黄酮类化合物的药物代谢研究进展

Research progress on drug metabolism of flavanoids

黄酮类化合物是食物和传统中药中所含的一类重要的天然植物成分。大多数黄酮具有很强的还原活性故在体内易被氧化代谢,该过程通常由CYP1A酶家族参与。此外,某些甲氧基黄酮在体内还可进行脱甲基代谢;黄酮类化合物的分子结构中往往含有1个或多个酚羟基,易和葡萄糖醛酸、硫酸或谷胱甘肽等结合,生成水溶性较大的化合物排出体外;天然黄酮类化合物多以苷类形式存在,口服后易被肠道菌群产生的水解酶代谢为苷元再吸收入血。不少黄酮类化合物对CYP酶有较强的抑制作用,该作用是某些黄酮类化合物预防和抑制肿瘤的重要机制之一。该文总结了黄酮类化合物药物代谢的特点,并对黄酮类化合物和CYP酶的代谢相互作用进行了综述。

Flavanoids are important phytochemistry compositions in foods and traditional Chinese medicines（TCM） and are mainly oxidized by CYP1A family in vivo.Some methoxyflavones could also be metabolized through demethylation.Usually,flavanoids own one or more phenolic hydroxyl group in their molecular structures,which facilitate conjugation with glucuronic acid and sulphuric acid,forming metabolites with good water-solubility to excrete.Natural flavanoids mainly exist in glycoside,and after oral,they would be easily metabolized to aglycone by hydratase in gut microflora and then absorbed into blood.Besides,many flavanoids have strong inhibitory actions on Cytochrome P450 enzymes,which are significant mechanisms in cancer precaution and tumor inhibition.In this paper,we reviewed lots of articles and summarized metabolism characteristics of flavanoids and metabolism interaction with Cytochrome P450 enzymes.