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题名: Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7
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
发表日期: 2013-12-01
DOI: 10.1691/ph.2013.2641
卷: 68, 期:12, 页:945-950
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, Multidisciplinary ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ;  Chemistry
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.
关键词[WOS]: LIVER CYTOCHROME-P450 ENZYMES ;  TIME-DEPENDENT INHIBITION ;  DRUG-DRUG INTERACTIONS ;  REVERSIBLE INHIBITION ;  IN-VITRO ;  GLUCURONIDATION ;  METABOLISM ;  VIRUS ;  PHARMACOKINETICS ;  IDENTIFICATION
语种: 英语
WOS记录号: WOS:000334260800005
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/137773
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: 1.3 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

Recommended Citation:
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.
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