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.
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.
出处
《中国药理学报》
CSCD
1995年第1期21-25,共5页
Acta Pharmacologica Sinica
关键词
石杉碱甲
毒扁豆碱
胆碱酯酶抑制剂
东莨菪碱
huperzine A
isovanihuperzine A
physostigmine
galanthamine
cholineste-rase inhibitors
scopolamine
isoflurophate
cognition disorders
memory
