[Biotransformation of (+)- and (-)-clausenamide in rats].
OBJECTIVE
To study the metabolic pathway of chiral clausenamide in the rat and understand its stereoselectivity.


METHODS
The urine, feces and blood of rat were gathered after the drug was administered, the known metabolites were analyzed by HPLC-DAD and one unknown metabolite was elucidated by using LC-MS analysis. Metabolic stereoselectivity was determined by comparing the metabolic results of (+)- and (-)-clausenamide.


RESULTS
Six known metabolites were determined and one unknown metabolite was elucidated as N-demethylclausenamide. The metabolic stereoselectivity was shown distinctly.


CONCLUSIONS
Chiral clausenamide was mainly metabolized by hydroxylation in liver and the biotransformation exhibited pronounced substrate stereoselectivity.
Yao
Q Q
QQ
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China. Yqingqiang@yahoo.com
Wang
Y
Y
Yang
S M
SM
Wang
M Z
MZ
D000818:Animals; D001711:Biotransformation; D002851:Chromatography, High Pressure Liquid; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification / Q000493:pharmacokinetics*; D007769:Lactams / Q000302:isolation & purification / Q000493:pharmacokinetics*; D017705:Lignans / Q000302:isolation & purification / Q000493:pharmacokinetics*; D008297:Male; D018515:Plant Leaves / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D027821:Rutaceae / Q000737:chemistry; D013237:Stereoisomerism
D004365:Drugs, Chinese Herbal; D007769:Lactams; D017705:Lignans; C053048:clausenamide