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芥子碱对大鼠脑匀浆和血清中乙酰胆碱酯酶的抑制作用
引用本文:何玲,李海涛,郭胜伟,刘丽芳,邱嘉斌,李富,蔡宝昌.芥子碱对大鼠脑匀浆和血清中乙酰胆碱酯酶的抑制作用[J].中国中药杂志,2008,33(7):813-815.
作者姓名:何玲  李海涛  郭胜伟  刘丽芳  邱嘉斌  李富  蔡宝昌
作者单位:何玲 (南京中医药大学,博士后科研流动站,江苏,南京,210029中国药科大学,江苏,南京,210009); 李海涛 (南京中医药大学,博士后科研流动站,江苏,南京,210029); 郭胜伟 (南京中医药大学,博士后科研流动站,江苏,南京,210029); 刘丽芳 (中国药科大学,江苏,南京,210009); 邱嘉斌 (中国药科大学,江苏,南京,210009); 李富 (中国药科大学,江苏,南京,210009); 蔡宝昌 (南京中医药大学,博士后科研流动站,江苏,南京,210029);
基金项目:中国博士后科学基金面上项目,江苏省博士后科学基金,江苏省药效研究平台项目
摘    要:目的:考察中药单体芥子碱(3,5-二甲基,4-羟基苯丙烯酰胆碱,sinapine)对大鼠血清和大鼠大脑匀浆乙酰胆碱酯酶(acetylcholinesterase,AChE)的体外抑制作用。方法:大鼠眼球取血后断头,取大脑,匀浆,用双缩脲法测定脑组织匀浆总蛋白含量。采用乙酰胆碱脂酶试剂盒和改良Ellman比色法测定AChE的活力,检测芥子碱对大鼠血清和脑匀浆乙酰胆碱酯酶的抑制作用。结果:芥子碱明显抑制大鼠大脑匀浆AChE的活力,而对血浆AChE活性的抑制相对较弱,对脑匀浆和血清AChE的抑制IC50分别为3.66和22.1μmol.L-1,IC50血清/IC50脑=6.042(倍)。结论:芥子碱能显著抑制脑组织AChE活性,有可能作为中枢乙酰胆碱酯酶抑制剂(acholinesterase inhibi-tors,AChEIs)具有防治阿尔茨海默病(Alzheimer's disease,AD)的应用前景。

关 键 词:芥子碱  乙酰胆碱酯酶  胆碱酯酶抑制剂  阿尔茨海默病
收稿时间:2007/10/11 0:00:00

Inhibitory effects of sinapine on activity of acetylcholinesterase in cerebral homogenate and blood serum of rats
HE Ling ; LI Hai-tao ;GUO Sheng-wei ;LIU Li-fang ;QIU Jia-bin ;LI Fu ;CAI Bao-chang.Inhibitory effects of sinapine on activity of acetylcholinesterase in cerebral homogenate and blood serum of rats[J].China Journal of Chinese Materia Medica,2008,33(7):813-815.
Authors:HE Ling ; LI Hai-tao ;GUO Sheng-wei ;LIU Li-fang ;QIU Jia-bin ;LI Fu ;CAI Bao-chang
Institution:Postdoctoral scientific research afflux station, Nanjing University of Traditional Chinese Medicine, Nanjing 210029, China.
Abstract:OBJECTIVE: The present study investigated the inhibitory effects of Chinese herb component sinapine on activity of acetylcholinesterase (AChE) in cerebral homogenate and blood serum of rats. METHOD: AChE was prepared from cerebral homogenate and blood serum of rats, respectively. Acetylcholinesterase activity assay kit and Chromatometry were used to detect the AChE activity. RESULT: Sinapine significantly inhibited AChE activity in vitro, with more effective on cerebral homogenate (IC50 3.66 micromol x L(-1)) than blood serum (IC50 22.1 micromol x L(-1)). CONCLUSION: Sinapine could significantly inhibit the cerebral AChE activity and may be a promising drug used for prevention and cure of Alzheimer's disease as a cholinesterase inhibitor.
Keywords:sinapine  acetylcholinesterase  cholinesterase inhibitors  Alzheimer's disease
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