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: Characterization of Human UDP-Glucuronosyltransferase Isoforms Responsible for the in vitro Glucuronidation of Esculetin
作者: Ge GB(葛广波) ;  Liang SC(梁思成) ;  Liu HX(刘慧鑫) ;  Zhang YY(张延延) ;  Yang L(杨凌)
会议名称: 16th North American Regional ISSX Meeting
会议日期: 2009-10-18
出版日期: 2009-10-18
会议地点: 美国
通讯作者: 杨凌
部门归属: 十八室
主办者: The International Society for the Study of Xenobiotics (ISSX)
摘要: Esculetin (6,7-dihydroxycoumarin), is one of coumarin analogs isolated from various plant including Cichorium intybus, Artemisia scoparia and Fraxinus japonica Blume, has been found to exhibit broaden biological effects, such as analgesic, anti-inflammatory, anti-tumor, anti-arrhythmic, and scavenging activity against reactive oxygen species. Esculetin has been widely used in many Asia countries, and a previous study showed that it can be metabolized by recombinant human UDP-glucuronosyltransferase (UGT) 2B15. However, the metabolic pathway of esculetin in human has not been well-characterized. In the present study, the glucuronidation pathway of esculetin was investigated by using human liver microsomes (HLMs) and 12 commercially available recombinant human UGTs. The results showed that only one metabolite (M-1) can be rapidly formed in the presence of UDPGA with HLMs, which was identified as a C-6 mono glucuronidation metabolite by liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR), indicating that C-6 phenolic group of esculetin was a preferred glucuronidation site. Recombinant human UGTs study revealed that many UGT isoforms (including UGT1A6, UGT1A1, UGT1A7, UGT1A8 and UGT2B15) involved in C-6 glucuronidation of esculetin, and further study revealed that Km value of M-1 in human liver microsomes was 208 + 31 μM. These results indicated that many UGT isoforms have contributed glucuronidation clearance of esculetin via the selective glucuronidation of C-6 phenolic group.
语种: 中文
Citation statistics: 
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113674
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:
Ge GB,Liang SC,Liu HX,et al. Characterization of Human UDP-Glucuronosyltransferase Isoforms Responsible for the in vitro Glucuronidation of Esculetin[C]. 见:16th North American Regional ISSX Meeting. 美国. 2009-10-18.
Service
 Recommend this item
 Sava as my favorate item
 Show this item's statistics
 Export Endnote File
Google Scholar
 Similar articles in Google Scholar
 [葛广波]'s Articles
 [梁思成]'s Articles
 [刘慧鑫]'s Articles
CSDL cross search
 Similar articles in CSDL Cross Search
 [葛广波]‘s Articles
 [梁思成]‘s Articles
 [刘慧鑫]‘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