Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7
文献类型：期刊论文
| 作者 | Liu, Xin1; Huang, Ting2; Chen, Jian-Xing2; Zeng, Jia2; Fan, Xu-Ran3; Zhu, Xu3; Vu, Zhen-Wen3; Sun, Xiao-Yu3; Hong, Mo3; Sun, Hong-Zhi1 |
| 刊名 | pharmazie
 |
| 出版日期 | 2013-12-01 |
| 卷号 | 68期号:12页码:945-950 |
| 英文摘要 | the aim of the present study was to investigate arbidol's inhibition towards udp-glucuronosyltransferase (ugt) 1a9 and 2b7. the nonspecific probe substrate 4-methylumbelliferone (4-mu) and recombinant ugt enzymes (ugt1a9, ugt2b7) were firstly used to evaluate the inhibition of arbidol towards ugt1a9 and ugt2b7. furthermore, specific substrates of ugt1a9 and ugt2b7 propofol and zidovudine (azt) were used to determine the inhibition of arbidol towards ugt1a9 and ugt2b7. inhibition type and inhibition kinetic parameters (k-i) were determined. in vitro-in vivo extrapolation (iv-ive) was performed to predict in vivo ddi magnitude induced by arbidol. arbidol was demonstrated to exhibit competitive inhibition towards ugt1a9 and ugt2b7 without substate-dependent behaviour. the inhibition kinetic parameters (k-i) were calculated to be 0.5 mu m, 3.5 mu m, 2.8 mu m, 29.7 mu m for ugt2b7-mediated 4-mu glucuronidation, ugt1a9-mediated 4-mu glucuronidation, ugt2b7-mediated azt glucuronidation, and ugt1a9-mediated propofol glucuronidation, respectively. using these parameters, the in vivo alteration of area under of concentration-time curve (auc) was calculated to be 156%, 22%, 28% and 2.6%, respectively. given that arbidol exhibits strong inhibition towards ugt1a9 and ugt2b7, clinical monitoring should be given when arbidol was co-administered with drugs mainly undergoing ugt1a9, ugt2b7-mediated metabolism. |
| WOS标题词 | science & technology ; life sciences & biomedicine ; physical sciences |
| 类目[WOS] | chemistry, medicinal ; chemistry, multidisciplinary ; pharmacology & pharmacy |
| 研究领域[WOS] | pharmacology & pharmacy ; chemistry |
| 关键词[WOS] | liver cytochrome-p450 enzymes ; time-dependent inhibition ; drug-drug interactions ; reversible inhibition ; in-vitro ; glucuronidation ; metabolism ; virus ; pharmacokinetics ; identification |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000334260800005 |
| 公开日期 | 2015-11-10 |
| 源URL | [http://159.226.238.44/handle/321008/137773]  |
| 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 | 1.3 Joint Ctr Translat Med, Dalian 116023, Peoples R China 2.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China 3.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Xin,Huang, Ting,Chen, Jian-Xing,et al. Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7[J]. pharmazie,2013,68(12):945-950. |
| APA | Liu, Xin.,Huang, Ting.,Chen, Jian-Xing.,Zeng, Jia.,Fan, Xu-Ran.,...&Sun, Hong-Zhi.(2013).Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7.pharmazie,68(12),945-950. |
| MLA | Liu, Xin,et al."Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7".pharmazie 68.12(2013):945-950. |
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。