| 石杉碱乙的抗胆碱酯酶作用 |
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| 引用本文： | 刘静 唐希灿. 石杉碱乙的抗胆碱酯酶作用[J]. 中国药理学报, 1999, 20(2): 141-145 |
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| 作者姓名： | 刘静 唐希灿 |
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| 摘 要： | 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６５．８和０．５４，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的抑制作用明业强于他克林，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产生较对稳定的抑制作用，
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| 关 键 词： | 石杉碱乙 胆碱酯酶抑制剂 |
Inhibitory effects of huperzine B on cholinesterase activity in mice. |
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| J Liu,H Y Zhang,L M Wang,X C Tang. Inhibitory effects of huperzine B on cholinesterase activity in mice.[J]. Acta Pharmacologica Sinica, 1999, 20(2): 141-145 |
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| Authors: | J Liu H Y Zhang L M Wang X C Tang |
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| Affiliation: | State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China. |
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| Abstract: | AIM: To determine the anticholinesterase properties of huperzine B (Hup B) and compare with tacrine in vitro and in vivo. METHODS: Spectrophotometry was used to determine ChE activity. RESULTS: Hup B showed much more selective inhibition to acetylcholinesterase (AChE) than tacrine. The IC50 ratios of Hup B and tacrine for butyrylcholinesterase (BuChE): AChE were 65.8 and 0.54, respectively. Hup B ig exhibited higher efficacy on the inhibition of brain AChE than that of tacrine. Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. A single ig dose of Hup B produced steady state of AChE inhibition in 4 h. CONCLUSION: Hup B exhibits higher selectivity and efficacy in the inhibition of AChE, and lower toxicity in mice than tacrine. |
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