芥子碱对大鼠脑匀浆和血清中乙酰胆碱酯酶的抑制作用

Inhibitory effects of sinapine on activity of acetylcholinesterase in cerebral homogenate and blood serum of rats

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。

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 3.66μmol · L^-1 ） than blood serum （IC50 22. 1 μmol · 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.