DICP OpenIR
Arbidol exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A9 and 2B7
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
Source PublicationPHARMAZIE
2013-12-01
DOI10.1691/ph.2013.2641
Volume68Issue:12Pages:945-950
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectChemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS KeywordLIVER CYTOCHROME-P450 ENZYMES ; TIME-DEPENDENT INHIBITION ; DRUG-DRUG INTERACTIONS ; REVERSIBLE INHIBITION ; IN-VITRO ; GLUCURONIDATION ; METABOLISM ; VIRUS ; PHARMACOKINETICS ; IDENTIFICATION
AbstractThe 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.
Language英语
WOS IDWOS:000334260800005
Citation statistics
Cited Times:18[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/137773
Collection中国科学院大连化学物理研究所
Affiliation1.3 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
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.
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