Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential
文献类型：期刊论文
| 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 |
| 刊名 | chirality
 |
| 出版日期 | 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 |
| 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. |
入库方式： OAI收割
来源：大连化学物理研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。