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干燥阿拉伯艾蒿的酒精提取物对体外[~3H]地西泮和大鼠大脑皮质细胞膜结合产生抑制作用,两种化合物被分离纯化,其化学结构为毛地黄黄酮和玄参黄酮(IC_(50)分别为1.3±s0.1和22.7±S2.5μmol·L~1),两种化合物在体外还能抑制[~3H]哌唑嗪和大鼠脑皮质细胞膜结合,但不能改变[~3H]蝇蕈碱乙酰胆碱受体,[~3H]蝇蕈醇,[~3H]SCH 23390和[~3H]螺哌隆和膜的结合,Scatchard plot分析提示两种化合物对[~3H]地西泮和膜结合的抑制作用是通过竟争性和非竞争性混合机理而实现的。
The alcohol extracts of the dried Artemisia annua L. inhibited the binding of [~ 3H] diazepam and rat cerebral cortex cell membrane in vitro. The two compounds were isolated and purified. The chemical structure of the extracts was luteolin and Radix Astragali (IC 50 ) Were 1.3 ± s0.1 and 22.7 ± S2.5μmol·L ~ 1, respectively. Both compounds could inhibit the binding of [~ 3H] prazosin and the rat cerebral cortex membrane in vitro, but could not change [~ 3H] Muscarinic acetylcholine receptors, binding of [~ 3H] muscimol, [~ 3H] SCH 23390 and [~ 3H] spiperone to membranes. Scatchard plot analysis suggested that the combination of [~ 3H] diazepam and Inhibition of membrane binding is achieved through a competitive and noncompetitive mixing mechanism.