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The isolation and identification of a new phloroglucinol derivative (2), a diterpenol (4), together with the known compounds flavesone (1) and sarothralen B (3), from the aerial parts of Hypericum japonicum are reported. Their structures were established by extensive spectral analysis and the structure of (3) has also been confirmed by a single crystal X-ray determination.
The present study investigated the possible involvement of sigma receptors and of serotonergic mechanisms in the effects of Hypericum perforatum extract (HPE) on immobility time in the forced swimming test (FST) and on ethanol intake in Marchigian Sardinian alcohol-preferring rats. The HPE employed was a dry extract containing 0.3% hypericin and 3.8% hyperforin. Intraperitoneal pretreatment with 20 mg/kg of the sigma receptor antagonist rimcazole (RIM), 30 min prior to HPE, completely suppressed the antiimmobility effect of HPE (3 intragastric injections of 250 mg/kg). Intracerebroventricular pretreatment with 5, 7-dihydroxytryptamine (5,7-DHT), which produced a marked depletion of brain serotonin, reduced the antiimmobility effect, although this reduction was not as pronounced as that of RIM. On the other hand, the inhibitory effect of HPE on 10% ethanol intake was modified neither by 5,7-DHT nor by RIM pretreatment. These results suggest that the antidepressant-like effect of HPE in the FST may be mediated by interaction with sigma receptors and to some extent by increased serotonergic neurotransmission. On the other hand, these mechanisms appear to be unimportant for the effect of HPE on ethanol intake.
The study investigates the effects of acute and chronic oral treatment with Hypericum perforatum L. (HP LI 160, 62.5-500 mg/kg) in rats submitted to different anxiety models: the elevated T-maze (for inhibitory avoidance and escape measurements), the light/dark transition, and the cat odor test. These models were selected for their presumed capacity of evidencing specific subtypes of anxiety disorders as recognized in clinical practice. The results showed that acute HP (125 mg/kg) impaired elevated T-maze inhibitory avoidance, an anxiolytic effect, without altering escape performance. Chronic HP (250 mg/kg) enhanced avoidance latencies only in animals that were preexposed to the open arms of the maze. Preexposure shortens escape latency, improving it as an escape index. Differently from the reference drug imipramine (IMP, 15 mg/kg), chronic HP did not impair escape from the open arms of the maze. On the other hand, similarly to IMP, the extract increased the number of transitions between the two compartments in the light/dark transition model. Treatment regimens with HP and IMP did not alter behavioral responses of rats to a cloth impregnated with cat odor. These observations suggest that HP LI 160 exerts anxiolytic-like effects in a specific subset of defensive behaviors, particularly those related to generalized anxiety.
Since (a) Hypericum perforatum shows anxiolytic-like effect in some animal models, (b) antidepressant drugs (AD) have been used as the main drug treatment for panic disorder (PD), (c) AD are also effective in generalized anxiety disorder (GAD), and (d) H. perforatum exhibits antidepressant activity, it was hypothesized that H. perforatum might possess an antipanic-like and/or anxiolytic-like effect. Previous studies with the mouse defense test battery (MDTB) have suggested that this model may be useful for the investigation of anxiolytic-like and antipanic-like compounds. Thus, the aim of the present study was to evaluate the effect of H. perforatum extract in the MDTB. The effect of acute, subchronic (7 days), and chronic (21 days) H. perforatum (150 and 300 mg/kg) extract administration was evaluated in mice submitted to the MDTB. Paroxetine (5 mg/kg), a selective serotonin re-uptake inhibitor with anxiolytic and antipanic effect, was used as a positive control. The results showed that 21 days of repeated administration of H. perforatum 300 mg/kg and paroxetine 5 mg/kg reduced flight reactions (number of avoidances, avoidance distance, and overall flight speed) to the presence of the predator. While the effect of paroxetine confirms that MDTB is useful for the detection of antipanic-like drugs, the effect of H. perforatum suggests a putative antipanic-like effect for this extract. Moreover, after 21 days of repeated administration, paroxetine increased the number of approaches/withdrawals and reduced the number of upright postures, suggesting a partial anxiolytic-like effect, while H. perforatum only reduced the number of upright postures. The present results suggest anxiolytic-like and antipanic-like effects of H. perforatum extract. However, it should be emphasized that the risk assessment (the main index of anxiety) was not affected by the extract, while the attack reactions were only weakly modified.
Clinical trials have extensively reported the ability of Hypericum perforatum extracts to exert a significant antidepressant activity. Hypericin, the main constituent of H. perforatum extract, is no more regarded as the active principle of the antidepressant activity of the drug. Hence, the question of which constituents are involved in the basic activity of the total extract, is still waiting for an answer. In the present study we focused our attention on the potential anxiolytic activity of H. perforatum total extract, and of some pure components such as protohypericin and a fraction containing hypericin and pseudohypericin. Herein we report that the total extract of H. perforatum increases the locomotor activity in the open field and exerts anxiolytic activity in the light-dark test, whereas the single components did not show any effect. Interestingly, the anxiolytic activity of the total extract was blocked by pretreatment of rats with the benzodiazepine antagonist Flumazenil, hence suggesting an implication of benzodiazepine receptor activation in the anxiolytic effect of H. perforatum extract. Electrophysiological studies, performed to gain more information on the mechanism of action, showed that hypericin reduced the GABA-activated chloride currents, while pseudohypericin did an opposite effect. Furthermore, both hypericin and pseudohypericin inhibited the activation of NMDA receptors.
St. John's Wort (Hypericum perforatum; H. perforatum) is a popular herbal supplement used to treat mild to moderate depression. H. perforatum possesses serotonergic properties such as inhibition of serotonin (5-hydroxytryptamine; 5-HT) reuptake. Serotonergic pharmacotherapy is associated with amelioration of depression as well as increases in natural killer (NK) cell activity (NKCA). Also, 5-HT and 5-HT analogs augment NKCA in vitro. Considering the serotonergic properties of H. perforatum, the effects of H. perforatum on NKCA were assessed in vitro. Mononuclear cells (MNCs) from normal donors were exposed in vitro to an extract of H. perforatum (LI160s) or established 5-HT stimulators of NKCA. After an overnight incubation, cells were washed and a standard 51Cr-release cytotoxicity assay performed to assess NKCA. LI160s at all concentrations failed to augment NKCA. However, in corroboration of previous studies, 5-HT, the selective serotonin reuptake inhibitors (SSRIs), paroxetine and norfluoxetine, and alpha-interferon augmented NKCA above control levels. Though an efficacious treatment for mild to moderate depression, H. perforatum differs from commonly prescribed serotonergic antidepressants insofar as H. perforatum fails to enhance NKCA in vitro. Therefore, the present results are consistent with pharmacologic studies indicating that H. perforatum possesses, at best, weak serotonergic activity.
The medicinal plant Hypericum perforatum Linn, commonly known as St. John's wort, has been used as an antidepressant. To investigate whether St. John's wort possesses a protective effect against hydrogen peroxide (H(2)O(2))-induced cytotoxicity in neuronal cells, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, 4,6-diamidino-2-phenylindole staining, terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling assay, flow cytometry analysis, DNA fragmentation assay, and caspase-3 enzyme assay were performed on SK-N-MC human neuroblastoma cells. Cells treated with H(2)O(2) exhibited several apoptotic features, while those pre-treated with St. John's wort prior to H(2)O(2) exposure showed a decreased occurrence of apoptotic features. In addition, pre-treatment with St. John's wort inhibited H(2)O(2)-induced increase in caspase-3 enzyme activity. These results suggest that St. John's wort may exert a protective effect against H(2)O(2)-induced apoptosis in human neuroblastoma cells.
The antimicrobial activity of the n-hexane (H) and chloroform (C) extracts, the methanol extract (M) and its ethyl acetate (E) and n-butanol (B) fractions, and six isolated constituents of the aerial parts of Hypericum hircinum was investigated using an agar diffusion method. The maximum activity was exhibited by the methanolic extract against Staphylococcus aureus, while all pure constituents showed no antimicrobial activity against the tested microorganisms.
In the present study, extracts of 34 species and varieties of the genus Hypericum were screened for activity against a clinical isolate of methicillin-resistant Staphylococcus aureus, which in addition possessed a multidrug efflux mechanism conferring a high level of resistance to therapeutically useful antibiotics. Thirty-three of the 34 chloroform extracts showed significant activity in a disk diffusion assay, and five extracts had minimum inhibitory concentrations of 64 microg/ml, indicating that this genus has great potential to yield compounds with potent activity against multidrug-resistant bacteria.
The antioxidant activity of the methanol extract of Hypericum triquetrifolium Turra (Hypericaceae) aerial part and of flavonoids isolated therein, I3,II8-biapigenin, quercetin-3-O-galactoside, kaempferol-3-O-glycoside, (-)-epicatechin and hypericin, was evaluated. The IC(50) resulted between 0.062 and 1 mg/ml.
The volatile fraction of Hypericum coris aerial parts, consisting mainly of alpha-curcumene was screened for activity against five microbial strains. The maximum activity was against Saccharomyces cerevisiae.
Repeated examination of the aerial parts of Hypericum perforatum yielded a new degradation product of hyperforin (1) namely deoxyfurohyperforin A (2), together with the previously identified furohyperforin (3), furoadhyperforin (4), furohyperforin A (5a and 5b), pyrano[7,28-b]hyperforin (6) and 3-methyl-4,6-di(3-methyl-2-butenyl)-2-(2-methyl-1-oxopropyl)-3-(4-methyl-3-pentenyl)-cyclohexanone (7). The antimicrobial activity of the compounds 3, 5a and 5b, 6 and 7 was tested against Staphylococcus aureus, Candida albicans, Bacillus subtilis and Escherichia coli.
The effect of a standardised 50% ethanolic extract of Indian Hypericum perforatum (IHp) was investigated for its putative nootropic activity on various experimental paradigms of learning and memory, viz. transfer latency (TL) on elevated plus-maze, passive avoidance (PA), active avoidance (AA), scopolamine and sodium nitrite induced amnesia (SIA & NIA) in albino rats. Pilot studies indicated that single dose administration of IHp had little or no acute behavioural effects, hence the extract of IHp was administered orally at two dose levels (100 and 200 mg/kg, p.o.), once in daily for three consecutive days, while piracetam (500/kg, i.p.), a clinically used nootropic agent, was administered acutely to rats as the standard drug. Control rats were treated with equal volume of vehicle (0.3% carboxymethyl cellulose (CMC)). IHp and piracetam when given alone shortened the TL on day 1, 2, 9 and also antagonised the amnesic effects of scopolamine and sodium nitrite on the TL significantly. IHp had no significant per se effect on the retention of the PA in rats. Only the higher dose (200 mg/kg, p.o.) produced a significant reversal of scopolamine induced PA retention deficit but no significant reversal was observed with sodium nitrite. Piracetam showed significant per se facilitatory effect on PA retention and also reversed the scopolamine and sodium nitrite induced impaired PA retention. In the AA test, IHp in both the doses, and piracetam, facilitated the acquisition and retention of AA in rats and the IHp effects were found to be dose dependent. Both the doses of IHp and piracetam significantly attenuated the scopolamine and sodium nitrite induced impaired retention of AA. These results indicate a possible nootropic action of IHp, which was qualitatively comparable with that induced by piracetam.
The aim of the present study was to explore the probable antiinflammatory effect of Hypericum triquetrifolium Turra. in a rat model of carrageenan induced inflammation. Male Wistar rats were treated intraperitoneally with 0.4% dimethylsulphoxide (DMSO) (as control group) and H. triquetrifolium extract (25, 50, 60 mg/kg), 30 min before 0.1 ml 1% carrageenan injection. Paw volume was measured before and 1, 2, 3, 4, 5 and 6 h after the injection of carrageenan. The results are expressed as the mean+/-s.e. mean and the statistical significance of differences between groups was analyzed by One Way Analysis of Variance (ANOVA). The intraplantar injection of carrageenan caused a time-dependent paw edema in the rat although saline injection caused no swelling. Intraperitoneal administration of H. triquetrifolium extract (25, 50, 60 mg/kg) inhibited paw swelling dose-dependently at 2, 3, 4, 5 and 6 h after carrageenan injection (P<0.05). We can conclude that H. triquetrifolium extract may exert an antiinflammatory effect in rats.
Dried methanol extract of Hypericum hyssopifolium subsp. elongatum var. elongatum was dissolved in distilled water, and then fractioned by re-extracting with petroleum ether, chloroform, and ethyl acetate, subsequently. Antioxidant and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activities of these fractions were determined, in vitro. The amounts of total phenolic compounds were also determined. None of these fractions showed antioxidant activity, in contrast water and ethyl acetate fractions acted as prooxidant. However, the ethyl acetate fraction exhibited the highest DPPH radical-scavenging activity and the amount of its total phenolic compound was highest, too. Therefore, ethyl acetate fraction was subjected to further separation by chromatographic methods. Thus, five flavonoids (I3,II8-biapigenin, quercetin, quercetin-3-O-alpha-L-arabinofuranoside, quercetin-3-O-beta-D-galactopyranoside, quercetin-3-O-beta-D-galactopyranoside-7-O-beta-D-glucopyranoside) and a napthodianthrone (hypericin) were isolated, and their structures were determined by UV, IR, NMR, and MS spectroscopic methods. All isolated compounds showed antioxidant and DPPH radical-scavenging activities. Although, I3,II8-biapigenin and hypericin were able to show highest antioxidant activity, they had the lowest DPPH radical-scavenging activities. From these results, it can be suggested that these compounds may be used as potential antioxidants. In addition, the petroleum ether fraction was subjected to silica gel column chromatography (CC). Then, n-dotriacontanyl hexadecanoate, bis(2-methylheptyl) phthalate, and beta-sitosterol were isolated from it. It is of interest to present the spectral data of bis(2-methylheptyl) phthalate first time in the present study.
The aim of the present study was to investigate the antinociceptive activity of Hypericum triquetrifolium Turra. extract. The lyophilized extract was administered to male Swiss mice. Formalin paw test and tail flick tests were used for the evaluation of the antinociceptive activity. Plant extract (10, 25, 50 and 60 mg kg(-1), i.p.) (n = 16-24 for each group) or vehicle (n = 27) was administered 30 min before the subplantar formalin injection. In the tail flick test, mice were examined for latency to withdraw their tails from a noxious thermal stimulus using a tail flick meter (n = 8 for each group). The effects of the extract on sensorimotor performance was also assessed (n = 16-24 for each group). The extract caused a significant dose-related inhibition of the first phase (50, 60 mg kg(-1), i.p.) and second phase (10, 25, 50 and 60 mg kg(-1), i.p.) of formalin induced hindpaw licking. Additionally, the extract administration (50, 60 mg kg(-1), i.p.) increased the tail flick latencies. No significant change was observed in any of the treatment groups in the sensorimotor performance test. The observed antinociceptive activity of the extract may be due to its noradrenaline and serotonin reuptake blocking activity. Moreover, the probable antiinflammatory activity of the extract may play a role in the dose-related inhibition of the second phase of formalin paw test.
The methanol extract of Hypericum patulum Thumb. leaves were investigated for the evaluation of their wound healing potential on different experimental models of wounds in rats. The methanol extract of leaves (HPM), in the form of an ointment with two different concentrations (5% and 10% w/w ointment of leaf extract in simple ointment base) was evaluated for wound healing potential in an excision wound model and an incision wound model in rats. Both concentrations of the methanol extract ointment showed significant responses in both the wound types tested when compared with the control group. The effect produced by the extract ointment, in terms of wound contracting ability, wound closure time, regeneration of tissues at wound site, tensile strength of the wound and histopathological characteristics were comparable to those of a standard drug nitrofurazone ointment.
Metals have been investigated in different plant materials in order to establish their normal concentration range and consider their role in plants as part of human medicinal treatment. Metal monitoring as a pattern recognition method is a promising tool in the characterization and/or standardization of phytomedicines. In the present work measurable amounts of Ca, Cu, K, Li, Mg, Mn, Na, Ni, and Zn were detected in phytopharmaceutical derivatives of Hypericum perforatum by atomic techniques. Atomic methodologies like flame atomic absorption spectrometry (FAAS) and electrothermal atomic absorption spectrometry (ETAAS) allow reliable determination of mineral content in pharmaceutical quality control of medicinal plants. Additionally, capillary electrophoresis (CE) patterns of characteristic components (fingerprints) have been performed for the search of adulterants in phytopharmaceutical products.