【摘要】 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IC₅₀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.更多还原

【Abstract】 AIM:To study the effects of isovanihuper-zine A (IVHA) on cholinesterase and scopo-lamine-induced memory deficit. METHODS: AChE and BuChE activities were determined by the colorimetric method of Ellman. The K, value was determined by the plotting method of Lineweaver and Burk. In a behavioral test, fats were trained to perform a radial arm maze task using a partially baited procedure. RESULTS: The anti-AChE activity of IVHA was comparable to huperzine A (Hup-A) , and was more potent than those of physostigmine and galanthamine with an IC50 value of 0. 11 umol.L-1.IVHA was a mixed competitive type with a Ki value of 32 nmol .L-1. It bound to AChE in a reversible manner. IVHA at a dose of 0. 2 mg .kg-1 ip significantly reversed scopolamine-induced working memory and reference memory impairments in radial arm maze. CONCLUSION: IVHA is a new potential reversible AChE inhibitor and merits further study as a cognitive enhancer.更多还原