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St. John’s Wort (Hypericum perforatum)

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Abstract

Hypericum perforatum L. also known as St John’s wort (SJW) is an effective dietary supplement for treating various nervous system related disorders. It overcome anxiety, mild to moderate depression, mood disorders and stress due to the presence of vast number of bioactive compounds. As such, hypericin and hyperforin are the major compounds along with other less abundant compounds such as flavonoids, biflavonoids, phloroglucinols, napthodianthrones, xanthones, proanthocyanidins, phenolic acid, etc. Beside its effect over nervous system, SJW also effective against cancer, oxidative stress, inflammation and microbial infections. It is one of the high selling natural supplements in USA and other western countries. However, interaction of SJW with other medicines such as warfarin, phenoprocumon, cyclosporine, oral contraceptives, theophylline, digoxin, indinavir and lamivudine have been reported and thus cautions must be taken while using these medicines along with SJW.

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... Though, there is little data about the influence of temperature on drying of St. John's wort. As common drying temperature applied in practice, a wide range between 40 and 60 °C is mentioned (5,9). Soysal and Öztekin (19) achieved high quality in terms of color when drying St. John's wort in a tray dryer at a temperature of 46 ± 4 °C, but they did not investigate other temperatures. ...
Article
St. John's wort (Hypericum perforatum L.) is a medicinal plant and a base material for mild to moderate antidepressants. For most processing procedures harvesting is followed by drying. However, there is little data about the influence of temperature on drying. Therefore, purpose of this study was to investigate the impact of drying air temperature on quality in terms of color and hypericin content. Drying curves have been established by a laboratory dryer with continuous weighing system. Color was measured in the L,a,b-system and characterized by hue-value. Hypericin was measured according to DAC standard. Applying 60 degrees C drying air temperature instead of 45 degrees C resulted in 80% drying time reduction. Drying air temperature between 30 and 90 degrees C did not affect the hypericin content. Values ranged between 0.05 and 0.10% and even for drying air temperature of 90 degrees C hypericin content was 0.07%. For drying temperatures above 50 degrees C, however the leaves turned yellow, indicated by a considerable reduction of hue-values. Two-phase drying, starting at temperatures of 40 degrees C until reaching a moisture content of 45 to 50% followed by final drying at 60 degrees C preserved color at a 55% drying time reduction compared to one-phase drying at 45 degrees C. Higher reductions can be achieved by optimizing drying temperature and duration of the pre-drying-phase by further investigations.
... This plant has also been reported from temperate locations in Asia, Africa, Australia, New Zealand and North and South America. [1] In India, it is reported from Western Himalayas from Jammu and Kashmir to Himachal Pradesh at an altitude of 2000-3000 m. [6,9] This plant is called by various names in different countries that is, Dendhu, Balsana and Bassant in India; Blutkraut, Herrgottsblut and Johaniskraut in Germany; Herba de Millepertuis and Herba de Saint Jean in France and Saint John's-wort in England. [10][11][12] The pharmacognostic and fluorescence studies of H. perforatum L. have been conducted to carry out correct identification of plant species for homoeopathic drug preparation and to lay down the standards of the raw drug. ...
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Follow this and additional works at: https://ijrh.researchcommons.org/journal Part of the Homeopathy Commons Anatomical characterisation and foliar microscopy of Hypericum perforatum L. Anatomical characterisation and foliar microscopy of Hypericum perforatum L. Abstract Abstract Background Background: Hypericum perforatum L. (family: Hypericaceae), commonly known as St. John's-wort, is a perennial herb and traditionally used for treating anxiety, depression, gastritis, insomnia also menstrual disorders and for healing cuts and burns. In homoeopathy, this remedy is used for the treatment of injuries, tetanus, neuritis, tingling, burning and numbness and constant drowsiness, coccydynia, spasmodic asthmatic attacks with changes of weather, etc.
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The Hypericum genus contains one of the few genera of flowering plants that contains a species with authorization for marketing as a traditional medicine, H. perforatum. Due to the fact that this is a large genus, comprising numerous species, a large amount of interest has been shown over the years in the study of its various pharmacological activities. The chemical composition of these species is quite similar, containing compounds belonging to the class of phloroglucinol derivatives, naphthodianthrones, phenols, flavonoids and essential oils. Taking all of this into consideration, the present study aims to offer an overview of the species of the genus from the point of view of their extraction techniques and analysis methods. An extensive study on the scientific literature was performed, and it revealed a wide range of solvents and extraction methods, among which ethanol and methanol, together with maceration and ultrasonication, are the most frequent. Regarding analysis methods, separation and spectral techniques are the most employed. Therefore, the present study provides necessary data for future studies on the species of the genus, offering a complete overview and a possible basis for their development.
Chapter
Hypericum perforatum (St. John’s wort) is the most commonly used and best studied nutraceutical. The most common preparations, made from the flowering aerial parts (Hyperici herba), are extracts and oleums. The method and solvent determine the phytochemicals that are extracted from H. herba. In Germany, standardized H. perforatum extracts are sold as prescription phytopharmaceuticals for mild to moderate depression. H. perforatum has substantial scientific evidence that standardized extracts are efficacious for mild to moderate depression. H. perforatum extracts are also used to treat premenstrual and menopause syndromes. H. perforatum extracts are used in pain management and likely act synergistically with morphine, including reduction of morphine tolerance. H. perforatum oleums are used to treat burns and wounds including boiling water burns in children, and surgical wounds from excision of scalp neoplasms, cesarean sections, and episiotomies. The phytochemicals in H. perforatum extracts, when taken orally, can alter drug-transporter and drug-metabolizing enzymes (CYPs). Excessive use of H. perforatum can cause photosanitization. H. perforatum extracts should be taken under the supervision of a physician or pharmacist, and the patient should advise physicians and nurses if they are using H. perforatum extracts. Also, it is important that physicians and nurses include nutraceuticals and supplements when taking a use of medications history and be knowledgeable of potential interactions.
Chapter
Hypericum perforatum L. (Hypericaceae) is a perennial plant commonly known as St. John’s Wort that has been used for centuries as a medicinal herb (it has antidepressant, antiviral, wound healing, antiinflammatory, etc. properties). It contains numerous pharmacologically active ingredients, including naphthodianthrones (hypericin, pseudohypericin). These natural compounds have beneficial activity in neurodegenerative disorders, such as Alzheimer’s disease, because of their neuroprotective and antidepressant properties.
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Hypericum L. (Hypericaceae) extracts have been used for their therapeutic effects; however, not much is known about the immunomodulatory activity of essential oils extracted from this plant. We isolated essential oils from the flowers and leaves of H. perforatum and analyzed their chemical composition and innate immunomodulatory activity. Analysis of flower (HEOFl) versus leaf (HEOLv) essential oils using gas chromatography–mass spectrometry revealed that HEOFl was comprised mainly of monoterpenes (52.8%), with an abundance of oxygenated monoterpenes, including cis-p-menth-3-en-1,2-diol (9.1%), α-terpineol (6.1%), terpinen-4-ol (7.4%), and limonen-4-ol (3.2%), whereas the sesquiterpenes were found in trace amounts. In contrast, HEOLv was primarily composed of sesquiterpenes (63.2%), including germacrene D (25.7%) and β-caryophyllene (9.5%). HEOLv also contained oxygenated monoterpenes, including terpinen-4-ol (2.6%), while monoterpene hydrocarbons were found in trace amounts. Both HEOFl and HEOLv inhibited neutrophil Ca2+ mobilization, chemotaxis, and reactive oxygen species (ROS) production, with HEOLv being much more active than HEOFl. Furthermore, the pure sesquiterpenes germacrene D, β-caryophyllene, and α-humulene also inhibited these neutrophil responses, suggesting that these compounds represented the active components of HEOLv. Although reverse pharmacophore mapping suggested that potential protein targets of germacrene D, β-caryophyllene, bicyclogermacrene, and α-humulene could be PIM1 and mitogen-activated protein kinase (MAPK)-activated protein kinase 2 (MAPKAK2), a kinase binding affinity assay did not support this finding, implying that other biological targets are involved. Our results provide a cellular and molecular basis to explain at least part of the beneficial immunotherapeutic properties of the H. perforatum essential oils.
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Nigella sativa (NS) has been reported to have a therapeutic effect towards skin wound healing via its anti-inflammatory, tissue growth stimulation, and antioxidative properties. This review examines all the available studies on the association of Nigella sativa (NS) and skin wound healing. The search was performed in Medline via EBSCOhost and Scopus databases to retrieve the related papers released between 1970 and March 2020. The principal inclusion criteria were original article issued in English that stated wound healing criteria of in vivo skin model with topically applied NS. The search discovered 10 related articles that fulfilled the required inclusion criteria. Studies included comprise different types of wounds, namely excisional, burn, and diabetic wounds. Seven studies unravelled positive results associated with NS on skin wound healing. Thymoquinone has anti-inflammatory, antioxidant, and antibacterial properties, which mainly contributed to wound healing process.
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St. John’s Wort (SJW) is an herbaceous medical plant. Since ancient times, SJW has been used to treat different kinds of mental and physical diseases and, for its antiseptic, anti-inflammatory and antibacterial properties. The aim of this study was to evaluate the wound healing activity of a phytotherapeutic product from St. John’s Wort (SJW), herbaceous medical perennial plant, on skin lesions of different origins, in horses housed in Sicily (Italy). Six horses of different breeds, age and attitude were enrolled in the study. All the lesions were treated with an oil prepared from the aerial parts of Hypericum perfoliatum (H. perfoliatum), macerated in oil under the sun. Topical application of the oil determined a significant improvement of skin lesions in all the horses involved in the study. Wound healing begun (Time1) in a period ranging from 2 days to 2 weeks (mean ± SD, 4 ± 1.89 days). The treatment resulted in complete resolution of wounds (Time2) in a period between 1 and 5 weeks (mean ± SD, 14.5 ± 8.2 days), while hair re-growth (Time3) was completed in period between 25 days and 2 months (mean ± SD, 33.25 ± 12.58 days). This study has certainly given a scientific point of view to a century of empiricism about the use of SJW in veterinary practice. The findings of this study seem to suggest that SJW may be considered an “all-in-one” remedy for wound healing, in order to make the management of skin injuries easier even for severe and complicated lesions.
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Background: The purpose of this study was assessed the efficacy of Achillea millefolium and Hypericum perforatum ointments on episiotomy wound healing in primiparous women. Materials and Methods: This is double blind clinical trial study that was performed on 140 primiparous women. They were randomly divided into four groups each one containing 35 women: 2control groups including non-intervention and placebo ointment; and 2case groups including Hypericum perforatum ointment, and Achillea millefolium ointment. Healing process was assessed by 5 specifications: redness, ecchymosis, edema, discharge and wound dehiscence at 7th, 10th, and 14th days after delivery, pain level was assessed by means of visual analogue scale. Results: There was significant difference between groups in perineal pain level at 7th & 10th & 14th, redness and edema at 7th & 10th and ecchymosis at 7th days postpartum, as pain level, redness, edema and ecchymosis in groups who consume Hypericum perforatum and Achillea millefolium ointments were less than control groups (P < 0.05). But discharge and dehiscence incidence showed no significant difference between groups (P > 0.05). Conclusion: Achillea millefolium and Hypericum perforatum ointments reduce perineal pain level, redness, edema and ecchymosis of episiotomy wound so, it seems that consuming them is useful for episiotomy treatment.
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Background: Patients with high levels of total cholesterol (TCH), low-density lipoprotein cholesterol (LDL-CH), and triglyceride (TG) are at increased risk of coronary heart disease. Studies have shown that flavonoids and antioxidant compounds have beneficial effects on hyperlipidemia. Objectives: The aim of the present study was to evaluate the effects of extract of Hypericum perforatum (EHP) on the serum lipid profile (TCH, TG, and LDL-CH), aminotransferase, alkaline phosphatase, and lipid peroxidation in hyperlipidemic rats. Materials and methods: Thirty-two male rats weighting 200 ± 10 g were randomly divided into four experimental groups: 1) control, 2) control + EHP, 3) hyperlipidemia, and 4) hyperlipidemia + EHP. The rats in the hyperlipidemic groups were fed a high-fat diet for 60 days, and EHP (300 mg/kg) was injected intraperitoneally for 2 weeks in the rats in the second and fourth groups. At the end of the experimental period, blood samples from each group were analyzed. Results: There was a significant reduction in LDL-CH in the control + EHP group and the hyperlipidemia + EHP group (P < 0.05). TCH was significantly reduced in the control + EHP group (P < 0.05). There were no significant changes in the levels of TG and HDL-CH. Malondialdehyde, aspartate aminotransferase, and alanine aminotransferase were significantly reduced in the hyperlipidemia + EHP group (P < 0.05), with no significant change in alkaline phosphatase. Conclusions: EHP was able to both reduce LDL-CH and to significantly decrease markers of oxidative stress and lipid peroxidation induced by hyperlipidemia. Therefore, this herb, as a new pharmacological component, could be used to reduce certain blood lipids, lipid peroxidation, and aminotransferase markers.
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Context: One traditional medicines, Hypericum perforatum L. (Hypericaceae), possesses several beneficial effects against depression, ulcers, dyspepsia, abdominal pains, burns, bacterial infections, migraine headaches, and sciatica. Objective: The present study investigates the antimicrobial activity of the ethanol extract (HP-EtOH) of H. perforatum and its sub-extracts, namely n-hexane (HP-hexane), chloroform (HP-CHCl3), ethyl acetate (HP-EtOAc), n-butanol (HP-n-BuOH), and water (HP-H2O) extracts, against Streptococcus mutans, S. sobrinus, Lactobacillus plantarum, and Enterococcus faecalis. Materials and methods: For the evaluation of the antimicrobial activity, flowering aerial parts of H. perforatum were extracted with EtOH and then this extract was fractionated to obtain five sub-extracts in different polarities. Antimicrobial activities of HP-EtOH and its sub-extracts against Streptococcus mutans, S. sobrinus, L. plantarum, and E. faecalis were assessed by using colorimetric micro-well dilution at concentration ranges of 64–0.5 μg/ml as well as resazurin microplate and modified microtiter-plate assays between the ranges of 100 and 0.78125 μg/ml. Results: According to the results of the present study, HP-H2O sub-extract displayed strong antibacterial activity (MIC values 8 μg/mL) against S. sobrinus and L. plantarum, and exerted moderate activity against S. mutans and E. faecalis at 32 and 16 μg/mL concentrations, respectively. Other sub-extracts also demonstrated antimicrobial activity against S. sobrinus at a concentration of 16 μg/mL. HP-EtOAc and HP-n-BuOH showed antimicrobial activity against L. plantarum and HP-EtOAc and HP-H2O were also active against E. faecalis at the same concentrations (16 μg/mL). Conclusion: According to the results, we suggest that H. perforatum could be employed as a natural antibacterial agent in oral care products.
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The genus Hypericum L. (Hypericaceae) comprises around 500 species divided in 36 sections. From ancient times, the common St. John’s wort (Hypericum perforatum L.) was often used in traditional pharmacy and medicine, and as important source of traditional drugs was, subjected to wide spectra of researches. Summarised data assured several clinical indications, which confirm the effectiveness of traditional uses. Thus, constant worldwide rise of demand for Hyperici herba is present. World Health Organization (WHO) has marked H. perforatum as the only botanical source of Hyperici herba, but some pharmacopoeias list Hypericum maculatum side by side with H. perforatum. So, the question is whether some other species of the genus also could be used for that purpose. Depending on indications, two main types of preparations obtained from Hyperici herba are available on the market. Water alcoholic extracts are mainly indicated in the cases of mild to moderate depression and oil macerates are being used in treatment of burns, eczema, dyspepsia, gastric ulcer and inflammation. Recently, more and more attention is being given to the other representatives of the genus, such are H. maculatum, H. barbatum, H. rocheli, H. umbellatum, H. rumeliacum, etc. Different analytical methods such are liquid and gas chromatography revealed the chemical profiles of these species. Also, numerous in vitro test-systems gave the opportunity for evaluation of their biological potential. Considering that the main bioactive compounds present in H. perforatum are flavonoids (rutin, quercitrin, quercetin, hyperoside, amentoflavone), naphtodianthrones (hypericin, pseudohypercin), phloroglucinol derivatives (hyperforin, adhyperforin), tannins and essential oil, a certain level of resemblance between chemical profiles of these representatives of the genus can be observed. Furthermore, the existence of similarity in main compounds of analysed essential oils cannot be denied. It is important to highlight that in some species of the genus certain compounds occur even in higher levels than in H. perforatum (e.g. H. rumeliacum and H. barbatum are especially rich in hypericins). But, it is confirmed that the amounts of secondary metabolites vary not only related to the species, but also in relation to ecological factors of the habitats and stage of plant development. Additionally, novel possible botanical sources of Hyperici herba show comparable and, in some cases, stronger antioxidant, cytotoxic, antimicrobial, antifungal and antiviral potential than the H. perforatum.
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BACKGROUND/OBJECTIVES This study was conducted to assess the potential of St. John's Wort (Hypericum perforatum) to prevent obesity and abnormalities in lipid metabolism induced by ovariectomy in a rat model without stimulatory activity on uterus. MATERIALS/METHODS Ovariectomized (OVX) rats were treated for 6 weeks with 70% ethanol extracts of Hypericum perforatum [HPEs: whole plant (WHPE) and flower and leaves (FLHPE)], β-estradiol-3-benzoate at a dose of 50 µg/kg/day (E2) or vehicle (distilled water). RESULTS As expected, OVX increased body weight gain and adiposity and showed higher food efficacy ratio. OVX also increased the serum cholesterol as well as insulin resistance, while reducing uterus weight and uterine epithelial proliferation rate. HPEs (WHPE and FLHPE) showed estrogen-like effect on body weight gain, adipose tissue weight and food efficacy ratio in OVX rats. HPEs prevented hypercholesterolemia induced by OVX more effectively than E2. E2 increased uterus weight and epithelial proliferation rate in OVX rats, while HPEs maintained them at the level of the sham-operated animals. CONCLUSIONS Our finding demonstrates that HPEs can be considered as an effective agent to prevent OVX-induced obesity without stimulatory activity on uterus.
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Background This experiment was performed to compare the effects of Phenytoin (PHT) and Hypericin (HP) cream on healing of burn wounds in rats. Material/Methods Twenty rats were divided into 3 groups and second-degree burn wounds were created. The burn wounds in the first, second, and third groups were covered twice daily with PHT cream, HP cream, and saline (control), respectively. At the end of days 3, 7, 14, and 21, full-thickness skin biopsies were done for histopathologic and immunohistochemical analyses. Results Histopathologic evaluations at the 14th day showed that re-epithelialization scores were greater in the HP group than the PHT group, but on day 21, re-epithelialization scores were higher in the PHT group than the HP group. Collagen content on days 3 and 14 in the PHT group was found to be higher than in the HP group. Well-vascularized granulation tissue on day 7 in the PHT group was higher than in other groups. HP and PHT groups had a significant increase in VEGF and TGF-β expression in burn wound healing area compared to the control group on all days. Conclusions Topical application of HP can promote re-epithelialization in burn wounds to shorten the wound healing time for superficial burns. Phenytoin, on the other hand, contributes to healing by increasing vascularized granulation tissue and collagen synthesis through re-epithelialization. The increased VEGF and TGF-β expression following PHT and HP treatment strongly indicate that PHT and HP treatment promotes VEGF and TGF-β production and action in the burn wound area.
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Context: Hypericum perforatum Linn. (Hypericaceae) (St. John's wort) attenuates opium withdrawal signs. Aim: To explore the therapeutic potential of Hypericum perforatum in the management of opium-induced withdrawal syndrome. Materials and methods: The effect of the Hypericum perforatum hydro-ethanol extract was investigated for potential to reverse naloxone (0.25 mg/kg)-induced opium withdrawal physical signs. Rats received opium extract (80-650 mg/kg) twice daily for 8 days along with Hypericum perforatum (20 mg/kg, orally) twice daily in chronic treatment and the same single dose 1 h before induction of withdrawal syndrome in the acute treated group. Results: Hypericum perforatum reduced stereotype jumps and wet dog shake number in the chronic treatment compared to the saline control group (F(2, 24) = 3.968, p < 0. 05) and (F(2, 24) = 3.689, p < 0.05), respectively. The plant extract in the acutely treated group reduced diarrhea (F(2, 24) = 4.850, p < 0. 05 vs. saline). It decreased rectal temperature by chronic treatment at 30 min (F(2, 24) = 4.88, p < 0.05), 60 min (F(2, 240 = 5.364, p < 0.01) and 120 min (F(2, 24) = 4.907, p < 0.05). Discussion and conclusion: This study reveals that the extract of Hypericum perforatum attenuates some physical signs of opium withdrawal syndrome possibly through direct or indirect interaction with opioid receptors. Further study is needed to clarify its mechanism.
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Kalopanax pictus is known as Castor-Aralia or Prickly Castor-oil tree. K. pictus extracts have been used for dietary health supplements and are an important area in drug development with numerous pharmacological functions in East Asia; however, their pharmacological functions have not been introduced in Western countries. This paper briefly reviews the most relevant experimental data on the pharmacological actions of K. pictus to overcome the lack of information on this plant. K. pictus extracts have proved to be effective in the treatment of inflammation and were shown to have a number of pharmaceutically relevant benefits that include anti-rheumatoidal, hepatoprotective, anti-diabetic, anti-cancer effects, etc. There are a few known active pharmacological components such as kalopanaxsaponin A and I. Although the molecular mechanisms of most of the effects are not fully understood, major mechanisms seem to involve the interplay between active components and signaling mediated by phosphorylation events during stress adaptation.
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AIMS AND METHOD St John's wort is popularly taken as a herbal remedy, but it interacts with prescribed drugs. The aim of this survey was to estimate the prevalence of patients self-medicating with St John's wort. All new referrals to a community mental health team over 5 months were asked about any use of St John's wort. RESULTS Fifteen patients, of 101, had taken St John's wort at some time and of those seven were currently taking it. Patients who used St John's wort tended to be younger and female. Only nine of the 15 patients took it for depressive symptoms and none had received medical advice. One patient was taking an interacting medication. CLINICAL IMPLICATIONS A significant number of patients are taking St John's wort. In order to prevent drug interactions, doctors should ask all patients whether they use it, especially young women who may be on the contraceptive pill. Patients need better education about its risks and benefits and it should be taken with medical advice.
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The content of hypericins (hypericin and pseudohypericin), hyperforin, and flavonoids (rutin, hyperoside, quercitrin, and quercetin) and genetic profiles of eight accessions of Hypericum perforatum L., collected from different locations in India, have been determined. The secondary metabolite content was determined using a highly selective LC/MS/MS method. Pearson and Spearman's correlation coefficient were used to investigate the relationships between the secondary metabolites and a significant positive correlation was found between hypericin and pseudohypericin contents. Genetic profiling was undertaken using the random amplification of polymorphic DNA (RAPD) and single sequence repeat (SSR) methods. Among the 49 random primers used for the initial screening, only nine yielded polymorphic RAPD profiles. The SSR analysis shows that seven out of the 11 primers were polymorphic. There exists only a partial correlation between the chemical content and genetic profiling data among the accessions under study.
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Little is known about the effective role of Hypericum perforatum on hepatic ischemia-reperfusion (I/R) injury in rats. Hence, albino rats were subjected to 45 min of hepatic ischemia followed by 60 min of reperfusion period. Hypericum perforatum extract (HPE) at the dose of 50 mg/kg body weight (HPE50) was intraperitonally injected as a single dose, 15 min prior to ischemia. Rats were sacrificed at the end of reperfusion period and then, biochemical investigations were made in serum and liver tissue. Liver tissue homogenates were used for the measurement of malondialdehyde (MDA), catalase (CAT) and glutathione peroxidase (GPx) levels. At the same time alanine aminotransferase (ALT), aspartate aminotransferase (AST) and lactate dehydrogenase (LDH) were assayed in serum samples and compared statistically. While the ALT, AST, LDH activities and MDA levels were significantly increased, CAT and GPx activities significantly decreased in only I/R-induced control rats compared to normal control rats (p < 0.05). Treatment with HPE50 significantly decreased the ALT, AST, LDH activities and MDA levels, and markedly increased activities of CAT and GPx in tissue homogenates compared to I/R-induced rats without treatment-control group (p < 0.05). In oxidative stress generated by hepatic ischemia-reperfusion, H. perforatum L. as an antioxidant agent contributes an alteration in the delicate balance between the scavenging capacity of antioxidant defence systems and free radicals in favour of the antioxidant defence systems in the body.
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The present study describes the influence of hypericin of Hypericum perforatum on TPA- and LPS-induced arachidonic acid (AA) metabolism, as well as interleukin 1 α and nitric oxide (NO) production in human immunocompetent cells. The results show that hypericin inhibits the release of arachidonic acid (AA) from membrane phospholipids in calcium ionphore A23187-TPA stimulated human granulocytes in a dose-dependent manner (IC(50) 4 μM), but that calcium ionophore is not the only inducer. An inhibitory effect could be observed at concentrations of < 0.4 μM and in the presence of low concentrations of TPA (0.16 - 0.32 μM). As a result of this inhibition hypericin inhibits the release of LTB(4) but not of PGE(2). Hypericin also inhibits the production of IL-1α in LPS-stimulated human monocytes and activates NO production in isolated human leukocytes. This effect is comparable to the effect of LPS and is probably not associated with the IL 1 a or intermediates of the cycloxygenase pathway. The results as a whole let us assume that one important mechanism for the antiviral, antiinflammatory and antitumoral effects of hypericin and Hypericum extracts is the inhibition of the PKC-mediated signalling pathway which in turn influences the AA metabolism, and the interleukin-1 α production resulting in an immunosuppressive effect on the host immune system.
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The relative stereochemistry of hyperforine - an antibiotic from hypericum perforatum L. was elusidated by X-ray crystalography.
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To investigate if extracts of Hypericum perforatum (St John's wort) are more effective than placebo in the treatment of depression, are as effective as standard antidepressive treatment, and have fewer side effects than standard antidepressant drugs. Systematic review and meta-analysis of trials revealed by searches. TRIALS: 23 randomised trials including a total of 1757 outpatients with mainly mild or moderately severe depressive disorders: 15 (14 testing single preparations and one a combination with other plant extracts) were placebo controlled, and eight (six testing single preparations and two combinations) compared hypericum with another drug treatment. A pooled estimate of the responder rate ratio (responder rate in treatment group/responder rate in control group), and numbers of patients reporting and dropping out for side effects. Hypericum extracts were significantly superior to placebo (ratio = 2.67; 95% confidence interval 1.78 to 4.01) and similarly effective as standard antidepressants (single preparations 1.10; 0.93 to 1.31, combinations 1.52; 0.78 to 2.94). There were two (0.8%) drop outs for side effects with hypericum and seven (3.0%) with standard antidepressant drugs. Side effects occurred in 50 (19.8%) patients on hypericum and 84 (52.8%) patients on standard antidepressants. There is evidence that extracts of hypericum are more effective than placebo for the treatment of mild to moderately severe depressive disorders. Further studies comparing extracts with standard antidepressants in well defined groups of patients and comparing different extracts and doses are needed.
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The Iowa Center for Research on Botanical Dietary Supplements seeks to optimize Echinacea, Hypericum, and Prunella botanical supplements for human-health benefit, emphasizing anti-viral, anti-inflammatory, and anti-pain activities. This mini-review reports on ongoing studies on Hypericum. The Center uses the genetically diverse, well-documented Hypericum populations collected and maintained at the USDA-ARS North Central Regional Plant Introduction Station (NCRPIS), and the strength of research in synthetic chemistry at Iowa State University to tap natural diversity, to help discover key constituents and interactions among constituents that impact bioactivity and toxicity. The NCRPIS has acquired more than 180 distinct populations of Hypericum, with a focus on Hypericum perforatum L. (Hypericaceae), representing about 13% of currently recognized taxa. Center chemists have developed novel synthetic pathways for key flavones, acyl phloroglucinols, hyperolactones, and a tetralin that have been found in Hypericum, and these compounds are used as standards and for bioactivity studies. Both light-dependent and light-independent anti-viral activities have been identified by using bioactivity-guided fractionation of H. perforatum and a HIV-1 infection test system. Our Center has focused on light-independent activity, potentially due to novel chemicals, and polar fractions are undergoing further fractionation. Anti-inflammatory activity has been found to be light-independent, and fractionation of a flavonoid-rich extract revealed four compounds (amentoflavone, chlorogenic acid, pseudohypericin, and quercetin) that interacted in the light to inhibit lipopolysaccharide-induced prostaglandin E2 activity. The Center continues to explore novel populations of H. perforatum and related species to identify constituents and interactions of constituents that contribute to potential health benefits related to infection.
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The ability for synthesis of hypericins and phloroglucinols was studied in in vitro grown Hypericum perforatum seedlings. HPLC analysis of hypericin, pseudohypericin and their immediate precursors protohypericin and protopseudohypericin, and phloroglucinols, hyperforin and adhyperforin, revealed great intraspecific variation. A significant correlation was found between the total content of hypericins and phloroglucinols and between the content of hypericin/protohypericin and pseudohypericin/protopseudohypericin. The presence of hyperforin and adhyperforin was first proved in the Hypericum perforatum seedlings at early stage of development. Peculiarities in reproduction pathways do not primarily affect the formation of secondary metabolites but significantly contribute to genetic variation. Genetic factors as ploidy level, inheritance of the mode of reproduction, coexistence of several reproductive pathways in a particular plant that contribute to chemical variation, which is expressed in the early stages of ontogeny are discussed.
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Objective: To evaluate the antihyperglycemic activity of ethyl acetate extract of Hypericum perforatum (H. perforatum) in streptozotocin (STZ)-induced diabetic rats. Methods: toxicity and oral glucose tolerance test were performed in normal rats. Acute rendered diabetic by Male albino rats were orally administered toS dTiZa b(4e0ti cm rga/tksg ,a ti ntraperitoneally). H. perforatum ethyl acetate extract was antihyperglycemic activity. 50, 100 and 200 mg/kg doses for 15 days to determine the Biochemical parameters were studied at the end of the treatment. Results: H. perforatum ethyl acetate extract showed dose dependant fall in fasting blood glucose (nFoBrGm)a. lA rfatetsr. 3H0 . mpeinrf oorfa etxutmra cett haydlm aicneitsattrea teioxntr,a FctB pGr owdausc reedd usicgendi fsicigannitf irceadnutclyti ownh ienn pcloamsmpaar geldu cwoisthe cleovnetle,n st,e rHuDmL -tocthaol lcehstoelreoslt,e rgolul,c torsieg-ly6c-eprihdoessp,h galtuec doseeh-yd6-ropgheonsapshea twaesree lseivgenlisf.i cTainsstluye inglcyrceoagseend compared with diabetic control. No death and lethal effect was observed in the toxic study. Conclusions: The results demonstrate that H. perforatum ethyl acetate extract possesses potent antihyperglycemic activity in STZ induced diabetic rats.
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Sambucus ebulus is known as dwarf elder or elderberry. S. ebulus extracts are an important area in drug development with numerous pharmacological functions in the Middle East. However, their pharmacological functions have not been clearly studied. For a long time, S. ebulus has been prescribed in traditional medicines for the treatment of inflammatory reactions, such as hemorrhoid, bites and sore-throat. In addition, S. ebulus has recently been shown to have anti-inflammatory, antinociceptive, anti-cancer, anti-angiogenic and anti-oxidative activities. Ebulitin, ebulin 1, flavonoid, athocyanin and other components have been isolated from S. ebulus and identified as active ingredients of biological and pharmacological activities. Due to the easy collection of the plant and remarkable biological activities, this plant has become both food and medicine in the coastal area of Iran. This review presents comprehensive analyzed information on the botanical, chemical, toxicopharmacological and clinical aspects of S. ebulus.
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Hypericum perforatum is known to have diverse medicinal uses for centuries. The antidepressant activity of Hypericum perforatum is widely accepted and proved in both animal and clinical studies. Present study was undertaken to investigate the effect of Hypericum perforatum in a battery of animal models for metabolic disorder. Hypericum is tested for hypolipidemic activity in normal rats, antiobesity activity in high-fat-diet induced obese rats, and fructose-fed rats. Hypericum was orally administered as suspension in 0.3% carboxymethyl cellulose at the doses of 100 and 200 mg/kg body weight for 15 consecutive days. Hypericum significantly lowered total cholesterol and low-density cholesterol in normal rats. Hypericum significantly inhibited weight gain in high-fat-fed rats. In fructose-fed rats, Hypericum normalised the dyslipidemia induced by fructose feeding and improved the insulin sensitivity. Taken together, Hypericum could be the antidepressant therapy of choice for patients suffering from comorbid diabetes and obesity.
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A randomized, double-blind study examining the effectiveness and tolerance of a standardized hypericum preparation when compared to maprotiline was performed in a group of 102 patients with depression, in accordance with ICD-10, F 32.1. The study was conducted in the offices of neurology and psychiatry specialists. The patients received, over a period of 4 weeks, either 3 x 300 mg of the hypericum extract or 3 x 25 mg maprotiline pills of identical appearance. Effectiveness was determined using the Hamilton Depression Scale (HAMD), the Depression Scale according to von Zerssen (D-S), and the Clinical Global Impression Scale (CGI). The total score of the HAMD scale dropped during the 4 weeks of therapy in both treatment groups by about 50%. The mean values of the D-S scale and the CGI scale showed similar results, and after 4 weeks of therapy, no significant differences in either treatment group were noticed. The onset of the effects occurred up to the second week of treatment, but were observed earlier with maprotiline than with the hypericum extract. On the other hand, maprotiline treatment resulted in more cases of tiredness, mouth dryness, and heart complaints.
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Background: Surgical wounds in diabetic patients still remain a problem till the present day. As a common plant found around the world, Hypericum perforatum L. (Hypericaceae) is traditionally prepared as an oily extract and used as a folk remedy for various diseases such as wounds, burns, cuts, etc. This study aims to evaluate the effect of St. John's wort (Hypericum perforatum) on problematic wounds while comparing oral and topical applications. Methods: Incisional and excisional wound models were made on the dorsal regions of 54 diabetic Spraque-Dawley rats. The rats were divided into the following six groups (n = 9): Group 1: control, Group 2: diabetic, Group 3: diabetic oral Hypericum perforatum, Group 4: diabetic topical Hypericum perforatum, Group 5: diabetic oral olive oil, and Group 6: diabetic topical olive oil. Results: Groups 3 and 4 had significantly higher tensile strength, tissue hydroxyproline concentration, and collagen density compared with Group 2. Inflammatory cell density and collagen density on day 3 were significantly higher in Groups 3 and 6 compared with Group 2. On day 21, Groups 3 and 6 had significantly higher fibroblastic activity compared with Group 2. Conclusions: This study has proved that oral St. John's wort has more positive effects on problematic wounds compared with topical St. John's wort and olive oil, which is a vehicle. Hypericum perforatum results with faster inflammatory response and better healing. These results could be an addition to literature about the clinical usage of Hypericum perforatum on diabetic wounds.
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Ethnopharmacological relevance: Topical formulations such as oily extracts or ointments prepared with the flowering aerial parts of St.John's wort (Hypericum perforatum L., Hypericaceae) have been used in the management of a wide range dermatological problems including superficial wounds and burns, bruises, contusions and many others in the worldwide traditional medicines. Aim of the study: This is the first case study reporting the beneficial effects of an oily extract of St.John's wort in the treatment of pressure sores in a intensive care unit (ICU) patient. Material and methods: The oily extract of St.John's wort was applied to a volunteer patient at ICU daily for forty successive days for wound care and treatment. Healing status was monitored macroscopically by measuring the wound size and stages at certain intervals as well as histopathological evaluation of the tissue sections taken at the initial and final dates of treatment. Results: Evaluation of the results obtained from the macroscopical and histopathological experimentation have shown that oily extract of St.John's wort provided significant efficacy for the treatment of pressure sore wounds. Conclusion: St.John's wort oily extract may be suggested as a cost-effective option for the prevention or treatment of pressure sores in ICU patients.
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The aim of this study was to investigate effects of the Hypericum perforatum (St John’s Wort) on bone healing in rabbit calvarium. Ten male New Zealand rabbits each had three bicortical defects made in the calvarial bones, which were filled with xenograft, xenograft + H perforatum oil extract, and autogenous graft. Four weeks postoperatively all rabbits were killed and the bony defects examined histomorphometrically. Tissue compartments including new bone (p < 0.001), marrow space (p < 0.001), and residual bone grafts (p = 0.014) differed significantly among groups (p = 0.00?). The volume of residual graft was significantly decreased in the xenograft/H perforatum group compared with those with xenografts alone (p = 0.0147). The differences in microarchitectural variables of de novo bone formation were also significant (trabecular thickness (p < 0.001), trabecular width (p < 0.001), trabecular separation (p = 0.001). There were no significant differences in node:terminus ratio between the xenograft/H perforatum group and the other two groups. However, the difference in node:terminus ratio between the autogenous graft and xenograft group was significant (p = 0.001) Oil extracts of H perforatum improved bony healing in defects filled with bovine-derived xenografts.
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Objective: Our aim was to investigate the curative role of topical Hypericum perforatum (HP) in a rat model of tympanic membrane perforation in a histopathological manner. Materials and methods: This study was conducted on 30 female Sprague-Dawley rats. An HP extract was prepared as a suspension in pure olive oil. In all rats, the right and left tympanic membranes were perforated by a fine puncture under a microscope. Rats were randomly assigned to three groups. The HP extract was given as drops on a daily basis in Group 1, while olive oil alone was given on a daily basis in Group 2. In Group 3, the rats were allowed spontaneous recovery without any intervention. Three rats from each group were sacrificed on days 7, 14, and 21. Temporal bullae were removed for histopathological examination to evaluate fibroblast proliferation, leukocyte infiltration, neovascularization, and subepithelial thickness and to compare these among the groups. Results: In histopathological examination of the rats from each group on days 7, 14, and 21, there were significant differences in leukocyte infiltration, fibroblast proliferation, and subepithelial thickness. No significant difference was observed in neovascularization among the groups. Conclusion: Compared with the spontaneous recovery group, HP was found to be more effective in a wound-healing model of the tympanic membrane. HP may be applied in clinical practice if it is shown to be safe with regard to ototoxicity.
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The antimicrobial activity of Hypericum perforatum, H. perfoliatum and H. hircinum, all of Sicilian origin, was investigated. H. perforatum was found to be the most active and showed activity against Gram-positive and Gram-negative bacteria.
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St. John's wort (SJW) extracts, prepared from the aerial parts of Hypericum perforatum, contain numerous pharmacologically active ingredients, including aphthodianthrones (e.g., hypericin and its derivatives) and phloroglucinols derivatives (e.g., hyperforin)[5]. Hyperforin is a structurally novel anti-depressant isolated from Hypericum perforatum commonly known as St.John's Wort. Hyperforin used as antidepressants by blocking the reuptake of the neurotransmitters norepinephrine, serotonin, and dopamine. Recent study found that hyperforin, in high daily doses, is superior to paroxetine[40] as a treatment for even severe depression. Hyperforin is photo and oxygen labile compound that is highly unstable and difficult to isolate in pure form. The standardization of Hypericum perforatum is based on presence of both Hyperforin and Hypericin. It is designated in percentile, meaning that if a 100mg dose of St. John's Wort is extracted at a standardized 5%, we will get 5 mg of hyperforin from that dose. However, relevant and, in some cases, life-threatening interactions have been reported, particularly with drugs which are substrate of cytochrome P450 and/or P-glycoprotein.
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The antiviral and virucidal compound, hypericin, was studied regarding its activity and possible mechanism against herpes simplex virus (HSV-1). It was determined that hypericin caused slight inhibition of viral adsorption to and penetration of Vero cells. Additionally, yield reduction assays suggested that hypericin was most effective against HSV-1 as a virucidal agent rather than as an intracellular antiviral agent. Fluorescence microscopy revealed that hypericin initially associated with cytoplasmic membranes and that over the course of time it became concentrated in intracellular membranous regions, probably the Golgi apparatus or endoplasmic reticulum (ER). These concentration events failed to inhibit glycosylation of either viral or cellular proteins and were effectively blocked by compounds which inhibit endocytosis or membrane cycling between the ER and Golgi. Based on fluorescence studies, it was determined that hypericin had non-specific affinity for protein and higher affinity for detergent and lipid. The evidence suggested that strong, non-specific association with membranes, both viral and cellular, are probably the basis of hypericin's virucidal and antiviral activity.
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(1) A population of the summer annual Erucastrum gallicum (Brassicaceae) colonizing an abandoned limestone quarry near Syracuse, New York, U.S.A., was monitored for five consecutive years and its demographic performance was interpreted in relation to rainfall patterns. (2) Survival and percentage reproduction of plants that emerged in the spring varied markedly depending upon rainfall. Deevey survivorship curves, Types I, II, and III were observed in cohorts from a year with abundant rainfall, a year with intermittent rainfall and drought, and a year with spring drought, respectively. Growth and the number of seeds produced by the population were also influenced by rainfall. (3) The number of seeds produced per plant ranged from 24 to 1675. The latter value is similar to or greater than that recorded in many other annual species. (4) Several lines of evidence suggest that less than half the viable seeds in the soil germinate in any one year and that a substantial proportion of seeds survive from one year to the next. (5) Unlike some annual plants, that persist in variable habitats by exhibiting phenotypic plasticity in growth coupled with high seedling survival, E. gallicum persists in the quarry through a suite of traits including high seed output by those plants that survive to reproduce, germination by a small proportion of the seeds in the seed bank in any one year, and viability of seeds that remain in the soil for at least 1 year.
Article
In this work,the biochemical reactions of the fingi A. niger, P. verrucosum, T. viride, T. harzianum and D. stemonitis to the presence of 30 mg/ml, hypericin, added to the standard nutrient base, were investigated. Hypericin acts in two ways either as an activator of biochemical reactions or as an inhibitor, depending on the fungual species. In already prepared methylene chloride extracts of 14-day old fungi, both the number and the chemical structures of biodegradational products were examined in order to register the possible involvement of hypericin in fungal biochemical reactions and to determine the level of biodegradation. The rate of biodegradation and the number of biodegradational products differed from case to case, with protohypericin as a common intermediary compound. Hypericin was bactericidal to Streptocococcus,A.Streptococcus B, Enteroccocus, E. coli and P. mirabilis in the concentrations of 10 mg/ml, and 20 mg./ml.
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The on-line separation and structure elucidation of naphthodianthrones, flavonoids, and other constituents of an extract from Hypericum perforatum L. using high performance liquid chromatography (HPLC) coupled on-line with ultraviolet−visible, nuclear magnetic resonance (NMR), and mass spectrometry (MS) is described. A conventional reversed-phase HPLC system using ammonium acetate as the buffer substance in the eluent was used, and proton NMR spectra were obtained on a 500 MHz NMR instrument. The MS and MS/MS analyses were performed using negative electrospray ionization. In the present study, all of the major known constituents in extracts from Hypericum perforatum L. were identified, and two new substances which had not previously been reported as constituents of extracts of Hypericum perforatum L. were identified and their structures elucidated.
Article
Evidence suggests that diets with high contents of cholesterol will increase serum lipoproteins and apolipoproteins, thereby increase risk of atherosclerosis. According to literature, some plants show hypolipidemic, hypocholestrolemic, and antiatherosclerotic activities. In this study, antiatherosclerotic effect of Hypericum perforatum hydroalcoholic extract on hypercholesterolemic rabbits was compared with that of lovastatin. Twenty five mature male New Zealand rabbits were randomly divided into five groups of five and were fed for 60 days as follows: Standard diet (GroupI), standard diet and hydroalcoholic extract of Hypericum perforatum (150 mg/kg daily)(GroupII), standard diet, hydroalcoholic extract of Hypericum perforatum (150 mg/ kg daily) and cholesterol (1% of food content) (Group III), standard diet and cholesterol (1% of food content)(GroupIV), and finally standard diet, lovastatin (10 mg/kg), and cholesterol (1% of foodcontent) (GroupV). Hypericum perforatum extract significantly decreased the levels of apolipoprotein B(apoB), apolipoprotein B/apolipoprotein A (apoB/apoA), triglyceride, cholesterol, low density lipoprotein cholesterol, oxidized LDL, malondialdehyde, and C-reactive protein (CRP) as well as atherosclerosis index, and increased high density lipoprotein and apoA in rabbits of Group III compared to the rabbits of Group IV. The effect of Hypericum perforatum extract in decreasing the level of some biochemical factors like apoB, apoB/apoA, and CRP was meaningfully more than that of lovastatin. Histopathological findings confirmed that hydroalcoholic extract of Hypericum perforatum restricted the atherosclerotic lesions. This study indicates that hydroalcoholic extract of Hypericum perforatum possesses hypolipidemic and anti-atherosclerotic effects and could be beneficial in the management of hyperlipidemia and atherosclerosis.
Article
Germination of new seeds (1–6 months old) of Hypericum perforation L. was restricted by high temperatures (16h/8h, 20/30°C), darkness and a chemical inhibitor in exudate from the capsule, whereas germination of old seeds (9 years) was only restricted by the inhibitor. The effect of the chemical inhibitor and high temperatures was overcome, respectively, by washing seeds in water and by reducing temperatures to constant 15°C. Calcium in solution from CaCO3 and from three different soils did not prevent the germination of new or old seeds or of seeds collected from five different locations. There were differences in the germination characteristics and dormancy mechanisms of seeds collected from different localities, Restriction of the emergence of seedlings by a covering of > 2 mm of soil appeared to be due to lack of seedling vigour rather than to lack of light. Seedling growth was much slower than in other pasture species. Thus the requirements for germination of H. perforatum of low temperature and moisture to wash away the chemical inhibitor favour its establishment but the slow growth of its seedling restricts its emergence and renders it extremely susceptible to competition from other plants.
Article
An altered ploidy level was observed in plants regenerated by adventitious shoot formation from seedlings of Hypericum prformatum L. (2n = 4x = 32). Among the somaclones of the Ro generation, the presence of diploids (2n = 2x = 16), triraploids (2n = 3x = 24), tetraploids (2n = 4x = 32) and mixoploids was detected. Cytogenetic analyses of the R1 and R2 progenies showed that the chromosomal instability of the Ro somaclones was transferred onto the next generation. While almost all the seed progeny of diploids (100% in R1 and 94% in R2) progenies showed that the chromosomal instability of the Ro somaclones was transferred onto the next generations. While almost all the seed progeny of diploids (100% in R1 and 94% in R2) and more than 60% of tetraploids (61% in R1 and 73% in R2) retained their chromosome number, cytogenetic diversity was observed in the progeny of triploids, mixoploids and some tetraploids. Somaclones and their offspring were analyzed for hypericin content. Statistical evaluation showed a correlation between hypericin content and ploidy during a two-year cultivation of R0 somaclones and in their R1 and R2 progenies.
Article
A prospective, randomized, multicentre, double-blind placebo controlled study is described which compares the efficacy and tolerability of hypericum administered as a concentrated ethanolic extract of St John's wort (ZE117) to patients with mild–moderate depression (ICD-10; F 32·0 mild; F 32·1 moderate). Patients on active medication received 250 mg extract tablets twice daily, corresponding to 1 mg hypericin daily, for 6 weeks. The primary efficacy variable was the 21 item Hamilton Depression Scale (HAMD); secondary variables were the risk-benefit Clinical Global Impression (CGI) scales I–III and a validated patient self-assessment on a Visual Analogue Scale (VAS). 162 patients entered the trial. 159 patients (80 on active medication) were evaluated in an intention-to-treat analysis; 136 patients (66 on active medication) in a protocol-compliant analysis. Patients in the two treatment groups did not differ with respect to the distribution of age, gender, weight and height. Based on differences in HAMD scores (p<0·001), both the intention-to-treat and protocol-compliant analyses demonstrate that ZE117 is clinically effective in the treatment of patients with mild to moderate depression following 6 weeks' treatment. Using the criteria of ≥50% reduction in HAMD score from baseline and/or an actual HAMD score ≤10 as evidence of a clinically relevant response, 56% patients treated with ZE117 were classified as responders, compared with 15% patients on placebo. The secondary efficacy variables data confirmed these findings. Compliance was high; using electronic devices within the medication containers, a therapeutic coverage of 81·7% was found. This was probably due, in part, to the low number of adverse events reported (11 total, 5 placebo, 6 active), the majority of which were transient, self-limiting and, in the case of active treatment, mostly non-specific gastrointestinal complaints. These results demonstrate that hypericum (ZE117) provides a safe and effective treatment for patients with mild to moderate depression. The good tolerability profile contributes to the high observed compliance, possibly conferring a clinical advantage in achieving efficacy over other antidepressants with less favourable side effect profiles. © 1998 John Wiley & Sons, Ltd.
Article
This study evaluated the wound healing activity of microcurrent application alone or in combination with topical Hypericum perforatum L. and Arnica montana L. on skin surgical incision surgically induced on the back of Wistar rats. The animals were randomly divided into six groups: (1) no intervention (control group); (2) microcurrent application (10 μA/2 min); (3) topical application of gel containing H. perforatum; (4) topical application of H. perforatum gel and microcurrent (10 μA/2 min); (5) topical application of gel containing A. montana; (6) topical application of A. montana gel and microcurrent (10 μA/2 min). Tissue samples were obtained on the 2nd, 6th and 10th days after injury and submitted to structural and morphometric analysis. Differences in wound healing were observed between treatments when compared to the control group. Microcurrent application alone or combined with H. perforatum gel or A. montana gel exerted significant effects on wound healing in this experimental model in all of the study parameters (P<0.05) when compared to the control group with positive effects seen regarding newly formed tissue, number of newly formed blood vessels and percentage of mature collagen fibers. The morphometric data confirmed the structural findings. In conclusion, application of H. perforatum or A. montana was effective on experimental wound healing when compared to control, but significant differences in the parameters studied were only observed when these treatments were combined with microcurrent application.
Article
Accumulating evidence indicates that CYP2C9 ranks amongst the most important drug metabolizing enzymes in humans. Substrates for CYP2C9 include fluoxetine, losartan, phenytoin, tolbutamide, torsemide, S-warfarin, and numerous NSAIDs. CYP2C9 activity in vivo is inducible by rifampicin. Evidence suggests that CYP2C9 substrates may also be induced variably by carbamazepine, ethanol and phenobarbitone. Apart from the mutual competitive inhibition which may occur between alternate substrates, numerous other drugs have been shown to inhibit CYP2C9 activity in vivo and/or in vitro. Clinically significant inhibition may occur with coadministration of amiodarone, fluconazole, phenylbutazone, sulphinpyrazone, sulphaphenazole and certain other sulphonamides. Polymorphisms in the coding region of the CYP2C9 gene produce variants at amino acid residues 144 (Arg144Cys) and 359 (Ile359Leu) of the CYP2C9 protein. Individuals homozygous for Leu359 have markedly diminished metabolic capacities for most CYP2C9 substrates, although the frequency of this allele is relatively low. Consistent with the modulation of enzyme activity by genetic and other factors, wide interindividual variability occurs in the elimination and/or dosage requirements of prototypic CYP2C9 substrates. Individualisation of dose is essential for those CYP2C9 substrates with a narrow therapeutic index.
Article
The composition of essential oils obtained from flowers and leaves in 11 accessions of Hypericum perforatum L. was analysed by GC and GC–MS. All the analysed oils were dominated by their oxygenated sesquiterpene fraction. Differences were attributed to the main components: caryophyllene oxide, spathulenol and viridiflorol. There were only a few monoterpenes in essential oil of all accessions. The data indicated some differences in sesquiterpene and aliphatic hydrocarbons, as well as in oxygenated aliphatics biosynthesis in flowers and leaves. The concentrations of β-caryophyllene and caryophyllene oxide in essential oils from leaves were higher than those from flowers, whereas dodecanol, spathulenol, viridiflorol, carotol and tetradecanol were present in higher quantities in flowers. Cluster analysis of all identified components grouped oils from flowers and from leaves into three clusters that corresponded with their major components: caryophyllene oxide, tetradecanal, tetradecanol and manool. Chemical variability of the analysed accessions seems likely to result from the genetic variability, since the influence of different environmental factors has been eliminated.
Article
17 α-Ethynylestradiol is extensively sulfated but the sulfate is thought to primarily be a storage form of this estrogen. 2-Hydroxylation is clearly the major oxidative reaction, and the 2-hydroxy derivative is further transformed by methylation and glucuronidation prior to urinary and fecal excretion. Alterations in the rate of 2-hydroxylation can have major effects on the pharmacokinetics and effectiveness of 17 α-ethynylestradiol as a contraceptive. The major human catalyst of the 2-hydroxylation reaction is liver microsomal cytochrome P-450 IIIA4. Lesser amounts of this enzyme are found in other tissues such as the intestine and may contribute to overall clearance of the orally administered contraceptive. In individuals with very low amounts of this enzyme other forms of cytochrome P-450 may make some contribution. Levels of cytochrome P-450 IIIA4 vary widely among individuals and can explain the variation in rates of 17 α-ethynylestradiol 2-hydroxylation. The known inducibility of the enzyme by barbiturates and rifampicin explains their effects in enhancing 17 α-ethynylestradiol clearance and reducing the effectiveness of the drug. Mechanism-based inactivation of cytochrome P-450 IIIA4 can be seen with 17 α-ethynylestradiol and other 17 α-acetylenic steroids, and the progestogen gestodene appears to be unusually active in this regard. Other unknown factors may also modulate levels of cytochrome P-450 IIIA4 and its ability to catalyze 17 α-ethynylestradiol 2-hydroxylation.
Article
The antioxidant potentials of a total ethanolic extract of Hypericum perforatum (TE) and fractions were evaluated and correlated with their phenolic contents. The extracts were fully characterised by HPLC–DAD–MS–MS. Kaempferol 3-rutinoside and rutin-acetyl were identified for the first time in TE extracts. The free radical-scavenging properties of TE (EC50=21 μg dwb/ml) and fractions were studied using DPPH. Fractions containing flavonoids and/or caffeoylquinic acids were found to be the main contributors to the free radical-scavenging activity of the TE. Lipid peroxidation, induced with ascorbate/Fe2+, was significantly reduced in the presence of the TE (EC50=26 μg dwb/ml) and fractions containing flavonoids and/or caffeoylquinic acids. The fraction containing flavonoid aglycones was found to be responsible for a major part of the TE protection against lipid peroxidation. Hypericins and hyperforins made no significant contributions to the antioxidant properties of TE. Human consumption of H. perforatum extract or fractions could be beneficial.
Article
The present study was undertaken to investigate the putative activity of a methanol extract of Hypericum montbretti (Guttiferae) on the central nervous system. Rutin (1519 ppm) and quercitrin (784 ppm) were identified as the major phenolic compounds in the extract. When administered at 25, 50 and 100 mg/kg doses, the extract decreased the total number of head-dipping behaviours performed by mice during a hole-board test. Administration of both the extract and diazepam (2 mg/kg) reduced spontaneous locomotory activity, potentiated hexobarbital (60 mg/kg)-induced sleeping parameters and prevented pentylenetetrazole (80 mg/kg)-induced seizures relative to the controls. These findings are the first to indicate the sedative and anticonvulsant activities of H. montbretti extract. Atropine (2 mg/kg) and naloxone (5 mg/kg) pre-treatment did not reverse the sedative effect, indicating that muscarinic and opioidergic mechanisms did not contribute to the pharmacological action. However, pre-treatment with flumazenil (a benzodiazepine receptor antagonist) reversed both the sedative and anticonvulsant effects induced by a 100 mg/kg dose of the extract, indicating the involvement of the GABA(A)-benzodiazepine receptor complex. In conclusion, H. montbretti extract is a novel candidate as a sedative and anticonvulsant drug for the treatment of sleep disorders and for the prevention of epileptic seizures. Copyright © 2012 John Wiley & Sons, Ltd.