手性黄皮酰胺生物转化的立体选择性

以相同的肝微粒体温孵体系对(+) 和(-) 黄皮酰胺(Cla)进行了温孵，以HPLC分析比较了代谢结果，发现(+)-和(-)-Cla所产生的主要代谢产物基本相同，但主要代谢产物在(+)-和(-)-Cla温孵体系中含量差别较大，左旋体代谢产生的CM1和CM5的量比右旋体大；CM2是左旋Cla的主要代谢产物之一，右旋体产生极小的量；而CM3是右旋Cla的主要代谢产物，左旋体产生的量较少. CM4, CM6是由CM3进一步代谢所产生的双羟基代谢产物，右旋体产生的量多于左旋体. 定量分析(+)-，(-)-Cla在肝微粒体中不同时间的代谢情况，发现(+)-，(-)-Cla在实验浓度下均为非线性动力学，二者代谢速率基本相同，不同时间代谢的立体选择性基本相同.

Stereoselectivity of chiral clausenamide biotransformation

The metabolic differences between ( ) and (-) clausenamide in rat liver microsomes were found by comparing their metabolites. The (-) clausenmide generates more CM1 and CM5 than the ( ) clausenamide. CM2 is one of the main metabolites of (-) clausenamide but only minor was detected in ( ) clausenamide incubate. The amount of CM3 generated from ( ) clausenamide is much more than from (-) clausenamide. The ( ) clausenamide produces more CM4 and CM6 than the (-) clausenamide. By quantitative analysis of the amount of ( ) and (-) clausenamide metabolized in rat liver microsomes at different times, it was found that the pharmacokinetics of both ( ) and (-) clausenamide were non linear.