Effects of synthetic (-)-huperzine A on cholinesterase activities and mouse water maze performance.
OBJECTIVE
To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance.


METHODS
Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect.


RESULTS
The IC50 of synthetic Hup A for acetylcholinesterase (AChE) of rat cortex and rat erythrocyte membrane determined in vitro were 64.7 (52.6-79.5) and 53.9 (43.6-66.6) nmol.L-1, respectively, and for butyrylcholinesterase of rat serum was 53.6 (44.9-63.8) mumol.L-1. Synthetic Hup A 0.12-0.48 mg.kg-1 ig produced a dose-dependent inhibition of brain AChE in mice. Synthetic Hup A 0.05 mg.kg-1 ig attenuated scopolamine-induced impairment of spatial memory. The efficacy of synthetic Hup A was the same as natural Hup A.


CONCLUSIONS
Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A.
Liu
J
J
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhang
H Y
HY
Tang
X C
XC
Wang
B
B
He
X C
XC
Bai
D L
DL
D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids; D000818:Animals; D002091:Butyrylcholinesterase / Q000097:blood; D002540:Cerebral Cortex / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004910:Erythrocyte Membrane / Q000378:metabolism; D005260:Female; D008297:Male; D018782:Maze Learning / Q000187:drug effects*; D008568:Memory / Q000187:drug effects; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000494:pharmacology*
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; C050426:huperzine A; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase