Inhibitory effects of huperzine B on cholinesterase activity in mice.
OBJECTIVE
To determine the anticholinesterase properties of huperzine B (Hup B) and compare with tacrine in vitro and in vivo.


METHODS
Spectrophotometry was used to determine ChE activity.


RESULTS
Hup B showed much more selective inhibition to acetylcholinesterase (AChE) than tacrine. The IC50 ratios of Hup B and tacrine for butyrylcholinesterase (BuChE): AChE were 65.8 and 0.54, respectively. Hup B ig exhibited higher efficacy on the inhibition of brain AChE than that of tacrine. Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. A single ig dose of Hup B produced steady state of AChE inhibition in 4 h.


CONCLUSIONS
Hup B exhibits higher selectivity and efficacy in the inhibition of AChE, and lower toxicity in mice than tacrine.
Liu
J
J
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhang
H Y
HY
Wang
L M
LM
Tang
X C
XC
D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000201:enzymology*; D002091:Butyrylcholinesterase / Q000378:metabolism*; D002417:Cattle; D002540:Cerebral Cortex / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D005260:Female; D008297:Male; D051379:Mice; D051381:Rats; D013619:Tacrine / Q000494:pharmacology
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D004365:Drugs, Chinese Herbal; C053016:huperzine B; D013619:Tacrine; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase