中药化学成分体内代谢产物的制备方法

Preparation method for in vivo metabolites of chemical constituents from traditional Chinese medicines

传统中药多为口服用药,其在体内发挥药效的物质可能是中药中的化学成分,还可能是中药成分在体内的代谢产物,中药产生毒副作用和不良反应的原因也可能与中药成分的体内代谢产物有关。而迄今中药成分代谢产物的研究多局限在分析和结构推测鉴定水平,仅对少数可通过简单方法间接获取的代谢产物进行了较深入的生物学研究。因此,代谢产物的获取是深入研究其生物活性,进而明确中药药效和毒效的关键物质基础。本文结合本课题组近几年来的研究成果,对目前中药活性成分体内代谢产物的制备方法进行了总结和综述,希望能够为中药成分的体内代谢研究提供借鉴。

Objective Traditional Chinese medicines （TCM） are taken orally in most cases, and their chemical constituents generally have low blood concentrations and poor oral bioavailabilities. The absorbed chemical constituents of TCM, especially the in vivo biotransformed products might play an important role in explaining the effectiveness, and even the toxicities and side effects of TCM. Up to now, most of the studies on the in vivo metabolites of TCM constituents are still limited to structural identification, and on- ly a few researches on the bioactivities and toxicities of the metabolites have been carried out since they are not easy to obtain. There- fore, the preparation of in vivo metabolites is necessary for deeply investigating how and why TCM show the effectiveness or toxicity. Based on the studies of our group on the metabolism of TCM bioactive compounds in recent years, the preparation methods for in vivo metabolites are summarized, which might be helpful for the study of metabolism of TCM.