Xiong Z Q, Tang X C, Lin J L, Zhu D Y
Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Zhongguo Yao Li Xue Bao. 1995 Jan;16(1):21-5.
To study the effects of isovanihuperzine A (IVHA) on cholinesterase and scopolamine-induced memory deficit.
AChE and BuChE activities were determined by the colorimetric method of Ellman. The Ki value was determined by the plotting method of Lineweaver and Burk. In a behavioral test, rats were trained to perform a radial arm maze task using a partially baited procedure.
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 mumol.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.
IVHA is a new potential reversible AChE inhibitor and merits further study as a cognitive enhancer.
研究异长春西汀（IVHA）对胆碱酯酶及东莨菪碱诱导的记忆缺陷的影响。
采用Ellman比色法测定乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）活性。通过Lineweaver和Burk绘图法测定Ki值。在行为学试验中，使用部分诱饵程序训练大鼠执行放射状臂迷宫任务。
IVHA的抗AChE活性与石杉碱甲（Hup-A）相当，且比毒扁豆碱和加兰他敏更强，IC50值为0.11μmol·L-1。IVHA为混合型竞争性抑制剂，Ki值为32nmol·L-1。它以可逆方式与AChE结合。腹腔注射剂量为0.2mg·kg-1的IVHA可显著逆转东莨菪碱诱导的放射状臂迷宫工作记忆和参考记忆损伤。
IVHA是一种新型潜在的可逆性AChE抑制剂，作为认知增强剂值得进一步研究。
