act as non-competitive antagonists and are not significantly different from each other.
Article
The compound-action potential (cAP) of the nerve evoked at 1 Hz was reversibly inhibited and the threshold for nerve stimulation increased between 0.065 and 0.97 mM eugenol. The inhibition showed a sigmoid log10 dose-response relationship. With 2.44 mM or higher concentrations the block became irreversible. The inhibition was enhanced during stimulation at 100 Hz in 5 s with 0.487 mM or higher concentrations. The muscle tetanic tension also showed this high frequency inhibition (HFI). After 40-min exposure to 0.65 mM eugenol, the twitch contractions were unaffected. The indirectly induced tetanic tension was inhibited to 16.6 per cent of control in the initial and to 0.5 per cent in the terminal phase of a 5-s period of 100-Hz stimulation, whereas the directly-induced tetanic tension was inhibited to 38.0 and 13.6 per cent, respectively. Thus, eugenol had affected the neuromuscular transmission during tetanic stimulation in addition to its effect on the directly-stimulated preparation. Intracellular recordings of the end-plate potential (EPP) and miniature end-plate potential (MEPP) indicated both a pre- and a post-synaptic mechanism of action for eugenol. Experiments with eugenol plus d-tubocurarine showed a synergistic effect between these two drugs, suggesting a curare-like effect by eugenol. The resting membrane potential of the muscle was unaffected by eugenol. The following findings suggest that eugenol is a membrane-stabilizing (local anaesthetic) drug at low concentrations: reversible cAP inhibition, increased threshold, high-frequency inhibition, and unresponsiveness of the resting membrane potential of the muscle to the drug.
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The antispasmodic activity of 2.5 and 10.0 ml/l of alcoholic extracts of Melissa officinalis, Rosmarinus officinalis, Mentha piperita, Matricaria chamomilla, Foeniculum vulgare, Carum carvi and Citrus aurantium prepared from 1 part of the plant and 3.5 parts of ethanol (31 % w/w) was tested employing the guinea pig ileum and using acetylcholine and histamine as spasmogens. Most of the extracts shifted the dose response curves of acetylcholine and histamine to the right in a dose dependent manner. Extracts from Carum carvi, Mentha piperita, Citrus aurantium and Matricaria chamomilla showed a significant rise of the DE50 of cetylcholine-induced contractions and a significant decrease of the maximal possible contractility. In histamine-induced contractions, all plant extracts except Extractum Melissae exhibited a significant increase of the DE50, and all extracts used here decreased the maximal possible contractility produced by histamine. The alcoholic extract of Mentha piperita was most effective when tested with acetylcholine and the extract of Citrus auran-tium was most active when tested with histamine. Melissa officinalis did not show significant antispasmodic activity. When the antispasmodic activities of the most effective plant extracts were compared with the activity of atropine, it was evident that their effects were less than that of the usual therapeutic dosage of atropine in man. The most pronounced effects with 10 ml/l Extractum Citrus aurantii and 10 ml/l Extractum Menthae piperitae correspond to the effect of 0.07 resp. 0.13 mg atropine.
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Commercial preparations of essences of sage, hyssop, thuja, and cedar have caused human intoxication in eight cases, from which tonico-clonic convulsions were the major symptom. The experimental study of the toxic properties of commercialized essential oils of sage and hyssop has revealed that their convulsant action was of central nervous system origin in unanesthetized rats, as proven by electrocortical records. The toxicity of the hyssop oil seems to be more powerful than that of sage, since the dose limit from which the cortical events are only subclinical is 0.08 g/kg for hyssop oil and 0.3 g/kg for sage oil. Above 0.13 g/kg for hyssop oil and 0.50 g/kg for sage oil, the convulsions appeared and became lethal above 1.25 g/kg with hyssop oil and 3.2 g/kg with sage oil. The daily repeated injection of subclinical doses revealed the cumulative toxic effect of hyssop oil, since the same low dose induced electrocortical clonic seizures. The toxicity of each oil appeared to be related to the presence of terpenic ketones, camphor in sage commercial oil, camphor and thujone in sage Dalmatian oil, thujone in thuja and cedar oils, and pinocamphone in hyssop oil. The convulsant properties of camphor are well known. The neurotoxicity of thujone and pinocamphone is demonstrated in rats for the first time.
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Sixty-four flavonoids were tested for their antimutagenic potencies with respect to IQ in Salmonella typhimurium TA98 and in part also towards MeIQ, MeIQx, Trp-P-2, and Glu-P-1 and in S. typhimurium TA100. Antimutagenic potencies were quantified by the inhibitory dose for 50% reduction of mutagenic activity (ID50). A carbonyl function at C-4 of the flavane nucleus seems to be essential for antimutagenicity: two flavanols and four anthocyanidines were inactive. Again, five isoflavons, except biochanin A, were inactive. Within the other groups of 21 flavones, 16 flavonols and 16 flavanones the parent compounds flavone, flavonol, and flavanone possessed the highest antimutagenic potencies (ID50: 4.1, 2.5, 5.5 nmoles). Increasing polarity by introduction of hydroxyl functions reduced antimutagenic potency. Reducing polarity of hydroxy flavonoids by methyl etherification, however, increased antimutagenic potency again. 6-Hydroxy- and 2'-hydroxy substituted flavonoids were considerably less potent antimutagens. Of 11 flavonoid glycosides tested all compounds except apigenin- and luteolin-7-glucoside (ID50:74, 115 nmoles) were inactive or only weakly antimutagenic. Rings C and A of the nucleus were not essential for antimutagenicity: chalcone and three derivatives were nearly as active as comparable flavones while antimutagenicity of benzylidenacetone was considerably reduced (ID50: 95 nmoles). Cinnamylaldehyde and cinnamoates, however, were inactive. A planar structure in the vicinity of the carbonyl group may also be important for antimutagenicity. Flavanones were less potent antimutagens than the corresponding flavones, but dihydrochalcones and 14 structurally related saturated aromatic carbonyl compounds were inactive. Fisetin and 6-hydroxyflavone were competitive inhibitors, but luteolin was a mixed type inhibitor. The inhibition mechanisms of flavone, kaempferol, morin, flavanone, and 2'-hydroxyflavanone were concentration dependent, being competitive at low concentrations and mixed or non-competitive (2'-hydroxyflavanone) at concentrations about the ID50 value. No fundamental differences between the two tester strains and no clear influence of mutagen structure on antimutagenic potency could be detected.
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Cocaine was the first drug to be used as a local anaesthetic. It was introduced into medicine in 1884 by Koller. Other drugs soon followed, for example, ethyl chloride spray, tropocaine, eugenol (oil of cloves) and Nupercaine. A wide range of uses for local anaesthetics soon developed and the term 'regional anaesthesia' was first used by Cushing in 1901 to describe pain relief by nerve blockade. Local anaesthetic drugs are water soluble salts of lipid soluble alkaloids. Each molecule is composed of an aromatic portion, intermediate chain and an amide portion. The portions are joined by either amide or ester linkages. Ester-linked drugs are hydrolysed in the plasma by plasma cholinesterase and their half-life varies from one to eight minutes. Amide-linked drugs are degraded by oxidative dealkylation in the liver. The half-life of these drugs varies from 1.5 to more than three hours. The addition of a vasoconstrictor, such as adrenaline, will prolong the duration of action of both the amide- and ester-linked drugs. Degradation of the amide-linked drugs depends on factors such as hepatic blood flow and liver conditions, such as cirrhosis, and congestive cardiac failure. Anaphylactic reactions are more common with ester-linked drugs than amide-linked drugs. The drugs are usually available for injection as hydrochlorides in a salt solution with small amounts of fungicides or preservatives added to give stability.
Article
With the commercial availability of a cream (EMLA) containing a eutectic mixture of local anaesthetics, 2.5% (w/w) lidocaine and 2.5% (w/w) prilocaine, effective topical anaesthesia of the intact skin is possible without the need for subcutaneous injections or exposure to high concentrations of local anaesthetics. In our hospital a topical anaesthetic product was designed for the same purpose. The home-made product contains a eutectic mixture of a local anaesthetic (5% w/w) and l-menthol (1% w/w). Prilocaine was used as the local anaesthetic because it is known for its safety and its well investigated analgesic effects. The eutectic mixture of prilocaine and l-menthol was mixed with a carbopol hydrogel (1% w/w). Preliminary testing of this anaesthetic hydrogel in our hospital has yielded satisfactory results. The anaesthetic hydrogel was found to be stable after at least 3 months' storage at ambient temperature.
Article
The present study was undertaken to assess and compare the in vitro cytotoxic effects of three resin acid analogues: dehydrobietic acid, podocarpic acid, O-methylpodocarpic acid; an essential oil from Australia (tea tree oil); and tapped oleoresin from Thailand, on human epithelial and fibroblast cells, using a quantitative neutral red spectrophotometric assay. All of the investigated compounds except for tea tree oil exhibited a cytotoxic activity which was proportional to their concentrations and time of exposure up to 24 h, i.e. higher concentrations and longer time of exposure caused increased cell death. Dehydroabietic acid and the oleoresin were the most toxic compounds followed by O-methylpodocarpic acid, whereas podocarpic acid and tea tree oil showed a lower level of toxicity. On the basis on these findings it is concluded that an isopropyl group on the aromatic C-ring is of great importance for the cytotoxicity of the tested abietane resin acids, thus indicating that the cytotoxic activity of oleoresins most probably is caused by synergistic or additive effects of resin acids. The results from this work support the view that antibacterial activity parallels cytotoxic activity which suggests a similar mode of action, most probably exerted by membrane-associated reactions.
Article
The purpose of this study was to investigate the relative efficacy of Emla cream (a eutectic formulation of lignocaine and prilocaine) and Bonain's solution (equal amounts of cocaine hydrochloride, menthol and phenol) as local anesthetic agents to the tympanic membrane. Fifty patients undergoing bilateral tympanocentesis were included. The patients were used as their own controls. One tympanic membrane was anesthetized with Emla cream and the other with Bonain's solution. The operating microscope was used. After a 30 min analgesic time, tympanocentesis was performed with aspiration of middle ear secretions. Each patient was then asked to fill in a questionnaire that graded the severity of pain experienced: none, very mild, mild, moderate or severe. Findings showed that Bonain's solution was more effective in tympanocentesis. All patients experienced no pain to very mild pain. With Emla cream 15 of 50 patients experienced mild to moderate pain. No significant side effects occurred with either anesthetic agent.
Article
R-(+)-hyoscyamine, the dextro enantiomer of atropine, has been shown to amplify cholinergic transmission. R-(+)-hyoscyamine, unlike S-(-)-hyoscyamine, was able to increase acetylcholine release both in vitro and in vivo at a range of concentrations (10(-14) to 10(-12) M) and doses (5 microg/kg i.p.) which were inadequate for blocking muscarinic receptors. The increase over control values in ACh release was 15.9 +/- 2.1% in in vitro experiments performed in rat phrenic nerve-hemidiaphragm preparations (n = 6), and 63.3 + 16.3% in cortical microdialysis performed in free-moving rats (n = 5). The maximum ACh release was reached 60 min after R-(+)-hyoscyamine administration in in vivo experiments. At the same doses and concentrations, R-(+)-hyoscyamine was also able to elicit: antinociception of a cholinergic type (55.6-112.7% depending on the test used); complete prevention of scopolamine- and dicyclomine-induced amnesia; potentiation of muscular contractions electrically evoked in isolated guinea-pig ileum (16.7 +/- 3.6%) and in rat phrenic nerve-hemidiaphragm (19.9 +/- 3.2%) preparations. Antinociception was performed using the hot-plate and acetic acid abdominal