葡萄糖醛酸化是一类重要的由葡萄糖醛酸转移酶(UDP-glucuronosyltransferase,UGT)催化的Ⅱ相代谢反应,负责多种体内内源性和外源性物质的清除。葡萄糖醛酸化影响内源或外源性物质在组织中的分布水平,对药物的药效和不良反应有巨大的影响。UGTs广泛分布于机体的各种组织中,不同亚型之间存在组织差异性和底物特异性。葡萄糖醛酸苷的制备为植物天然产物的药理活性、药动学性质、药物间相互作用等研究提供了基础。综述了植物天然产物酚类、香豆素类、木脂素类、生物碱类、萜类等葡萄糖醛酸苷生物合成的研究进展,为这类化合物的制备和药理活性研究提供参考。

Glucuronidation is an important phase Ⅱ metabolism catalyzed by UDP-glucuronosyltransferases (UGT), which is involved in the clearance of many endogenous and exogenous substances. Glucuronidation influences the tissue distribution of endogenous and exogenous compounds, and has a great impact on the efficacy, toxicity, and side effects of drugs. UGTs are widely distributed in various tissues of the body, featured by various tissue-abundance and substrate-specificity among different isoforms. Preparation of glucuronides for plant natural products provides foundation to evaluate their pharmacological activities, pharmacokinetic properties, and drug interactions. Research progress on biosynthesis of glucuronides of plant natural products such as polyphenols, coumarins, lignans, alkaloids, and terpenoids were summarized in this paper, in order to provide reference for their preparation and pharmacological studies.

R282.1

国家重点研发计划“合成生物学”重点专项（2020YFA0907900）；天津中医药大学研究生科研创新项目（YJSKC-20191021）