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学科主题: 物理化学
题名: Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms
作者: Song, Jin-Hui1;  Fang, Zhong-Ze2, 5;  Zhu, Liang-Liang4;  Cao, Yun-Feng3;  Hu, Cui-Min5;  Ge, Guang-Bo4;  Zhao, De-Wei1
通讯作者: De-Wei Zhao
关键词: arbidol ;  glucuronidation ;  UDP-glucuronosyltransferases (UGTs)
刊名: JOURNAL OF PHARMACY AND PHARMACOLOGY
发表日期: 2013-04-01
DOI: 10.1111/jphp.12014
卷: 65, 期:4, 页:521-527
收录类别: SCI
合作性质: 
文章类型: Article
部门归属: 18
项目归属: 1806
产权排名: 待补充
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Pharmacology & Pharmacy
资助者: 4,3
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Objectives The aim of this work was to identify the uridine glucuronosyltransferase (UGT) isoforms involved in the metabolism of the broad-spectrum antiviral drug arbidol. Methods A human liver microsome (HLM) incubation system was employed to catalyse the formation of arbidol glucuronide. The glucuronidation activity of commercially recombinant UGT isoforms towards arbidol was screened. A combination of kinetic analysis and chemical inhibition study was used to determine the UGT isoforms involved in arbidol's glucuronidation. Key findings The arbidol glucuronide was detected when arbidol was incubated with HLMs in the presence of UDP-glucuronic acid. The EadieHofstee plot showed that glucuronidation of arbidol was best fit to the MichaelisMenten kinetic model, and Km and apparent Vmax were calculated to be 8.0 +/- 0.7m and 2.03 +/- 0.05nmol/min/mg protein, respectively. Assessment of a panel of recombinant UGT isoforms revealed that UGT1A1, UGT1A3 and UGT1A9 could catalyse the glucuronidation of arbidol. Kinetic analysis and chemical inhibition study demonstrated that UGT1A9 was the predominant UGT isoform involved in arbidol glucuronidation in HLMs. Conclusions The major contribution of UGT1A9 towards arbidol glucuronidation was demonstrated in this study.
关键词[WOS]: HUMAN UDP-GLUCURONOSYLTRANSFERASES ;  MYCOPHENOLIC-ACID ;  HUMAN LIVER ;  IN-VITRO ;  GENETIC POLYMORPHISMS ;  VIRUS ;  PHARMACOKINETICS ;  IDENTIFICATION ;  METABOLISM ;  BIOACTIVATION
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000316292000006
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/119246
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Dalian Univ, Affiliated Zhongshan Hosp, Dept Orthoped, Dalian 116001, Peoples R China
2.Liaoning Med Univ, Jinzhou, Peoples R China
3.Shanghai Inst Planned Parenthood Res, Shanghai Engineer & Technol Res Ctr Reprod Hlth D, Key Lab Contracept & Devices Res NPFPC, Shanghai, Peoples R China
4.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian, Peoples R China
5.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA

Recommended Citation:
Song, Jin-Hui,Fang, Zhong-Ze,Zhu, Liang-Liang,et al. Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms[J]. JOURNAL OF PHARMACY AND PHARMACOLOGY,2013,65(4):521-527.
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