中国临床药理学杂志2011，Vol.27Issue(11)：847-850,4.
山姜素在人肝微粒体的葡萄糖醛酸化反应研究
Study on the glucuronidation of alpinetin in human liver microsomes
摘要
Abstract
Objective To investigate the glucuronidation of alpinetin in human liver microsomes, including elucidation of the structure of alpinetin glucuronide and identification of UDP - glucuronosyltransferases (UGT) isoforms involved in alpinetin's glucuronidation. Methods After incubation of alpinetin using in vitro human liver microsomal system, HPLC - UV was utilized to determine the glucuronides of alpinetin. MS and NMR were employed to elucidate the structures of metabolite. Screening assays with recombinant human UGTs were used to identify the UGT isoforms involved in the glucuronidation of alpinetin. Results One metabolite was identified and elucidated to be alpinetin - 0 - monoglucu-ronide. The metabolic behaviour of alpinetin was demonstrated to obey the typical monophasic Michaelis - Menten kinetics, and kinetic parameters were calculated tobe(101.9±3.0) nmol · Min-1 · Mg-1 · Pro and (40. 6 ±3.6) μmol · L-1 for Vmax and Km, respectively. UGT1A1, 1A3, 1A9 and 2B15 were determined to participate in the glucuronidation of alpinetin. Conclusion In the present experiment, the glucuronidation behaviour of alpinetin was clearly investigated, which is beneficial to deeply understanding of alpinetin's metabolism in human and its phar-macodynamic basis.关键词
山姜素/葡萄糖醛酸化反应/人肝微粒体Key words
alpinetin/ glucuronidation/ human liver microsomes分类
医药卫生引用本文复制引用
金学利,房中则,曲衍清,唐博,杨凌,王立明..山姜素在人肝微粒体的葡萄糖醛酸化反应研究[J].中国临床药理学杂志,2011,27(11):847-850,4.基金项目
科技部973基金资助项目(2009CB522808) （2009CB522808）
国家自然科学基金资助项目(81001473) （81001473）
