DICP OpenIR
Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential
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
KeywordZaltoprofen Chirality Udp-glucuronosyltransferases (Ugts) Inhibition Potential
Source PublicationCHIRALITY
2015-06-01
DOI10.1002/chir.22436
Volume27Issue:6Pages:359-363
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectChemistry, Medicinal ; Chemistry, Analytical ; Chemistry, Organic ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS KeywordHYPERBILIRUBINEMIA ; PHARMACOKINETICS ; WARFARIN
AbstractZaltoprofen (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.
Language英语
WOS IDWOS:000354998700001
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/146282
Collection中国科学院大连化学物理研究所
Affiliation1.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
GB/T 7714
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.
APA Jia, Lin.,Hu, Cuimin.,Wang, Haina.,Liu, Yongzhe.,Liu, Xin.,...&Fang, Zhong-Ze.(2015).Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential.CHIRALITY,27(6),359-363.
MLA Jia, Lin,et al."Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential".CHIRALITY 27.6(2015):359-363.
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