天然黄酮苷的代谢途径研究进展

黄酮苷是自然界中多种植物的次级代谢产物,具有多种生物活性,如抗癌、抗氧化及抗菌活性等。根据苷元与糖的连接形式,黄酮苷又可以分为黄酮O-苷和黄酮C-苷。黄酮苷在体内的代谢主要以胃肠道水解和肝脏代谢为主,胃肠道中水解葡萄糖、木糖、鼠李糖等糖基产生次生苷或苷元,肝脏则主要对入血的黄酮苷或苷元进行葡萄糖醛酸化、甲氧基化等II相代谢反应。对常用中药淫羊藿EpimediiFolium、甘草GlycyrrhizaeRadixetRhizoma、黄芩ScutellariaeRadix、陈皮Citri Reticulatae Pericarpium、大蓟Cirsii Japonici Herba、知母Anemarrhenae Rhizoma、葛根Puerariae Lobatae Radix等的黄酮类化合物体内代谢及体外肠道菌群转化进行综述,并对其代谢规律进行总结,以期明确黄酮苷的体内代谢规律,为科学阐释以黄酮苷为主要成分的中药发挥药效的体内物质基础及基于黄酮苷体内代谢产物的新药研发提供依据。

Advances in metabolism of natural flavonoid glycosides

Flavonoid glycosides (FGs) are secondary metabolites of many plants widely found in nature, and exhibit significant biological activities, such as anticancer, antioxidant and antimicrobial. According to the glycosidic bonds, FGs are divided into flavonoid O-glycosides and flavonoid C-glycosides. The main metabolic processes of FGs in vivo were specific hydrolysis in the gastrointestinal tract and glucuronidation in liver. Glucose, xylose, rhamnose and other glycosyl groups were hydrolyzed to produce secondary glycosides or aglycones in the gastrointestinal tract that were absorbed into blood, and then further glucuronidation and methylation metabolites are mainly produced by phase II metabolism in liver. This article reviews the metabolism in vivo and biotransformation in vitro of some typical natural flavonoid glycosides exited in Chinese materia medica (CMMs), such as flavonoid O-glycosides in Epimedii Folium. Glycyrrhizae Radix et Rhizoma. Scutellariae Radix. Citri Reticulatae Pericarpium, and Cirsii Japonici Herba, and flavonoid C-glycosides in Anemarrhenae Rhizoma and Puerariae Lobatae Radix. The investigation of the metabolisms of FGs in vivo is helpful for the clarification of the effective ingredients in CMMs, which will provide the basis for new drugs development based on metabolites in vivo.