石杉碱类似物对体外胆碱酯酶的抑制作用。
Effect of cholinesterase inhibition in vitro by huperzine analogs.
作者信息
Tang X C, Xu H, Feng J, Zhou T X, Liu J S
机构信息
Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
出版信息
Zhongguo Yao Li Xue Bao. 1994 Mar;15(2):107-10.
Huperzine (Hup) A and B were first discovered and studied by Chinese. Fourteen analogs of Hup were tested for their anticholinesterase (anti-ChE) activity by colorimetric method using rat erythrocyte membrane and serum as enzyme sources. Hup-A showed the highest anti-AChE potency. The anti-BuChE activity of (-)dihydro and (-)tetrahydro analogs were potent than those of Hup-A. Their anti-AChE activities were comparable to those of physostigmine and galanthamine. Dihydro analog inhibition was of the mixed competitive type with a Ki value of 0.12 mumol.L-1. Tetrahydro analog inhibition was of the competitive type with a Ki value of 0.56 mumol.L-1. They were different from isoflurophate to bond to AChE in a reversible manner.
石杉碱（Hup）A和B最初是由中国人发现并研究的。以大鼠红细胞膜和血清作为酶源，采用比色法对14种石杉碱类似物的抗胆碱酯酶（anti-ChE）活性进行了测试。石杉碱A显示出最高的抗乙酰胆碱酯酶（AChE）效力。（-）二氢和（-）四氢类似物的抗丁酰胆碱酯酶（BuChE）活性比石杉碱A更强。它们的抗AChE活性与毒扁豆碱和加兰他敏相当。二氢类似物的抑制作用为混合竞争型，Ki值为0.12 μmol·L-1。四氢类似物的抑制作用为竞争型，Ki值为0.56 μmol·L-1。它们与异氟磷不同，能以可逆方式与AChE结合。
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