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目的:测试石杉碱乙的抗胆碱酯酶作用并与他克林进行比较.方法:比色法用于测定胆碱酯酶活性.结果:石杉碱乙和他克林对BuChE和AChE抑制的IC50值的比率分别为658和054.石杉碱乙对乙酰胆碱酯酶有更强的选择性抑制作用.石杉碱乙灌胃对脑内AChE的抑制作用明显强于他克林.而他克林对BuChE的抑制作用强于石杉碱乙,并有严重副反应.单次灌胃石杉碱乙在4小时内对脑内AChE产生较为稳定的抑制作用.结论:与他克林比较石杉碱乙是乙酰胆碱酯酶的高选择性抑制剂,灌胃时药效高,毒性低.
4. Objective : To test the anticholinesterase effect of huperzine B and compare it with tacrine. Methods: Colorimetry was used to determine cholinesterase activity. RESULTS: The IC50 values for inhibition of BuChE and AChE by huperzine B and tacrine were 658 and 054, respectively. Huperzine B has a stronger selective inhibition effect on acetylcholinesterase. Huperzine B instillation inhibited brain AChE significantly more than tacrine. And tacrine has a stronger inhibitory effect on BuChE than huperzine B and has serious side effects. A single intragastric administration of huperzine B produced a more stable inhibition of brain AChE within 4 hours. Conclusion: Compared with tacrine, huperzine B is a highly selective inhibitor of acetylcholinesterase, high efficacy and low toxicity when gavage.