中国科学院大连化学物理研究所机构知识库
Advanced  
DICP OpenIR  > 中国科学院大连化学物理研究所  > 会议论文
学科主题: 物理化学
题名: UGT1A6 and UGT1A9 involving in the metabolism of daphnetin by human liver microsomes
作者: Liang SC(梁思成) ;  Liu HX(刘慧鑫) ;  Ge GB(葛广波) ;  Yang L(杨凌)
会议名称: 3rd asian pacific regional meeting of the International Society for Studies of Xenobiotics
会议日期: 2009-5-10
出版日期: 2009-05-10
会议地点: 泰国
通讯作者: Yang L
部门归属: 十八室
主办者: 國際藥物代謝學會
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
Citation statistics: 
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113644
Appears in Collections:中国科学院大连化学物理研究所_会议论文

Files in This Item:

There are no files associated with this item.


Recommended Citation:
Liang SC,Liu HX,Ge GB,et al. UGT1A6 and UGT1A9 involving in the metabolism of daphnetin by human liver microsomes[C]. 见:3rd asian pacific regional meeting of the International Society for Studies of Xenobiotics. 泰国. 2009-5-10.
Service
 Recommend this item
 Sava as my favorate item
 Show this item's statistics
 Export Endnote File
Google Scholar
 Similar articles in Google Scholar
 [梁思成]'s Articles
 [刘慧鑫]'s Articles
 [葛广波]'s Articles
CSDL cross search
 Similar articles in CSDL Cross Search
 [梁思成]‘s Articles
 [刘慧鑫]‘s Articles
 [葛广波]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
  Add to CiteULike  Add to Connotea  Add to Del.icio.us  Add to Digg  Add to Reddit 
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Powered by CSpace