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题名: Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential
作者: Jia, Lin1;  Hu, Cuimin3, 4;  Wang, Haina7;  Liu, Yongzhe2;  Liu, Xin1;  Zhang, Yan-Yan5, 6;  Li, Wei9;  Wang, Li-Xuan5, 6;  Cao, Yun-Feng1, 5, 6, 8;  Fang, Zhong-Ze2, 5, 6
关键词: zaltoprofen ;  chirality ;  UDP-glucuronosyltransferases (UGTs) ;  inhibition potential
刊名: CHIRALITY
发表日期: 2015-06-01
DOI: 10.1002/chir.22436
卷: 27, 期:6, 页:359-363
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Chemistry, Medicinal ;  Chemistry, Analytical ;  Chemistry, Organic ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ;  Chemistry
英文摘要: Zaltoprofen (ZLT) is a nonsteroidal antiinflammation drug, and has been clinically employed to treat rheumatoid arthritis, osteoarthritis, and other chronic inflammatory pain conditions. The present study aims to investigate the chirality influence of zaltoprofen towards the inhibition potential towards UDP-glucuronosyltransferases (UGTs) isoforms. In vitro a recombinant UGT isoforms-catalyzed 4-methylumbelliferone (4-MU) glucuronidation incubation system was employed to investigate the inhibition of (R)-zaltoprofen and (S)-zaltoprofen towards UGT isoforms. The inhibition difference capability was observed for the inhibition of (R)-zaltoprofen and (S)-zaltoprofen towards UGT1A8 and UGT2B7, but not for other tested UGT isoforms. (R)-zaltoprofen exhibited noncompetitive inhibition towards UGT1A8 and competitive inhibition towards UGT2B7. The inhibition kinetic parameters were calculated to be 35.3 M and 19.2 M for UGT1A8 and UGT2B7. (R)-zaltoprofen and (S)-zaltoprofen exhibited a different inhibition type towards UGT1A7. Based on the reported maximum plasma concentration of (R)-zaltoprofen in vivo, a high drug-drug interaction between (R)-zaltoprofen and the drugs mainly undergoing UGT1A7, UGT1A8, and UGT2B7-catalyzed glucuronidation was indicated. Chirality 27:359-363, 2015. (c) 2015 Wiley Periodicals, Inc.
关键词[WOS]: HYPERBILIRUBINEMIA ;  PHARMACOKINETICS ;  WARFARIN
语种: 英语
WOS记录号: WOS:000354998700001
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/146282
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.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou, Liaoning, Peoples R China
2.Tianjin Med Univ, Sch Publ Hlth, Dept Toxicol, Tianjin, Peoples R China
3.Tianjin Med Univ, Sch Basic Med Sci, Tianjin Life Sci Res Ctr, Tianjin, Peoples R China
4.Tianjin Med Univ, Sch Basic Med Sci, Dept Microbiol, Tianjin, Peoples R China
5.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian, Peoples R China
6.Liaoning Med Univ, Affiliated Hosp 1, Dalian, Peoples R China
7.Shandong Univ, Coll Pharmaceut Sci, Jinan 250100, Peoples R China
8.Shanghai Inst Planned Parenthood Res, Shanghai Engn & Technol Res Ctr Reprod Hlth Drug, Key Lab Contracept & Devices Res NPFPC, Shanghai, Peoples R China
9.Yangzhou Univ, Yangzhou 225009, Jiangsu, Peoples R China

Recommended Citation:
Jia, Lin,Hu, Cuimin,Wang, Haina,et al. Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential[J]. CHIRALITY,2015,27(6):359-363.
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