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学科主题物理化学
Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms
Song, Jin-Hui1; Fang, Zhong-Ze2,5; Zhu, Liang-Liang4; Cao, Yun-Feng3; Hu, Cui-Min5; Ge, Guang-Bo4; Zhao, De-Wei1; De-Wei Zhao
关键词Arbidol Glucuronidation Udp-glucuronosyltransferases (Ugts)
刊名JOURNAL OF PHARMACY AND PHARMACOLOGY
2013-04-01
DOI10.1111/jphp.12014
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
资助者4,3 ; 4,3 ; 4,3 ; 4,3
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]HUMAN UDP-GLUCURONOSYLTRANSFERASES ; MYCOPHENOLIC-ACID ; HUMAN LIVER ; IN-VITRO ; GENETIC POLYMORPHISMS ; VIRUS ; PHARMACOKINETICS ; IDENTIFICATION ; METABOLISM ; BIOACTIVATION
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.
语种英语
资助者4,3 ; 4,3 ; 4,3 ; 4,3
原文出处查看原文
WOS记录号WOS:000316292000006
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/119246
专题中国科学院大连化学物理研究所
通讯作者De-Wei Zhao
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
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GB/T 7714
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.
APA Song, Jin-Hui.,Fang, Zhong-Ze.,Zhu, Liang-Liang.,Cao, Yun-Feng.,Hu, Cui-Min.,...&De-Wei Zhao.(2013).Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms.JOURNAL OF PHARMACY AND PHARMACOLOGY,65(4),521-527.
MLA Song, Jin-Hui,et al."Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms".JOURNAL OF PHARMACY AND PHARMACOLOGY 65.4(2013):521-527.
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