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目的:比较合成和天然左旋石杉碱甲(HupA)对胆碱酯酶的抑制作用以及对东莨菪碱所致记忆障碍的改善作用.方法:比色法用于测定胆碱酯酶活性,小鼠水迷宫用于评价促智作用.结果:合成HupA抑制大鼠皮层和红细胞膜乙酰胆碱酯酶的IC50值分别为647(526-795),539(436-666)nmol·L-1,抑制大鼠血清丁酰胆碱酯酶的IC50为536(449-638)μmol·L-1.灌服合成HupA(012-048mg·kg-1),量效依赖性抑制小鼠体内的胆碱酯酶.行为实验证明,合成HupA(005mg·kg-1)明显地改善东莨菪碱所致的记忆损害.合成HupA具有与天然HupA相等的效力.结论:合成HupA与天然HupA具有相似的药理活性.
AIM: To compare the inhibition of cholinesterase by synthetic and natural LH-A and the improvement of scopolamine-induced memory impairment. Methods: The colorimetric method was used to determine the activity of cholinesterase, and the mouse water maze was used to evaluate the effect of nourishing the brain. Results: IC50 values of synthetic HupA in rat cortex and erythrocyte membrane acetylcholinesterase were 647 (526-795) and 539 (436-666) nmol·L-1, respectively. The IC50 of inhibiting rat serum butyrylcholinesterase was 536 (449-638) μmol·L-1. HupA (0.12-048 mg · kg-1) was administered orally in a dose-dependent manner to inhibit cholinesterase in mice. Behavioral experiments show that the synthetic HupA (0 05mg · kg-1) significantly improved scopolamine-induced memory impairment. Synthetic HupA has the same potency as native HupA. Conclusion: The synthetic HupA has similar pharmacological activities as native HupA.