中药以口服为主，很多中药中含有的苷类成分多在肠道或肝脏发生生物转化，以次级苷或苷元的形式吸收入血，从而发挥药效。因此，鉴定代谢产物，并解释代谢产物与药效的关联性，对于诠释中药的物质基础、作用机理、质量控制、创新药物研发均具有重要意义。本项目在前期研究的基础上，以代表性三七皂苷为对象，综合运用药代动力学、药理学、化学生物学等手段，分析、鉴定口服给药后的体内代谢产物，研究其体内代谢产物与药效的关联性，揭示代谢产物体内暴露量对药效的贡献度;以血小板P2Y12受体为主要作用靶点，研究不同母核、不同糖基化模式的皂苷及其代谢产物对受体的生物效应差异，并探讨其在有效体内暴露剂量下，三七皂苷原型及其代谢产物止血/活血的协同或拮抗作用及其分子机制, 为诠释中医药理论、源于中药的创新药物研发和科学质量控制奠定基础，也为其它含苷类中药复杂体系的解析提供借鉴。

Traditional Chinese medicines are dosed mainly by oral administgration and the glycosides existing in many TCMs as principle bioactive components are sbsorbed in to blood after biotransforming into their corresponding aglycons or secondary glycosides by intestinal bacteria. The aglycons or secondary glycosides may further be activated to produce active metabolites by liver micrisome enzymes to play effecy. Therefore, the identification of metabolites and understanding the possible relevance of the metabolites and the efficacy is of important significance for the interpretation of the traditional Chinese medicine and their underlying mechanisms, quality control, and discovory of new drugs or candidates.. The precent project deals with the pharmacokinetics and pharmacodynamics syudy of the representative notoginsenosides, isolated from Panax notoginseng by use of pharmacokinetics, pharmacology, chemical biology and other means to identify the metabolites in vivo after oral administration of the saponins, discover the relevance of the metabolites and pharmacodynamics, reveal the potency of the metabolic substances produced in effective exposed amount. .The synergistic agonistic or antagonistic effects of the prodrug of saponins and their biotransformed metabolites on platelet P2Y12 receptor and structure-activity relationship of the different types of skeletones and glucosidation patterns of the saponins on the target will also be compared and elucidated to explain the regulatory effect of Panax notoginseng for its bidirectional effects of hemostasis and promoting blood circulation. .In a word, this project will provide evidence-based mechansms for disclosing the active components of Panax notoginseng and and its broad spectral activities in clinical application of both the crude drug and Notoginseng-containing fishished products as well as other saponins-containing medicinal herbs.