谷歌浏览器插件
订阅小程序
在清言上使用

Identification of Human UDP-Glucuronosyltransferase Involved in Gypensapogenin C Glucuronidation and Species Differences

International journal of molecular sciences(2023)

引用 0|浏览13
暂无评分
摘要
Gypensapogenin C (GPC) is one of the important aglycones of Gynostemma pentaphyllum (GP), which is structurally glucuronidated and is highly likely to bind to UGT enzymes in vivo. Due to the important role of glucuronidation in the metabolism of GPC, the UDP-glucuronosyltransferase metabolic pathway of GPC in human and other species' liver microsomes is investigated in this study. In the present study, metabolites were detected using high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). The results show that GPC could generate a metabolite through glucuronidation in the human liver microsomes (HLMs). Additionally, chemical inhibitors combined with recombinant human UGT enzymes clarified that UGT1A4 is the primary metabolic enzyme for GPC glucuronidation in HLMs according to the kinetic analysis of the enzyme. Metabolic differential analysis in seven other species indicated that rats exhibited the most similar metabolic rate to that of humans. In conclusion, UGT1A4 is a major enzyme responsible for the glucuronidation of GPC in HLMs, and rats may be an appropriate animal model to evaluate the GPC metabolism.
更多
查看译文
关键词
gypensapogenin C,glucuronidation,human liver microsomes,species differences
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要