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学科主题物理化学
Characterization of Human UDP-Glucuronosyltransferases responsible for the in vitro Glucuronidation of Armillarisin A
Sun DX(孙冬雪); Ge GB(葛广波); Fang ZZ(房中则); Zhu LL(朱亮亮); Liang SC(梁思成); Yang L(杨凌)
会议名称9th International Meeting of the International-Society-for-the-Study-of-Xenobiotics
会议日期2010-9-4
2010-09-04
会议地点土耳其
页码218/2
部门归属十八室
主办者国际药物代谢学会
英文摘要Armillarisin A, a new coumarin derivative isolated from the fungus Armillariella tabescens (Scop. ex Fr.) Singer, has been used for treatment of acute cholecystitis, infection of biliary system and pancreatitis in China for several years, but its metabolic pathway remains unknown. In the current study, the UDP-glucuronosyltransferase (UGT) conjugation pathway of Armillarisin A was investigated by using human liver microsomes (HLMs) and 12 commercially available recombinant human UGTs. One mono-glucuronide Armillarisin A was identified by liquid chromatography/mass spectrometry (LC/MS), when Armillarisin A was incubated with human liver microsomes in the presence of UDPGA. Assays with the recombinant human UGT isoform(s) revealed that human UGT1A1, UGT1A9, UGT1A7 and UGT2B15 involved in the glucuronidation of Armillarisin A. The Km values of HLM, rUGT1A9, rUGT1A1, rUGT1A7 and rUGT2B15 for the glucuronidation of Armillarisin A were 799.8 ± 51.5, 134.0 ± 17.2, 124.3 ± 4.8, 399.4 ± 37.8 and 420.2 ± 41.5 μM respectively. The intrinsic clearance of rUGT1A9 (48 ul/min/mg protein) is significantly larger than that of other recombinant UGT isoforms. Furthermore, the glucuronidation of Armillarisin A in HLMs (n=11) had the strong correlation (r=0.93, p<0.001) with propofol glucuronidation, a probe reaction for UGT1A9, while the chemical inhibition study using a series of inhibitors to UGTs showed similar inhibitory effects towards HLMs and UGT1A9 mediated glucuronidation. These results suggested that UGT1A9 played an important role in hepatic glucuronidation of Armillarisin A.
语种中文
WOS记录号WOS:000281147700386
引用统计
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/114328
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Sun DX,Ge GB,Fang ZZ,et al. Characterization of Human UDP-Glucuronosyltransferases responsible for the in vitro Glucuronidation of Armillarisin A[C],2010:218/2.
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