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五味子醇甲通过改变戊巴比妥钠诱导的小鼠睡眠行为来评价其镇静催眠作用的药理学研究。

Pharmacological evaluation of sedative and hypnotic effects of schizandrin through the modification of pentobarbital-induced sleep behaviors in mice.

机构信息

School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, PR China.

School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang, PR China.

出版信息

Eur J Pharmacol. 2014 Dec 5;744:157-63. doi: 10.1016/j.ejphar.2014.09.012. Epub 2014 Oct 19.

Abstract

The fruits of Schisandra chinensis have been recorded as an effective somnificant for the treatment of insomnia in some oriental countries pharmacopoeias. However, the mechanism of sedative and hypnotic effects of this kind of herb is still unclear. In the present study, schizandrin, which is the main component of Schisandra chinensis, was selected as a target compound to investigate possible mechanisms through behavioral pharmacology methods. The results showed that schizandrin possessed dose-dependent (5-45 mg/kg, i.p.) sedative effects on locomotion activity in normal mice, and produced a dose-dependent decrease in sleep latency and an increase in sleep duration in pentobarbital-treated mice; thus, itself did not induce sleep at higher dose which was used in this experiment (45 mg/kg, i.p.). It also can reverse the rodent models of insomnia induced by p-chlorophenylalanine (PCPA) and caffeine, which could exhibit a syne with 5-hydroxytryptophan (5-HTP) as well; therefore, the hypnotic effects of schizandrin were not inhibited by flumazenil (a specific gamma aminobutyric acid (GABA)-A-BZD receptor antagonist). Altogether, these results indicated that schizandrin produces beneficial sedative and hypnotic bioactivity, which might be mediated by the modification of the serotonergic system.

摘要

五味子的果实已被记录为一些东方国家药典中治疗失眠的有效安眠药。然而,这种草药的镇静和催眠作用的机制仍不清楚。在本研究中,选择五味子醇甲作为目标化合物,通过行为药理学方法研究可能的机制。结果表明,五味子醇甲对正常小鼠的运动活动具有剂量依赖性(5-45mg/kg,ip)的镇静作用,并在戊巴比妥处理的小鼠中产生剂量依赖性的睡眠潜伏期缩短和睡眠时间延长;因此,自身在实验中使用的较高剂量(45mg/kg,ip)下不会引起睡眠。它还可以逆转 p-氯苯丙氨酸(PCPA)和咖啡因诱导的失眠啮齿动物模型,与 5-羟色氨酸(5-HTP)也有协同作用;因此,氟马西尼(一种特定的γ-氨基丁酸(GABA)-A-BZD 受体拮抗剂)不能抑制五味子醇甲的催眠作用。总的来说,这些结果表明,五味子醇甲产生有益的镇静和催眠生物活性,可能是通过对 5-羟色胺能系统的修饰来介导的。

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