合成（-）-石杉碱甲对胆碱酯酶活性及小鼠水迷宫行为的影响。
Effects of synthetic (-)-huperzine A on cholinesterase activities and mouse water maze performance.
作者信息
Liu J, Zhang H Y, Tang X C, Wang B, He X C, Bai D L
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
出版信息
Zhongguo Yao Li Xue Bao. 1998 Sep;19(5):413-6.
AIM
To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance.
METHODS
Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect.
RESULTS
The IC50 of synthetic Hup A for acetylcholinesterase (AChE) of rat cortex and rat erythrocyte membrane determined in vitro were 64.7 (52.6-79.5) and 53.9 (43.6-66.6) nmol.L-1, respectively, and for butyrylcholinesterase of rat serum was 53.6 (44.9-63.8) mumol.L-1. Synthetic Hup A 0.12-0.48 mg.kg-1 ig produced a dose-dependent inhibition of brain AChE in mice. Synthetic Hup A 0.05 mg.kg-1 ig attenuated scopolamine-induced impairment of spatial memory. The efficacy of synthetic Hup A was the same as natural Hup A.
CONCLUSION
Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A.
目的
比较合成型和天然型（-）-石杉碱甲（Hup A）对胆碱酯酶及小鼠水迷宫行为表现的影响。
方法
采用分光光度法测定胆碱酯酶活性。利用小鼠水迷宫评估其益智作用。
结果
体外测定合成型Hup A对大鼠皮层乙酰胆碱酯酶（AChE）和大鼠红细胞膜AChE的IC50分别为64.7（52.6 - 79.5）和53.9（43.6 - 66.6）nmol·L-1，对大鼠血清丁酰胆碱酯酶的IC50为53.6（44.9 - 63.8）μmol·L-1。合成型Hup A 0.12 - 0.48 mg·kg-1灌胃可使小鼠脑AChE产生剂量依赖性抑制。合成型Hup A 0.05 mg·kg-1灌胃可减轻东莨菪碱诱导的空间记忆损伤。合成型Hup A的药效与天然型Hup A相同。
结论
合成型Hup A在体外和体内产生的药理活性与天然型Hup A相似。
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