Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University, 26-21 Kongneung-dong, Nowon-gu, Seoul, 139-742, Republic of Korea.
J Nat Med. 2013 Oct;67(4):814-21. doi: 10.1007/s11418-013-0754-3. Epub 2013 Mar 3.
The present study seeks to evaluate the sedative and anxiolytic effects of the 70% ethanol extract of Sinomeni Caulis et Rhizoma (SR). The extract was orally administered to mice at dosages of 25, 50, 100, 200 or 400 mg/kg. The mice were then subjected to an array of behavioral tests to assess the sedative (open-field, rota-rod, and thiopental sodium-induced sleeping test) and anxiolytic (elevated plus maze test) effects of the substance. SR (100, 200 mg/kg) significantly reduced locomotor activity, decreased rota-rod performance, and potentiated thiopental sodium-induced sleeping in mice, all indicative of its sedative effects. SR (50, 100 mg/kg) also produced anxiolytic effects, as shown by an increase in entries and staying time on the open arm of the plus maze. SR's sedative and anxiolytic effects were comparable to that of the benzodiazepine, diazepam. Moreover, to identify SR's probable mechanism of action, intracellular Cl⁻ ion influx was observed in cultured human neuroblastoma cells. SR dose-dependently increased Cl⁻ influx, which was blocked by co-administration of the GABAA receptor competitive antagonist, bicuculline. Among the major constituents of SR, only magnoflorine showed a similar increment in Cl⁻ influx, which was also blocked by bicuculline. Altogether, the present results suggest that SR has sedative and anxiolytic effects, probably mediated by magnoflorine through a GABAergic mechanism of action.
本研究旨在评估青藤碱（Sinomeni Caulis et Rhizoma，SR） 70%乙醇提取物的镇静和抗焦虑作用。将提取物以 25、50、100、200 或 400mg/kg 的剂量口服给予小鼠，然后对其进行一系列行为测试，以评估该物质的镇静（旷场、转棒和戊巴比妥钠诱导睡眠测试）和抗焦虑（高架十字迷宫测试）作用。SR（100、200mg/kg）显著减少了小鼠的运动活性，降低了转棒性能，并增强了戊巴比妥钠诱导的睡眠，所有这些都表明了其镇静作用。SR（50、100mg/kg）还产生了抗焦虑作用，表现为在加迷宫的开放臂上的进入次数和停留时间增加。SR 的镇静和抗焦虑作用与苯二氮䓬类药物地西泮相当。此外，为了确定 SR 的可能作用机制，在培养的人神经母细胞瘤细胞中观察到细胞内 Cl⁻离子内流。SR 呈剂量依赖性地增加 Cl⁻内流，这一作用被 GABAA 受体竞争性拮抗剂，荷包牡丹碱所阻断。在 SR 的主要成分中，只有石蒜碱表现出类似的 Cl⁻内流增加，这也被荷包牡丹碱所阻断。总之，本研究结果表明，SR 具有镇静和抗焦虑作用，可能通过石蒜碱通过 GABA 能作用机制介导。
