基于HPLC-DAD-MS~n的柴胡皂苷A的体外生物转化研究

目的对柴胡皂苷A进行体外生物转化,分析其体外代谢产物。方法用人工胃液模拟胃酸环境,厌氧状态下与大鼠肠内容物共温孵模拟肠道环境,分别进行柴胡皂苷A的体外生物转化,采用HPLC-DAD-MS~n方法,分析鉴定代谢产物。结果在人工胃液中,柴胡皂苷A可转化为柴胡皂苷b1、柴胡皂苷g,在肠道菌群环境下,柴胡皂苷A可先转化为柴胡次皂苷F,进一步转化为柴胡皂苷元F。结论模拟体内环境,柴胡皂苷A可转化成其次生苷和苷元,采用HPLC-DAD-MS~n可以指认并鉴定其产物。柴胡皂苷A的药物分布与浓度不能全面反映其体内过程,应同时考察其次生代谢产物。

Research on biotransformation of saikosaponin A in vitro based on HPLC-DAD-MSn

Objective To study the biotransformation of saikosaponin A in vitro and analyze its metabolites. Methods Saikosaponin A was incubated in artificial gastric juice and intestinal contents of rats in anaerobic conditions, respectively, and the metabolites were analyzed and identified by HPLC-DAD-MSⁿ. Results By incubation of saikosaponin A in artificial gastric juice, saikosaponin b₁ and g were detected in the reaction mixture. By the anaerobic incubation of saikosaponin A with intestinal flora, prosaikogenin F was soon detected, but it was further converted to saikogenin F. Conclusion Saikosaponin A can be transformed to secondary glycosides and glycosides in artificial gastrointestinal environment. And the products can be identified by HPLC-DAD-MSⁿ. The distribution and concentration of saikosaponin A in vivo can not reflect its fate fully, and the metabolites should be considered simutaneously.