Brain neurotransmitter receptor binding and nootropic studies on Indian Hypericum perforatum Linn

The high affinity binding sites for serotonin and benzodiazepine in the frontal cortex, for dopamine in the striatum and muscarinic cholinergic receptors in the hippocampus were investigated in the brains of Charles Foster rats treated for 3 days. Transfer latency on elevated plus maze (TL), passive and active avoidance behaviour (PA and AA) and electroconvulsive shock (ECS) induced amnesia were also studied. Pilot studies indicated that single dose administration of Indian Hypericum perforatum (IHp) had little or no acute behavioural effects and hence the extract of IHp was administered orally at two dose levels (100 and 200 mg/kg, p.o.) once daily for 3 consecutive days, while piracetam (500 mg/kg, i.p.), a clinically used nootropic agent, was administered acutely to rats as the standard nootropic agent. Control rats were treated with an equal volume of vehicle (0.3% carboxymethyl cellulose). The results indicate that IHp treatment caused a significant decrease in the binding of [3H] spiroperone (DA-D2 receptor) to the striatum and an increase in the binding of [3H] ketanserin (5-HT2A receptor) and [3H] flunitrazepam (BDZ receptor) to the frontal cortex in rats. Preliminary pharmacological studies with IHp extract indicate the presence of two major behavioural actions, namely, antidepressant and anxiolytic. The present findings tend to elucidate the mechanism of earlier observations, the downregulation of the dopamine D2 receptor being consonant with anxiolytic and the upregulation of 5-HT2A and BDZ receptors being consonant with antidepressant activity. Piracetam when given alone, shortened the TL on days 1, 2 and 9 day and also antagonized the amnesic effects of ECS on the TL significantly, whereas IHp antagonized the amnesia produced by ECS. IHp had no significant effect per se on the retention of the PA in rats but produced a significant reversal of ECS induced PA retention deficit. Piracetam showed a significant facilitatory effect per se on PA retention and also reversed the ECS induced impaired PA retention. In the AA test, piracetam facilitated the acquisition and retention of AA in rats but IHp had no effect per se. Both the doses of IHp and piracetam significantly attenuated the ECS induced impaired retention of AA. These results indicate a possible nootropic action of IHp in amnesic animals, which was comparable qualitatively to piracetam.     

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.     

越鞠胶囊与贯叶连翘抗抑郁作用的对比研究

目的:研究越鞠胶囊、贯叶连翘的抗抑郁作用。方法:采用小鼠悬尾实验、小鼠强迫游泳实验、利血平诱导小鼠体温下降实验和开场实验研究越鞠胶囊、贯叶连翘的抗抑郁作用。结果:在小鼠悬尾实验中,越鞠胶囊大剂量组、贯叶连翘大、中剂量组能明显缩短模型小鼠的不动时间;在小鼠强迫游泳实验中,越鞠胶囊、贯叶连翘各剂量组能明显缩短模型小鼠的不动时间;在利血平诱导的体温下降实验中,越鞠胶囊大剂量组、贯叶连翘大、中剂量组能明显抑制小鼠体温的下降;实验表明贯叶连翘提取物的作用效价强度要大于越鞠胶囊。结论:越鞠胶囊、贯叶连翘有一定的的抗抑郁作用,贯叶连翘提取物的作用效价强度要大于越鞠胶囊。     

贯叶连翘活性成分研究新进展

介绍了贯叶连翘的活性成分,抗抑郁、抗肿瘤、抗病毒等药理作用和副作用的研究新进展。     

贯叶金丝桃的细胞培养

从贯叶金丝桃叶的嫩茎诱导愈伤组织的过程,探讨了悬浮培养和平板培养的方法,以及细胞悬浮培养时间、培养方法和接种密集度对贯叶金丝桃单细胞平板培养植板率的影响。在所实验的ＭＳ、Ｂ５、Ｗｈｉｔｅ３种培养基中,以ＭＳ培养基较好,其中ＭＳ＋２,４－Ｄ１ｍｇ／Ｌ＋ＮＡＡ １ ｍｇ／ｌ培养基愈伤组织诱导率为９２．８６％。细胞悬浮培养以Ｂ５培养基较好。普通单细胞平板培养法培养贯叶金丝桃单细胞的植板率很低,而以悬浮     

不同中药配伍对贯叶连翘中贯叶金丝桃素含量的影响

目的:观察比较不同中药与贯叶连翘配伍后贯叶金丝桃素含量的变化,探讨中药配伍对贯叶金丝桃素稳定性的影响.方法:选择常用抗抑郁中药与贯叶连翘配伍,分别为贯叶连翘组,贯叶连翘+姜黄组,贯叶连翘+郁金组,贯叶连翘桃+淫羊藿组,贯叶连翘+乌灵菌粉(WY)组;采用HPLC法测定贯叶金丝桃素含量.结果:贯叶连翘与姜黄、郁金配伍后,经过提取、浓缩干燥后,贯叶金丝桃素的提取率和保留率均比贯叶连翘组低,而与WY和淫羊藿配伍,提取率未有明显变化;在浓缩干燥过程中,WY组贯叶金丝桃素的保留率高于贯叶连翘组,淫羊藿组明显低贯叶连翘组.结论:实验结果表明中药配伍对中药复方有效成分的稳定性有影响.     

Inhibitory effects of flavonoids from Hypericum perforatum on nitric oxide synthase

The inhibitory effects of six flavonoids from Hypericum perforatum were assessed spectrophotometrically using nitric oxide synthase (NOS) in blood and cerebral homogenate of rats. Of the assayed compounds, quercetin and hyperoside showed concentration-dependent enzyme inhibitory actions. The IC50 values of quercetin for inhibiting NOS in rat cerebral homogenate and blood were 63.06 and 57.54 microM, and those of hyperoside 56.23 and 158.49 microM, respectively. The competitive patterns were discerned with the inhibition of the two flavonoids on NOS in serum and cerebral homogenate (except a mixed type inhibition was observed with quercetin in inhibiting cerebral NOS). Furthermore, similar inhibitions were found for quercetin upon NOS in cerebral homogenate and blood. However, a stronger inhibitory effect of hyperoside on the enzyme was discerned in cerebrum than in blood. These results suggested that the galactose moiety in hyperoside may be associated with the selectivity of the NOS inhibition.     

Development of pregnancy in rats treated with Hypericum perforatum

St John's wort (Hypericum perforatum) is a medicinal plant used in the treatment of depression and other psychiatric disorders. In the present paper, the toxicity of H. perforatum administered to female rats during the period of organogenesis (day 9-15 of pregnancy) was evaluated. Thirty inseminated Wistar rats were randomly distributed into control and treated groups, which received, by gavage, 0.5 mL of saline and 36 mg/kg body weight of Jarsin dried extract diluted into 0.5 mL of saline, respectively. Maternal toxicity was evaluated through: water and food intake, body weight gain, piloerection, locomotor activity, diarrhea and death occurrence. Animals were killed on day 21 of pregnancy, when fetuses and placentas were removed and weighed. The indices of implantation and resorption were calculated. Clinical signs of maternal toxicity were not observed and none of the variables analysed showed statistically significant differences. In the dose administered in the experimental model used, H. perforatum does not seem to be toxic to the mother nor to interfere with the progress of gestation during organogenesis.     

HPLC法测定贯叶连翘中贯叶金丝桃素含量

目的：测定贯叶连翘中贯叶金丝桃素的含量。方法：采用HPLC法,流动相：乙腈－水（140：1,内含1％冰醋酸）,流速：1mL/min,检测波长276nm,结果：该法的平均回收率为98．47％,RSD＝1．33％。结论：方法可用于贯叶金丝桃药材及其制剂 质量控制。     

基于TCMGIS的贯叶连翘生态适宜性研究

目的：分析贯叶连翘的全国适宜产地。方法：以贯叶连翘的主产地湖北板桥镇为基点,运用《中药材产地适宜性分析地理信息系统》（TCMGIS）进行分析。结果：全国共有湖北、重庆、安徽、湖南、四川、陕西、贵州、云南等8个省区的163个县市为贯叶连翘适宜产区,适宜产区面积总和为45773．53km^2。结论：为贯叶连翘引种栽培、合理布局及资源可持续利用提供了依据。     

Anticonvulsant effect of Hypericum perforatum: role of nitric oxide

Hypericum perforatum L. is used in traditional medicine for its anticonvulsant property. We studied the anticonvulsant activity of the aqueous and ethanolic extracts of Hypericum perforatum aerial parts in mice in order to evaluate the traditional use of this plant. The pentylenetetrazole (PTZ) and the maximal electroshock seizure (MES) tests were used for assessing the anticonvulsive effects of this plant. In the PTZ test, the extracts (0.1-1g/kg, i.p.) delayed the onset of tonic convulsions and protected mice against mortality. In the MES test, both extracts did not showed an antiseizure activity. L-NAME (1-10 mg/kg, i.p.), a nitric oxide (NO) synthase inhibitor, reduced the anticonvulsant activity of the extracts. The results of this study indicate that the extracts of Hypericum perforatum aerial parts could contribute to the control of petit mal seizure and this effect may be partially mediated by nitric oxide pathway.     

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。     

Pharmacological activity of three commercial Hypericum perforatum preparations in mice

St John's Wort (Hypericum perforatum) is the main herbal species used to treat depression. The products available on the pharmaceutical and dietary supplement markets are obtained by a variety of preparation processes and their pharmacological effects may differ significantly. The purpose of this study therefore was to investigate the effect of different St John's Wort commercial preparations available on the French market. Only one preparation gave significant results in the forced swimming test.     

大孔吸附树脂纯化贯叶连翘提取物的工艺

目的筛选纯化贯叶连翘提取物的最佳树脂型号及其最佳工艺。方法以金丝桃素为指标,对大孔吸附树脂的类型进行筛选,并采用正交试验,对最佳大孔吸附树脂工艺进行考察。结果最佳大孔吸附树脂为LSA-10,其最佳工艺为比上柱量1.954 2 mg/g;径高比1∶20;药液浓缩比1∶1,药液上样体积流量2 BV/h,分别以4 BV蒸馏水、3 BV 20%乙醇、8 BV 70%乙醇为洗脱剂洗脱,贯叶连翘提取物中的金丝桃素量提高到1.5%以上。结论该工艺合理、稳定,纯化效果好。     

Hepatoprotective activity of Hypericum perforatum L. alcoholic extract in rodents

In recent years, interest in the hepatoprotective plants and plant based chemicals is increasing. In Turkish folk medicine, Hypericum perforatum L. has been used for various purposes including liver protection. The hepatoprotective effect of H. perforatum was investigated in vivo by cannulating the rat bile duct for choleretic activity and by barbiturate sleeping time following CCI₄-induced hepatic injury. The increase in the bile secretion following intraduodenal injection of H. perforatum extract, and the appearance of its constituents in the bile were observed by its colour change and this observation was confirmed by thin layer chromatographic analysis suggesting the excretion of hypericin into the bile as well. It was observed that the extract shortens the barbiturate sleeping time of CCI₄-treated mice suggesting hepatoprotection.     

金丝桃属植物的HPLC指纹谱研究

目的 建立金丝桃属植物的HPLC指纹谱，对该属植物中所含的化学成分进行综合评价并为该属植物鉴定提供依据。方法 采用HPLC方法将获得的色谱数据转化为色谱指纹谱，据此对样品进行分折鉴别。结果 不同种金丝桃均显示了它们各自的指纹特征。结论HPLC指纹谱可以用来鉴别金丝桃属的不同种植物，该属植物种间的化学成分有较高的相似性，但各相应的成分含量差异显著。     

贯叶连翘提取物中金丝桃苷含量的RP-HPLC法测定

目的 建立测定贯叶连翘提取物中金丝桃苷含量的高效液相色谱法.方法 采用Agilent ZORBAX SB-C18(250 mm×4.6 mm,5μm)色谱柱,以乙腈-0.1％磷酸溶液(15∶ 85)为流动相,流速1.2 ml/min,检测波长256 nm;柱温为35C.结果 金丝桃苷检测浓度在11.4 ～91.2 μg/ml范围内与峰面积积分值呈良好的线性关系(r=0.999 9);平均回收率为100.7％,RSD为1.37％.结论 该法快速、简便、准确,重复性好,可用于贯叶连翘提取物中金丝桃苷的含量测定.     

贯叶连翘提取物中金丝桃苷的分析鉴别与稳定性研究

目的探讨贯叶连翘提取物中金丝桃苷鉴别方法和稳定性。方法对贯叶连翘提取物进行化学、薄层、紫外鉴别。通过加速实验从不同影响因素分析贯叶连翘提取物中金丝桃苷的稳定性。结果贯叶连翘提取物的盐酸-镁粉反应显阳性,薄层色谱斑点清晰,紫外光谱在363 nm处有最大吸收峰。贯叶连翘提取物在酸、碱、热、湿、光、氧化、加速实验等条件下金丝桃苷的含量均有不同程度的损失。结论3种鉴别方法能很好地鉴别出黄酮苷类(金丝桃苷)的存在,定性方法简便、准确、专属性强。鉴于金丝桃苷的稳定性,在对贯叶连翘进行贮存时,应密闭、闭光、置阴凉干燥处保存。     

光、赤霉素和乙烯利对贯叶连翘种子萌发的影响

目的 研究光，赤霉素和乙烯利对贯叶连翘Hypericum perforatum种子萌发的影响，为贯叶连翘的人工栽培提供理论依据。方法 直接发芽法，结果 贯叶连翘种子光下萌发率达79%，而暗中不萌发，赤霉素和乙烯利不仅能促进种子光下萌发，而且能诱导种子暗萌发，但乙烯利处理对幼苗胚根生长有明显的抑制作用。结论 贯叶连翘种子为需光种子，其需光性与赤霉素和乙烯利有关。     

贯叶连翘挥发性成分分析

目的：测定贯叶连翘叶挥发油成分。方法：用连续蒸馏萃取挥发油提取仪提取（水蒸汽蒸馏,乙酸乙酯萃取）,然后采用ＧＣ－ＭＳ分析,结合计算机检索技术对其挥发油化学成分进行分离鉴定,应用色谱峰面积归一法测定各成分的相对百分含量。结果：分离、鉴定了５４种成分,占挥发油总量的９２．３２％。结论：化学成分多为倍半萜类物质,与国外报道贯叶连翘叶挥发油的成分相差很大。