Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms
文献类型：期刊论文
| 作者 | Song, Jin-Hui1; Fang, Zhong-Ze2,5; Zhu, Liang-Liang4; Cao, Yun-Feng3; Hu, Cui-Min5; Ge, Guang-Bo4; Zhao, De-Wei1 |
| 刊名 | journal of pharmacy and pharmacology
 |
| 出版日期 | 2013-04-01 |
| 卷号 | 65期号:4页码:521-527 |
| 关键词 | arbidol glucuronidation UDP-glucuronosyltransferases (UGTs) |
| 产权排序 | 待补充 |
| 通讯作者 | de-wei zhao |
| 合作状况 | 英 |
| 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. |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 学科主题 | 物理化学 |
| 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 |
| 收录类别 | SCI |
| 资助信息 | 4，3 |
| 原文出处 | 527 |
| 语种 | 英语 |
| WOS记录号 | WOS:000316292000006 |
| 公开日期 | 2014-09-11 |
| 源URL | [http://159.226.238.44/handle/321008/119246]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 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 |
| 推荐引用方式 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.,...&Zhao, De-Wei.(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. |
入库方式： OAI收割
来源：大连化学物理研究所
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