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目的:研究石杉碱类似物异香兰石杉碱甲(IVHA)对胆碱酯酶的抑制作用和东莨菪碱导致的记忆障碍的影响.方法:乙酰胆碱酯酶和丁酰胆碱酯酶活力用Ellman比色法测定.抑制常数K_i值抑制机制用Lineweaver和Burk的双倒数作图法测定.行为测试用八臂迷宫装置.结果:IVHA的抗AChE作用稍弱于Hup-A.它对红细胞膜AChE的IC_(50)为0.11 μmol·L~(-1).作用强于Phys和Gal.属混合型抑制剂,K_i值为32 nmol·L~(-1).不同于异氟磷,与AChE为可逆性结合.ip给与IVHA0.2 mg·kg~(-1)翻转东莨菪碱导致的八臂迷宫记忆障碍.结论:IVHA是一个新的强效可逆胆减酯酶抑制剂,值得进一步研究.
OBJECTIVE: To study the inhibitory effect of huperzine analogue of huperzinone (IVHA) on cholinesterase and scopolamine-induced memory impairment.Methods Acetylcholinesterase and butyrylcholinesterase activities were measured by Ellman ratio Colorimetric method.The inhibitory K_i value inhibition mechanism was determined by double reciprocal mapping of Lineweaver and Burk.The behavioral test was performed with an eight-arm labyrinth device.Results: The anti-AChE effect of IVHA was slightly weaker than that of Hup-A, The IC 50 was 0.11 μmol·L -1, which was stronger than that of Phys and Gal.It had a K_i value of 32 nmol·L -1, different from isoflurane and AChE Reversible combined with .ip IV given ivHA0.2 mg · kg -1 reversed scopolamine-induced mammillary memory barrier.Conclusion: IVHA is a new potent and reversible bile-esterase inhibitor, worthy of further study.