Effect of cholinesterase inhibition in vitro by huperzine analogs.
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.
Tang
X C
XC
Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Xu
H
H
Feng
J
J
Zhou
T X
TX
Liu
J S
JS
D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids / Q000494:pharmacology; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004910:Erythrocyte Membrane / Q000201:enzymology*; D005702:Galantamine / Q000494:pharmacology; D010830:Physostigmine / Q000494:pharmacology; D051381:Rats; D012717:Sesquiterpenes / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; C050426:huperzine A; D005702:Galantamine; C053016:huperzine B; D010830:Physostigmine; D000110:Acetylcholinesterase