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学科主题物理化学
UGT1A6 and UGT1A9 involving in the metabolism of daphnetin by human liver microsomes
Liang SC(梁思成); Liu HX(刘慧鑫); Ge GB(葛广波); Yang L(杨凌); Yang L
会议名称3rd asian pacific regional meeting of the International Society for Studies of Xenobiotics
会议日期2009-5-10
2009-05-10
会议地点泰国
页码71/1
部门归属十八室
主办者國際藥物代謝學會
英文摘要Daphnetin (7, 8-dihydroxycoumarin), one of coumarin derivatives, is the major bioactive constituent from Daphne odora (Thymelaeaceae). Previous studies indicated that daphnetin has the anti-coagulant activity like other coumarin analogs, and other functions including anti-inflammatory, arthritis and rheumatic activities. Though daphnetin has been generally used and been found with good pharmacological applications, its metabolites and metabolic pathway in human remain unknown. In the present study, the in vitro metabolic studies were carried out. The results showed that no metabolite was formed in NADPH-dependent metabolic system with human liver microsomes (HLMs). In contrast, two metabolites (M-1 and M-2) can be formed rapidly in the presence of UDPGA with HLMs, and were identified to be mono-glucuronides of daphnetin by liquid chromatography/mass spectrometry (LC/MS). Further study revealed that UGT1A6 and UGT1A9 primarily involved in the formation of M-1 and M-2 by using a range of specific UGT inhibitors, recombinant UGTs, and correlation analysis. In human liver microsomes, the Km values of M-1 and M-2 are 111.0 ± 6.2 μM and 93.2 ± 5.0 μM, respectively, and the Vmax values are 19.0 ± 0.4 nmol/min/mg and 16.3 ± 0.4 nmol/min/mg, respectively. The metabolic pathway and kinetic properties of daphnetin indicated that daphnetin can be cleared by UGTs and its UGT metabolites may play an important role in some pharmacological activities in vivo.
语种中文
WOS记录号WOS:000269483300140
引用统计
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/113644
专题中国科学院大连化学物理研究所
通讯作者Yang L
推荐引用方式
GB/T 7714
Liang SC,Liu HX,Ge GB,et al. UGT1A6 and UGT1A9 involving in the metabolism of daphnetin by human liver microsomes[C],2009:71/1.
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