Liu J, Zhang H Y, Tang X C, Wang B, He X C, Bai D L
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1998 Sep;19(5):413-6.
To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance.
Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect.
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.
Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A.
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。
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。
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。
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。
