五味子醇甲的代谢转化

METABOLIC TRANSFORMATION OF SCHIZANDRIN

采用动物肝微粒体体外代谢法对五味子醇甲的代谢转化进行了研究。从体外代谢产物中鉴定其主要的三个代谢物为:7,8-顺二羟基五味子酸甲;7,7-顺二羟基-2-去甲基五味子醇甲及7,8-顺二羟基-3-去甲基五味子醇甲。在此基础上,建立了生物体液中五味子醇甲及其代谢物的反相HPLC分析方法,并用此法检测了服药后大鼠的胆汁及尿样,比较了体外代谢与体内代谢的异同。

The metabolic transformation of schizandrin, isolated from the kernelof Schizandra chinensis Bill,was studied in vitro with phenobarbital- induced rat liver micro-somal fractio containing the NADPH-generating system. The major metabolites wereisolated by preparative HPLC and identified as 7,8- dihydroxy-schizandrin, 7, 8- dihy-droxy-2- demethyl schizandrin and 7, 8- dihydroxy- 3- demethyl schizandrin by UV,NMR, MS spectral analysis. The 7, 8 - dihydroxy- schizandrin was confirmed further bycomparison with spectral and chromatographic behavior of the authentic compound. Themetabolic biotransformation of schizandrin in vivo was also determined.