title: Effect of cholinesterase inhibition in vitro by huperzine analogs.
abstract: 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.
authors.affiliation: Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
authors.forename: X C
authors.initials: XC
authors.lastname: Tang
authors.forename: H
authors.initials: H
authors.lastname: Xu
authors.forename: J
authors.initials: J
authors.lastname: Feng
authors.forename: T X
authors.initials: TX
authors.lastname: Zhou
authors.forename: J S
authors.initials: JS
authors.lastname: Liu
mesh_terms: 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
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; C050426:huperzine A; D005702:Galantamine; C053016:huperzine B; D010830:Physostigmine; D000110:Acetylcholinesterase