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.     

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.     

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.     

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.     

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。     

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 activity of some Hypericum reflexum L. fil. extracts in the forced swimming test in mice

We previously reported that oral administration of the methanol extract obtained from the aerial part in blossom of Hypericum reflexum L. fil. was active in the tetrabenazine and forced swimming test. In the present study, the effect of the aqueous, butanol and chloroform fractions obtained from the methanol extract of this species on the central nervous system was investigated in mice, particularly in animal models of depression. Antidepressant activity was detected in the butanol and chloroform fractions of this species using the forced swimming test since both fractions induced a significant reduction of the immobility time, producing no effects or only a slight depression on spontaneous motor activity when assessed in a photocell activity meter. Moreover, these fractions did not alter significantly the pentobarbital-induced sleeping time. On the other hand, the chloroform fraction produced a slight but significant hypothermia and was also effective in antagonizing the ptosis induced by tetrabenazine. Furthermore, the butanol fraction produced a slight potentiation of the head twitches and syndrome induced by 5-HTP. Taken together, these data indicate that the butanol and chloroform fractions from Hypericum reflexum 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.     

Studies on psychopharmacological effects of Cleome viscosa Linn. extract in rats and mice

Methanol extract of the entire plant Cleome viscosa Linn. (CVME) was evaluated for different psychopharmacological actions such as general behaviour, exploratory behaviour, muscle relaxant activity and phenobarbitone induced sleeping time and effects on normal body temperature in rats and mice. The extract was found to cause reduction in spontaneous activity, decrease in exploratory behavioural pattern by the head dip and Y-maze test, reduction in the muscle relaxant by rotarod, 30 degrees inclined screen and traction tests and caused significant lowering of body temperature. In addition, CVME significantly potentiated the phenobarbitone-induced sleeping time. Preliminary tests indicate that the methanol extract of Cleome viscosa Linn. in doses of 200-400 mg/kg has significant psychopharmacological activity.     

Effect of Hypericum perforatum on marble-burying by mice

The effect of Hypericum perforatum extract (LI 160) at a dose that exerts an antidepressive-like effect was studied in mice in the marble-burying test. Acute Hypericum perforatum (150, 300 and 500 mg/kg, p.o.) reduced immobility time in the forced swimming test. The number of marbles buried, but not locomotor activity, was reduced by acute treatment with Hypericum perforatum (150 and 300 mg/kg, p.o.). However, this effect was not seen after chronic treatment (21 days) with Hypericum perforatum (300 mg/kg, p.o.). Thus, Hypericum perforatum extract, at antidepressant dose, exerts an acute anxiolytic drug effect on the marble-burying test, which could indicate a potential anti-obsessive effect, although the development of tolerance could be an important drawback.     

越鞠丸提取物YJ-XCC1Z3抗抑郁作用研究

目的：观察越鞠丸提取物YJ-XCC1Z3用于抑郁症的实验治疗效果。方法：YJ-XCC1Z3分高、低剂量405,135 mg·kg^-1分别给予小鼠灌胃。采用自主活动测定仪,观测YJ-XCC1Z3对小鼠自主活动的影响；采用2种行为绝望模型小鼠悬尾试验和小鼠强迫游泳试验,观察YJ-XCC1Z3对小鼠不动时间的影响；采用利血平拮抗实验,观测YJ-XCC1Z3对小鼠体温及脑内单胺类神经递质代谢的作用；采用5-羟色胺酸(5-HTP)诱导小鼠甩头增强试验,观测YJ-XCC1Z3对小鼠甩头次数的影响。结果：YJ-XCC1Z3组小鼠的自主活动与对照组比较没有显著差异；YJ-XCC1Z3 405 mg·kg^-1能明显缩短小鼠强迫游泳不动时间与小鼠悬尾不动时间；YJ-XCC1Z3 405,135 mg·kg^-1均可显著拮抗利血平所致的小鼠体温下降；YJ-XCC1Z3 405 mg·kg^-1组可明显增加5-HTP诱导小鼠甩头总次数；YJ-XCC1Z3 405 ,135 mg·kg^-1均使5-羟色胺(5-HT)、去甲肾上腺素(NE)的含量增加,YJ-XCC1Z3 405 mg·kg^-1组可使多巴胺含量减少；YJ-XCC1Z3 135 mg·kg^-1使5-羟基吲哚乙酸(5-HIAA)含量增加,对高香草酸(HVA)和3,4-二羟基苯乙酸(DOPAC)的含量无影响；YJ-XCC1Z3 405, 135 mg·kg^-1均使5-HIAA／5-HT比值减少。结论：YJ-XCC1Z3可以改善小鼠抑郁状态的行为,具有一定的抗抑郁作用,并无精神运动兴奋作用。YJ-XCC1Z3可通过增加脑内5-HT, NE的含量而发挥抗抑郁作用,其中对5-HT的影响与YJ-XCC1Z3降低脑内5-HT的代谢有关。     

桂枝解郁方不同工艺抗抑郁作用的比较

目的:比较桂枝解郁方不同工艺的抗抑郁作用。方法:本实验将小鼠随机分成4组,即桂枝解郁方-A组、桂枝解郁方-B组(分别ig给予桂枝解郁液-A和桂枝解郁液-B 12.66 g.kg-1,每天1次,连续给药10 d)、盐酸阿米替林组(实验前3 dig给予盐酸阿米替林50 mg.kg-1,每天1次)、空白对照组(给予等体积的生理盐水)。采用小鼠强迫游泳实验、悬尾实验、自主活动实验和利血平拮抗实验,以小鼠不动时间、自主活动数和体温下降值为指标来评价桂枝解郁方不同工艺抗抑郁的作用。结果:在强迫游泳实验和悬尾实验中,桂枝解郁方-A能明显缩短小鼠的不动时间(P<0.05);在自主活动实验中,各组小鼠之间无显著性差异。利血平拮抗实验中,桂枝解郁方-A在4h能显著拮抗利血平诱发的小鼠体温降低(P<0.05)。结论:桂枝解郁方-A的抗抑郁作用优于桂枝解郁方B。     

Central nervous system activity of yangambin from Ocotea duckei Vattimo (Lauraceae) in mice

This work presents behavioral effects of yangambin isolated from the leaves of Ocotea duckei on open field, rota rod, barbiturate sleeping time, forced swimming and elevated plus maze test in mice. Yangambin was intraperitoneally administered to male mice at single doses of 12.5, 25 and 50 mg/kg. The results showed that yangambin in the doses of 25 and 50 mg/kg decreased the locomotor activity and the number of rearing. However, no change was observed in the rota rod test between the yangambin groups as compared to the control group. Reduction on the sleep latency and a prolongation of the sleeping time induced by pentobarbital was observed only with the yangambin dose of 50 mg/kg. In the forced swimming test, yangambin (25 and 50 mg/kg) increased the immobility time. Yangambin, in the doses of 25 and 50 mg/kg, decreased the number of entries and the time of permanence in the open arms of the elevated plus maze test. However, this effect can not be related to anxiogenic effects, but to a decrease in locomotor activity. The results showed that yangambin presents a depressant activity in the open field, forced swimming and pentobarbital sleeping time tests. These effects probably were not due to peripheral neuromuscular blockade, since there was no alteration on the rota rod test. Also, no anxiolytic effect was observed after the treatment with yangambin.     

Effects of Hypericum calycinum L. Extract on the Central Nervous System in Mice

Hypericum species have been used as herbal remedies for the therapy of various neurological disorders. In the present study, the effects of Hypericum calycinum on the central nervous system were investigated using various behavioural models including swimming time, locomotor activity, tail-flick and hole-board experiments. According to the results obtained, it was found that the extract prepared from H. calycinum is as effective as the antidepressant drugs, desipramine and trimipramine, which were used for comparison with this plant extract in animal models.     

Studies on Some Psychopharmacological Actions of Moringa oleifera Lam. (Moringaceae) Leaf Extract

The methanol extract of the leaves of Moringa oleifera Lam. was investigated for some psychopharmacological actions in animals. The extract was found to produce a significant alteration in general behavioural pattern by head dip test, Y-maze test, evasion test, and reduction in muscle relaxant activity by rotarod test, chimney test and traction test. Beside these, the extract also potentiated pentobarbitone induced sleeping time and lowered body temperature in experimental animals.     

贯郁胶囊治疗抑郁症的实验研究

目的:观察贯郁胶囊的抗抑郁作用。方法:小鼠悬尾、小鼠强迫游泳及利血平拮抗实验。结果:贯郁胶囊1. 2g kg、0. 6g kg均可显著缩短小鼠悬尾及强迫游泳不动时间(P <0 . 0 1,P <0. 0 5 ) ,并且均可显著对抗利血平所致的小鼠体温下降、眼睑下垂及运动不能(P <0. 0 1,P <0. 0 5 )。结论:贯郁胶囊具有明显的抗抑郁作用。     

藜欢解郁方中抗抑郁成分的不同提取方法比较

目的:优选藜欢解郁方中抗抑郁成分的提取方法.方法:采用水提法、醇提法、水提加醇提法提取藜欢解郁方中抗抑郁有效物质,运用小鼠强迫游泳试验、敞箱试验、拮抗利血平所致体温降低试验优选提取方法.结果:在小鼠强迫游泳试验中,藜欢解郁方水提物组与模型组比较能明显缩短小鼠不动时间,表现出抗抑郁作用.拮抗利血平所致体温降低试验中,水提物组与模型组比较有显著性差异,敞箱试验表明各组间小鼠自主活动无显著性差异.结论:水提法为藜欢解郁方藜欢解郁方抗抑郁的最佳提取方法.     

Neuropharmacological actions of Portulaca oleraceae L v. sativa (Hawk)

Portulaca oleracea L v. sativa (family: Portulacaceae) is a warm-climate annual, cultivated in the Arabian peninsula and used traditionally for alleviating pain and swelling. It was observed that a 10% ethanolic extract of this plant produced restriction of movement in animals during the routine screening studies. Therefore the effects of the extract on the locomotor activity, threshold to noxious stimulus, anti-convulsant activity and relaxant effects on the skeletal muscle were studied. The extract, on intraperitoneal administration, showed a significant reduction in the locomotor activity in mice, anti-nociceptive activity in rats using Tail Flick Method, an increase in the onset time of pentylenetetrazole-induced convulsions in mice and muscle relaxant activity in in vitro (rat hemidiaphragm) and in vivo (grip strength) experiments. The anti-nociceptive activity of the extract in rats was attenuated by naloxone pre-treatment indicating the involvement of opioid receptors in its anti-nociceptive effects. It is indicated from the results of the present study that P. oleracea v. sativa possesses varied effects on both the central and peripheral nervous system and the plant should be exhaustively studied for other neuropharmacological effects.     

Muscle relaxant activity of Elaeagnus angustifolia L. fruit seeds in mice

Muscle relaxant effect of Elaeagnus angustifolia L. (Elaeagnaceae) fruit seeds was studied in mice using traction test. The aqueous and ethanolic extracts (i.p) induced a muscle relaxant effect in a dose dependent manner as effective as diazepam (1 mg/kg). The aqueous extract was partitioned with methanol-chloroform (MeCh) and n-butanol (Bu.) saturated with water. The MeCh and Bu. fractions did not show activity. Preliminary phytochemical tests showed that the extract contains flavonoid. The results suggested that E. angustifolia fruit seeds exerted muscle relaxant activity via flavonoid component(s).     

Quercetin as the active principle of Hypericum hircinum exerts a selective inhibitory activity against MAO-A: extraction, biological analysis, and computational study

The methanol extract from Hypericum hircinum leaves exhibited in vitro inhibition of monoamine oxidases (MAO). Bioassay-guided fractionation led to the isolation of quercetin and five compounds identified for the first time from H. hircinum. Quercetin was the only compound with a selective inhibitory activity against MAO-A, with an IC50 value of 0.010 microM. To explain MAO selective inhibition at the molecular level, a computational study was carried out by conformational search and docking techniques using recently determined crystallographic models of both enzymatic isoforms. An in vivo study in mice was carried out using the forced swimming test in order to elucidate the behavioral effects of quercetin.