摘要
用比色法测试表明,14个半合成类似物的抗AChE作用均弱于Hup-A,左旋二氢及四氢类似物的抗BuChE作用稍强于Hup-A,前者属混合型抑制剂,K_i值为0.12μmol·L^(-1)。后者属竞争型抑制剂,K_i值为0.56μmol·L^(-1)。二者不同于异氟磷,与AChE为可逆性结合。
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 col-orimetric method using rat erythrocy.te 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 μmol·L-1. Tetrahydro analog inhibition was of the competitive type with a Ki value of 0. 56 μmol·L-1. They were different from isoflurophate to bond to AChE in a reversible manner.
出处
《中国药理学报》
CSCD
1994年第2期107-110,共4页
Acta Pharmacologica Sinica
关键词
石杉碱
红细胞
胆碱酯酶
抑制剂
huperzine
physostigmine
galanthamine
isoflurophate
erythrocyte membrane
cholinesterase inhibitors
struc- ture-activity relationship
