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从北美山梗菜叶中分离出的一种新型中枢活性化合物β-香树脂醇棕榈酸酯的药理特性。

Pharmacological properties of beta-amyrin palmitate, a novel centrally acting compound, isolated from Lobelia inflata leaves.

作者信息

Subarnas A, Tadano T, Oshima Y, Kisara K, Ohizumi Y

机构信息

Department of Pharmaceutical Molecular Biology, Tohoku University, Sendai, Japan.

出版信息

J Pharm Pharmacol. 1993 Jun;45(6):545-50. doi: 10.1111/j.2042-7158.1993.tb05596.x.

Abstract

Effects of beta-amyrin palmitate isolated from the leaves of Lobelia inflata were studied on the central nervous system of mice and were compared with those of antidepressant drugs, mianserin and imipramine. In the forced swimming test, beta-amyrin palmitate, like mianserin and imipramine, reduced the duration of immobility of mice significantly in a dose-dependent manner (5, 10 and 20 mg kg-1). beta-Amyrin palmitate (5, 10 and 20 mg kg-1) or mianserin (5, 10 and 20 mg kg-1) elicited a dose-related reduction in locomotor activity of mice and antagonized locomotor stimulation induced by methamphetamine. In contrast, imipramine (5, 10 and 20 mg kg-1) increased locomotor activity and potentiated methamphetamine-induced hyperactivity. beta-Amyrin palmitate showed no effect on reserpine-induced hypothermia, whilst mianserin (10 mg kg-1) and imipramine (10 and 20 mg kg-1) antagonized the reserpine-induced effect. Unlike imipramine, beta-amyrin palmitate and mianserin did not affect haloperidol-induced catalepsy, tetrabenazine-induced ptosis and apomorphine-induced stereotypy. beta-Amyrin palmitate and imipramine had no effects on the head-twitch response induced by 5-hydroxytryptophan, whereas mianserin (5, 10 and 20 mg kg-1) decreased it in a dose-dependent manner. A potentiating effect of beta-amyrin palmitate (5, 10 and 20 mg kg-1) on narcosis induced by sodium pentobarbitone was stronger than that of imipramine (10, 20 and 40 mg kg-1) but weaker than that of mianserin (2.5, 5 and 10 mg kg-1). These results suggest that beta-amyrin palmitate has similar properties in some respects to mianserin and might possess a sedative action.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究了从北美山梗菜叶片中分离出的β-香树脂醇棕榈酸酯对小鼠中枢神经系统的作用,并与抗抑郁药米安色林和丙咪嗪进行了比较。在强迫游泳试验中,β-香树脂醇棕榈酸酯与米安色林和丙咪嗪一样,能显著降低小鼠不动时间,且呈剂量依赖性(5、10和20mg/kg)。β-香树脂醇棕榈酸酯(5、10和20mg/kg)或米安色林(5、10和20mg/kg)能引起小鼠运动活动的剂量相关减少,并拮抗甲基苯丙胺诱导的运动兴奋。相比之下,丙咪嗪(5、10和20mg/kg)增加运动活动并增强甲基苯丙胺诱导的多动。β-香树脂醇棕榈酸酯对利血平诱导的体温过低无影响,而米安色林(10mg/kg)和丙咪嗪(10和20mg/kg)拮抗利血平诱导的效应。与丙咪嗪不同,β-香树脂醇棕榈酸酯和米安色林不影响氟哌啶醇诱导的僵住症、丁苯那嗪诱导的眼睑下垂和阿扑吗啡诱导的刻板行为。β-香树脂醇棕榈酸酯和丙咪嗪对5-羟色氨酸诱导的头部抽搐反应无影响,而米安色林(5、10和20mg/kg)呈剂量依赖性降低该反应。β-香树脂醇棕榈酸酯(5、10和20mg/kg)对戊巴比妥钠诱导的麻醉的增强作用强于丙咪嗪(10、20和40mg/kg),但弱于米安色林(2.5、5和10mg/kg)。这些结果表明,β-香树脂醇棕榈酸酯在某些方面与米安色林具有相似特性,可能具有镇静作用。(摘要截短至250字)

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