Effects of single intraperitoneal injections of an extract of Ginkgo biloba (EGb 761) and its terpene trilactone constituents on barbital-induced narcosis in the mouse

Effects of single intraperitoneal injections of an extract of Ginkgo biloba (EGb 761) and its terpene trilactone constituents on barbital-induced narcosis in the mouse
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DOI:
10.1016/s0306-3623(99)00018-x
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发表时间:
1999-09-01
期刊:
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM
影响因子:
--
通讯作者:
Drieu, K
Drieu, K
中科院分区:
其他
文献类型:
--
作者:
Brochet, D;Chermat, R;Drieu, K

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采用巴比妥钠诱导的小鼠麻醉模型,观察了单次腹腔注射银杏叶提取物(EGB761)、不含银杏内酯的提取物(CP205)和银杏内酯中的三种萜三内酯成分(银杏内酯A和银杏内酯B)的作用。给小鼠注射巴比妥钠(180 mg/kg,IF)会引起麻醉,测量为翻正反射的丧失。单次注射银杏叶提取物761(25 mg/kg和50 mg/kg)可显著缩短巴比妥钠诱导的睡眠时间,而相同剂量的CP205则无效。单次注射银杏内酯B(1 mg/kg)和白果内酯(2 mg/kg和5 mg/kg)可显著缩短小鼠的睡眠时间,而银杏内酯A无效。银杏内酯B和白果内酯的作用反映为开始睡眠的潜伏期延长,而银杏内酯761、银杏内酯B和白果内酯的作用与小鼠睡眠数量的减少相关。在行为水平上,EGb 761、银杏内酯B和白果内酯的这些体内有效作用类似于某些抗抑郁药物。在分子水平上,推测可能与GABA调节的中枢神经系统Cl-通道的苦参素/TBPT位点相互作用。这一信息似乎有助于解释临床上观察到的银杏叶提取物761的“提高警觉性”和“抗抑郁药样”作用。(C)1999 Elsevier Science Inc.保留所有权利。
A mouse model of barbital-induced narcosis was used to examine the effects of single intraperitoneal injections of an extract of Ginkgo biloba (EGb 761), an extract devoid of terpene trilactones (CP 205), and three terpene trilactone constituents of the extract (ginkgolides A and B, bilobalide). Administration of sodium barbital (180 mg/kg, IF) to the mice caused narcosis, measured as a loss in righting reflex. Single injections of EGb 761 (25 and 50 mg/kg), given 60 min prior to sodium barbital, significantly shortened barbital-induced sleeping time, whereas these same doses of CP 205 were ineffective. Single injections of ginkgolide B (1 mg/kg) and bilobalide (2 and 5 mg/kg) significantly shortened sleeping time, whereas ginkgolide A was ineffective. The effects of ginkgolide B and bilobalide were reflected as increases in latency to onset of sleep and those of EGb 761, ginkgolide B, and bilobalide were correlated with decreases in the number of mice that slept. At the behavioral level, these potent in vivo effects of EGb 761, ginkgolide B, and bilobalide resemble those of certain antidepressants. At the molecular level, it is hypothesized that interactions with the picrotoxinin/TBPT site of GABA-regulated Cl- channels of the CNS may be involved. This information appears useful in explaining the clinically observed "vigilance-enhancing" and "antidepressant-like" actions of EGb 761. (C) 1999 Elsevier Science Inc. All rights reserved.