Antidepressant properties of some Hypericum canariense L. and Hypericum glandulosum Ait. extracts in the forced swimming test in mice

It has been shown in a previous work that the methanol extract obtained from the aerial part in blossom of Hypericum canariense L. and Hypericum glandulosum Ait. was active in the tetrabenazine and forced swimming test. In the present study, the central nervous effect of the aqueous, butanol and chloroform fractions obtained from the methanol extracts of these Hypericum species was investigated in mice, particularly in animal models of depression. It was found that the immobility time in the forced swimming test was significantly reduced by the butanol and chloroform fraction of both species assayed, producing no effects or only a slight depression on spontaneous motor activity when assessed in a photocell activity meter. In this regard, the efficacy of the chloroform extract from Hypericum glandulosum Ait. (500 mg/kg p.o.) in the forced swimming test was comparable to that of the tricyclic antidepressant imipramine (50 mg/kg p.o.). In addition, the Hypericum glandulosum chloroform fraction was also effective in antagonizing the ptosis induced by tetrabenazine. Moreover, Hypericum canariense butanol fraction and Hypericum glandulosum chloroform fraction produced a slight but significant hypothermia. Taken together, these data demonstrate that the butanol and chloroform fractions from Hypericum canariense and Hypericum glandulosum possess antidepressant-like effects in mice, providing further support for the traditional use of these plants in the Canary Islands folk medicine against central nervous disorders.     

Hypericum grandifolium Choisy: A species native to Macaronesian Region with antidepressant effect

Aim of the study

Various species of Hypericum genus have been used in the Canary Islands as sedative, diuretic, vermifuge, wound healing, antihysteric and antidepressant agent. Studies have shown that methanol extract of Hypericum grandifolium Choisy is active in tetrabenazine-induced ptosis and forced swimming tests. In the current study, the aqueous, butanol and chloroform fractions obtained from the methanol extract as well as three sub-fractions derived from the chloroform fraction were evaluated for their central nervous effects in mice, particularly their antidepressant activity.

Materials and methods

The central nervous effect of different fractions and sub-fractions of Hypericum grandifolium was evaluated in mice using various behavioural models including locomotor and muscle relaxant activity, forced swimming test, effect on normal body temperature, barbiturate-induced sleep, tetrabenazine-induced syndrome and 5-hydroxytryptohan-induced head twitches and syndrome.

Results

We found that the butanol and chloroform fractions and all sub-fractions showed an antidepressant effect in the forced swimming test, the chloroform fraction being the most active. They produced no effects or only a slight depression of locomotor activity. Chloroform fraction significantly increased the pentobarbital-induced sleeping time, produced a slight but significant hypothermia and antagonized tetrabenazine-induced ptosis, whereas the butanol fraction produced a slight potentiation of 5-HTP-induced head twitches and syndrome.

Conclusions

The present results, together with previous pharmacological and phytochemical data, indicated that Hypericum grandifolium possess antidepressant-like effects in mice and that different constituents, such as the flavonoids and the benzophenone derivatives, could be responsible at least in part for the antidepressant effects observed for this species.     

Evaluation of the central properties of several Hypericum species from the Canary Islands

The infusions of the aerial parts in blossom of Hypericum canariense, H. glandulosum, H. reflexum and H. grandifolium (Hypericaceae) were evaluated for their pharmacological activity on the central nervous system in mice using various behavioural models including locomotor and muscle relaxant activity, effect on normal body temperature, pentobarbital-induced sleep, oxotremorine and tetrabenazine-induced syndrome, apomorphine-induced hypothermia and 5-hydroxytryptophan-induced head twitches, as well as a forced swimming test. These infusions did not alter significantly the locomotor activity, pentobarbital induced sleeping time and body temperature, with the exception of H. canariense which produced a slight but significant hypothermia. Additionally, no muscle relaxant or anticholinergic activity were observed. These infusions antagonized the ptosis and/or motor depression induced by tetrabenazine as well as shortening the immobility time in the forced swimming test. The observations suggest that the infusions of these Hypericum species possess antidepressant activity in mice, without inducing muscle relaxation, anticholinergic and sedative properties.     

Antidepressant effects of the methanol extract of several Hypericum species from the Canary Islands.

The aim of the present study was to investigate several neuropharmacological effects of the methanol extract of the aerial parts in blossom of Hypericum canariense, H. glandulosum, H. grandifolium and H. reflexum (Hypericaceae). These extracts did not alter significantly the locomotor activity, body temperature or the pentobarbital-induced sleeping time, with the exception of H. reflexum which significantly potentiated pentobarbital-induced sleeping time at both doses assayed (500 and 1000 mg/kg p.o.). Additionally, neither muscle relaxant nor anticholinergic activity was observed. These extracts antagonized the ptosis and/or motor depression induced by tetrabenazine and also shortened the immobility time in the forced swimming test. Moreover, the H. glandulosum and H. grandifolium extracts at 1000 mg/kg p.o. potentiated the head twitches induced by 5-HTP. These observations suggest that the methanol extract of the Hypericum species in doses of 500-1000 mg/kg p.o. possess antidepressant activity in mice, without inducing significant muscle relaxation, anticholinergic and sedative properties.     

Evaluation of the analgesic and topical anti-inflammatory effects of Hypericum reflexum L. fil

The present study investigates the analgesic and topical anti-inflammatory effects of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum reflexum L. fil. in mice. The acetic acid-induced writhing test, formalin test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of all extracts tested from this species significantly inhibit acetic acid-induced writhing in mice. Only the methanol extract and chloroform fraction were significantly active in both phases of formalin-induced pain and in the tail flick assays, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of methanol extract, butanol and chloroform fractions of this species significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.     

Analgesic and topical anti-inflammatory activity of Hypericum canariense L. and Hypericum glandulosum Ait

The present study investigates the analgesic and topical anti-inflammatory activities of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum canariense L. and Hypericum glandulosum Ait. in mice. The acetic acid-induced writhing test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of methanol extracts, and the aqueous, butanol and chloroform fractions of both species and the infusions of Hypericum glandulosum significantly inhibit acetic acid-induced writhing in mice. Only the infusion, methanol extract and butanol and chloroform fractions of Hypericum glandulosum were significantly active in the tail flick assay, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of all extracts tested from both species, with the exception of the infusions and the Hypericum canariense aqueous fraction, significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.     

Antimicrobial studies on three species of Hypericum from the Canary Islands

The antimicrobial activity of several extracts and fractions of the aerial parts of Hypericum canariense, Hypericum glandulosum and Hypericum grandifolium was investigated using the disc diffusion and broth microdilution methods against twelve reference microorganisms (eight bacterial and four fungal strains). The methanol extract and chloroform fraction of H. canariense, as well as the methanol extracts, butanol and chloroform fractions of both H. glandulosum and H. grandifolium exhibited a good antibacterial activity against four Gram-positive bacteria (Bacillus cereus var. mycoides, Micrococcus luteus, Staphylococcus aureus and Staphylococcus epidermidis) and the Gram-negative bacterium Bordetella bronchiseptica with the diameters of growth inhibition area in the range 10-25 mm and MICs values between 0.03 and 0.29 mg/ml. Neither the infusions and aqueous fractions of the species studied nor the butanol fraction of H. canariense showed any antibacterial activity against the tested microorganisms. Amongst the active extracts, the minimum inhibitory concentration (MIC) determination showed that the H. canariense chloroform fraction was the most active against M. luteus, S. aureus and S. epidermidis. No antifungal activity was seen with any of the extracts or fractions tested. The results of this study support the use of these species in Canarian traditional medicine to treat skin infections.     

Antihepatotoxic activity of Swertia chirata on carbon tetrachloride induced hepatotoxicity in rats

The methanol extract of Swertia chirata was evaluated for antihepatotoxic activity against carbon tetrachloride induced liver toxicity in experimental rats. The extract was found to be active and on fractionation into butanol soluble and chloroform soluble fractions, the activity was traced and found more profound in the chloroform soluble fraction. The butanol soluble bitter rich fraction showed marginal activity. The results based on biochemical estimations have been expressed statistically and are additionally supported by histopathological examination of the liver of experimental rats and pentobarbitone induced sleep time studies in mice.     

Effects of Gentiana lutea ssp. symphyandra on the central nervous system in mice

A methanolic extact of Gentiana lutea ssp. symphyandra roots has been investigated for its possible effects on the central nervous system of mice. At doses of 250 and 500 mg/kg (i.p.), the methanol extract of Gentiana roots caused a significant increase in the swimming endurance test and exhibited slight analgesic activity, but no lethality in mice suggesting some activity on the central nervous system. However, there was no indication of sedation or muscular fatigue at the doses employed. HPLC analysis showed that three secoiridoid compounds, gentiopicroside, swertiamarine and sweroside were present and may have been responsible for the CNS effects of the methanol extract of Gentiana lutea ssp. symphyandra roots.     

Sedative activity in mice of a hydroalcohol extract of Hypericum perforatum L.

The sedative activity of a hydroalcohol extract of Hypericum perforatum L. (Hypericaceae) and some of its isolated constituents was evaluated in mice. A dry hydroalcohol extract, orally administered at 26.5 mg/kg, induced a marked sedation as measured by two different tests (actimeter and sleep potentiation), compared with controls (diazepam, 2 mg/kg, per os). Several fractions were isolated from this hydroalcohol extract: hypericin, flavones, butanol fraction, aqueous fraction; a separation and purification method was developed for hypericin. None of the isolated fractions exhibited the same sedative activity as the hydroalcohol extract. © 1997 John Wiley & Sons, Ltd.     

Anxiolytic effects of fractions obtained from Passiflora incarnata L. in the elevated plus maze in mice

The purpose of this study was to characterize the putative anxiolytic-like activity of fractions prepared from a hydroethanol extract of Passiflora incarnata L. using the elevated plus-maze (EPM) in mice. The fractions were prepared as published recently, yielding a butanol, petroleum ether and chloroform fraction. From the tested fractions, the butanol fraction showed significant increases in the number of open arm entries in the EPM in concentrations of 2.1 mg/kg and 4.2 mg/kg corresponding to 150 and 300 mg/kg of the original extract. The highest activity was found for the chloroform fraction in doses of 0.17 mg/kg (10.0 ± 1.9, p < 0.001) and 0.34 mg/kg (6.6 ± 0.86; p < 0.05) which corresponds to a total extract dose of 150 and 300 mg/kg, respectively. Interestingly, the petroleum ether fraction did not show any effects in the elevated plus maze. A sedative or stimulatory effect of each of the fractions could be excluded, since none of the compounds had an influence on the total distance that the animals covered during the observation period. The results suggest that the active principle of passion flower seems to be in the chloroform fraction and to a lower extent in the butanol fraction.     

Anti-diarrhoea and analgesic activities of the methanol extract and its fractions of Jasminum amplexicaule Buch.-Ham. (Oleaceae)

Jasminum amplexicaule Buch.-Ham. (Oleaceae) has been commonly used in the traditional medicine in dysentery, diarrhoea and bellyache in China. In the present work, the methanol extract of Jasminum amplexicaule and different fractions of this extract were studied for anti-diarrhoea and analgesic activities. The anti-diarrhoea activities were investigated using castor oil-induced, magnesium sulphate-induced diarrhoea models, antienteropooling assay and gastrointestinal motility models in mice. The analgesic activities were studied using hot-plate, writhing and formalin models in mice. At the doses of 100, 200 and 400mg/kg, the methanol extract (ME) showed significant and dose-dependent anti-diarrhoea and analgesic activity in these models. The chloroform fraction (CHF), ethyl acetate fraction (EAF) and the residual methanol fraction (RMF) exhibited similar activity using a dose of 200mg/kg in these models. The pharmacological activities of the n-butanol fraction (BUF) were lesser than the ME extract and other fractions. These results may support the fact that this plant is traditionally used to cure diarrhoea and pain.     

Screening for the antidepressant activity of some species of Hypericum from South Brazil

The crude methanol extracts of three species of the genus Hypericum (H. brasiliense, H. caprifoliatum and H. myrianthum) native to South Brazil were evaluated for the antidepressant activity according to the forced swimming test, a classical animal model for antidepressant drug screening. Among the species studied, only H. caprifoliatum showed activity. Thus, this plant was fractionated with solvents in increasing polarity (petroleum ether; petroleum ether: chloroform (1:1); chloroform and methanol). The petroleum ether fraction was the only one which demonstrated antidepressant activity at a dose of 270 mg/kg/day (i.p.). The chemical analyses showed that this fraction is rich in phenolic compounds, mainly of the phloroglucinol type.     

三种贯叶连翘组药用植物醇提物对小鼠的抗抑郁作用

目的：对贯叶连翘组药用植物的抗抑郁作用进行研究，为筛选新的药用品种以及对其品质评价提供药效学依据。方法：采用小鼠尾悬挂试验，小鼠强迫游泳试验抑郁模型对三种贯叶连翘组药用植物醇提物的抗抑郁作用进行研究。结果：在小鼠尾悬挂试验，小鼠强迫游泳试验中，元宝草和扬子小连翘醇提物物与贯叶连翘一样，可以对抗小鼠的失望行为，使实验动物的绝望时间（不动时间）缩短，具有抗抑郁作用，但是贯叶连翘醇提物的抗抑郁作用明显强于扬子小连翘。结论：三种川产贯叶连翘组药用植物醇提物在行为绝望动物模型上有明显的抗抑郁作用。     

Antidepressant-like effect of Lafoensia pacari A. St.-Hil. ethanolic extract and fractions in mice

Ethnopharmacological relevance

Lafoensia pacari A. St.-Hil. (Lythraceae) has been referred in Brazilian traditional medicine for the treatment of different diseases, among them depression. Nevertheless, there are not studies about this possible effect on the central nervous system (CNS).

Aim of the study

To evaluate the antidepressant-like effects of the ethanolic extract of Lafoensia pacari (PEtExt) and its fractions on the performance of male mice.

Materials and methods

Antidepressant activity was studied using forced swimming (FST) and tail suspension (TST) tests, and motor activity in the open-field test. The ethanolic extract of Lafoensia pacari (PEtExt) were administered acutely (1.0 g/kg, p.o.), for 21 days (100, 300 mg, and 1.0 g/(kg day), p.o.), three administration in a 24-h period (1.0 g/kg, p.o.), and the fractions for 21 days. Imipramine (15 mg/(kg day), p.o.) was used as the control positive.

Results

The PEtExt significantly reduced immobility time in FST and TST, without affecting the motor activity. Only the chloroformic fraction (50 mg/(kg day), p.o.) increase the latency to immobility and decrease the immobility time in the FST.

Conclusions

These data indicate that the extract of Lafoensia pacari A. St.-Hil. possesses antidepressant-like properties in mice.     

Antihepatotoxic activity of Swertia chirata on paracetamol and galactosamine induced hepatotoxicity in rats

The extracts of Swertia chirata were evaluated for antihepatotoxic activity using paracetamol and galactosamine models. The methanol extract of the whole plant was found active at a dose of 100 mg/kg i.p. On fractionating this extract into chloroform soluble and butanol soluble fractions, the activity was retained in the chloroform soluble fraction which was most active at a dose level of 25 mg/kg i.p. with overall protection of 81% and 78% against paracetamol and galactosamine, respectively. The butanol soluble fraction, rich in bitter secoiridoids, was devoid of significant activity. The protective effect observed against these two hepatotoxins which are different in their mechanisms of inducing hepatotoxicity, suggests broader and non-specific protection of the liver against these two toxins by non-bitter components of Swertia chirata.     

高度富集黄酮类成分的贯叶连翘提取物抗抑郁作用

目的探讨贯叶连翘提取物中高度富集的黄酮类成分的抗抑郁作用。方法采用小鼠强迫游泳实验、小鼠悬尾实验、开野实验和拮抗利血平所致的体温降低实验,分别以小鼠不动时间、自主活动数和体温下降值作为评价指标。结果在强迫游泳和悬尾实验中,40,80,160,240mg/kg剂量组贯叶连翘提取物均能显著缩短小鼠不动时间,20mg/kg剂量组无显著性差异;开野实验结果表明给药后小鼠的自主活动不同程度地减少;在利血平拮抗实验中,30,60,120mg/kg剂量组在3h,4h和5h各时间点体温下降值与模型对照组相比有显著性差异,240和480mg/kg两剂量组在各测定时间点体温下降值与模型对照组相比均有显著性差异。结论高度富集总黄酮的贯叶连翘提取物(弃除贯叶金丝桃素)有抗抑郁作用。     

温郁金抗抑郁活性部位的筛选

目的:筛选温郁金抗抑郁活性部位。方法:选用小鼠行为绝望模型评价温郁金醇提取物及其不同极性部位的抗抑郁作用。结果:温郁金醇提取物及其4个不同极性部位均不同程度地缩短绝望模型中小鼠悬尾和强迫游泳的不动时间。其中以温郁金醇提取物(P<0.01)、石油醚部位(P<0.001)和乙酸乙酯部位(P<0.01)最为显著。结论:温郁金具有抗抑郁作用,活性成分主要分布在石油醚和乙酸乙酯部位。     

Anticonvulsive activity of Albizzia lebbeck, Hibiscus rosa sinesis and Butea monosperma in experimental animals

The ethanolic extracts of leaves of Albizzia lebbeck and flowers of Hibiscus rosa sinesis and the petroleum ether extract of flowers of Butea monosperma exhibited anticonvulsant activity. The bioassay guided fractionation indicated that the anticonvulsant activity lies in the methanolic fraction of chloroform soluble part of ethanolic extract of the leaves of A. lebbeck, acetone soluble part of ethanolic extract of H. rosa sinesis flowers and acetone soluble part of petroleum ether extract of B. monosperma flowers. The fractions protected animals from maximum electro shock, electrical kindling and pentylenetetrazole-induced convulsions in mice. The fractions also inhibited convulsions induced by lithium-pilocarpine and electrical kindling. However, they failed to protect animals from strychnine-induced convulsions. The fractions antagonised the behavioral effects of D-amphetamine and potentiated the pentobarbitone-induced sleep. The fractions raised brain contents of gamma-aminobutyric acid (GABA) and serotonin. These fractions were found to be anxiogenic and general depressant of central nervous system.     

Appraisal of antinociceptive and anti-inflammatory potential of extract and fractions from the leaves of Torreya grandis Fort Ex. Lindl

Torreya grandis (Taxaceae) was studied for antinociceptive and anti-inflammatory effects. Leaves were extracted with 80% ethanol at 80 °C for 3 h and fractionated with petroleum ether, chloroform, ethylacetate and n-butanol. The aqueous ethanolic extract (aq.EE), ethylacetate fraction (EaF) and butanol fraction (BtF) at the doses of (100 and 200 mg/kg, i.g.) body weight were used for study. Evaluation of antinociceptive activity was carried out by acetic acid-induced writhing response and formalin-induced paw licking time in the first and second phases of mice. The paw edema induced by formalin- and xylene-induced ear edema were used to assess anti-inflammatory activity. It was found that Torreya grandis extract and fractions at the doses of (100 and 200 mg/kg, i.g.) were significantly attenuated the writhing responses induced by acetic acid and second phase of pain response induced by subplantar injection of formalin in mice. In addition, these extract and fractions inhibiting the formaldehyde-induced arthritis as well as xylene-induces edema prolifically. From acute oral toxicity studies no mortality was pragmatic even at highest dose (2500 mg/kg, i.g.). Furthermore, our phytochemical studies indicated that the aq. ethanolic extract of leaves contains alkaloids, flavonoids, tannins, terpenoids and saponins. The results provide justification for the folkloric uses of Torreya grandis in the treatment of analgesic and inflammatory-based diseases across the China.