Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential

	Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential
	Jia, Lin 1; Hu, Cuimin 3,4; Wang, Haina 7; Liu, Yongzhe 2; Liu, Xin 1; Zhang, Yan-Yan 5,6; Li, Wei 9; Wang, Li-Xuan 5,6; Cao, Yun-Feng 1,5,6,8; Fang, Zhong-Ze 2,5,6
刊名	chirality
	2015-06-01
卷号	27 期号:6 页码:359-363
关键词	zaltoprofen chirality UDP-glucuronosyltransferases (UGTs) inhibition potential
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.
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
关键词[WOS]	hyperbilirubinemia ; pharmacokinetics ; warfarin
收录类别	SCI
语种	英语
WOS记录号	WOS:000354998700001
公开日期	2016-05-09
内容类型	期刊论文
源URL	[http://cas-ir.dicp.ac.cn/handle/321008/146282]
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.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
推荐引用方式 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.