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Strong Specific Inhibition of UDP-glucuronosyltransferase 2B7 by Atractylenolide I and III
Zhang, Qian1; Cao, Yun-Feng2; Ran, Rui-Xue3; Li, Rong-Shan3; Wu, Xue1,4,5,6; Dong, Pei-Pei7; Zhang, Yan-Yan4,5,8; Hu, Cui-Min9; Wang, Wei-Ming1
KeywordAtractylenolide i Atractylenolide Iii Drug-drug Interaction
Source PublicationPHYTOTHERAPY RESEARCH
2016
ISSN0951-418X
DOI10.1002/ptr.5496
Volume30Issue:1Pages:25-30
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy
WOS KeywordBILE-ACIDS ; VITRO ; UGT2B7 ; HYPERBILIRUBINEMIA ; GLUCURONIDATION ; ZIDOVUDINE ; VIVO ; UGTS
AbstractDrug-metabolizing enzymes inhibition-based drug-drug interaction remains to be the key limiting factor for the research and development of efficient herbal components to become clinical drugs. The present study aims to determine the inhibition of uridine 5-diphospho-glucuronosyltransferases (UGTs) isoforms by two important efficient herbal ingredients isolated from Atractylodes macrocephala Koidz, atractylenolide I and III. In vitro recombinant UGTs-catalysed glucuronidation of 4-methylumbelliferone was used to determine the inhibition capability and kinetics of atractylenolide I and III towards UGT2B7, and in silico docking method was employed to explain the possible mechanism. Atractylenolide I and III exhibited specific inhibition towards UGT2B7, with negligible influence towards other UGT isoforms. Atractylenolide I exerted stronger inhibition potential than atractylenolide III towards UGT2B7, which is attributed to the different hydrogen bonds and hydrophobic interactions. Inhibition kinetic analysis was performed for the inhibition of atractylenolide I towards UGT2B7. Inhibition kinetic determination showed that atractylenolide I competitively inhibited UGT2B7, and inhibition kinetic parameter (Ki) was calculated to be 6.4M. In combination of the maximum plasma concentration of atractylenolide I after oral administration of 50mg/kg atractylenolide I, the area under the plasma concentration-time curve ration AUC(i)/AUC was calculated to be 1.17, indicating the highly possible drug-drug interaction between atractylenolide I and drugs mainly undergoing UGT2B7-catalysed metabolism. Copyright (c) 2015 John Wiley & Sons, Ltd.
Language英语
WOS IDWOS:000367919300004
PublisherWILEY-BLACKWELL
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/171481
Collection中国科学院大连化学物理研究所
Corresponding AuthorWang, Wei-Ming
Affiliation1.Dalian Univ, Affiliated Zhongshan Hosp, Dalian 116001, Liaoning, Peoples R China
2.Shanghai Engineer & Technol Res Ctr Reprod Hlth D, Shanghai Inst Planned Parenthood Res, Key Lab Contracept & Devices Res NPFPC, Shanghai 200032, Peoples R China
3.Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, Tianjin 300070, Peoples R China
4.Chinese Acad Sci, Joint Ctr Translat Med, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
5.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China
6.Chinese Acad Sci, Joint Ctr Translat Med, Dalian Inst Chem Phys, Dalian 116001, Peoples R China
7.Dalian Med Univ, Inst Integrat Med, Dalian 116044, Peoples R China
8.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Liaoning, Peoples R China
9.Tianjin Med Univ, Sch Basic Med Sci, Dept Microbiol, Tianjin 300070, Peoples R China
Recommended Citation
GB/T 7714
Zhang, Qian,Cao, Yun-Feng,Ran, Rui-Xue,et al. Strong Specific Inhibition of UDP-glucuronosyltransferase 2B7 by Atractylenolide I and III[J]. PHYTOTHERAPY RESEARCH,2016,30(1):25-30.
APA Zhang, Qian.,Cao, Yun-Feng.,Ran, Rui-Xue.,Li, Rong-Shan.,Wu, Xue.,...&Wang, Wei-Ming.(2016).Strong Specific Inhibition of UDP-glucuronosyltransferase 2B7 by Atractylenolide I and III.PHYTOTHERAPY RESEARCH,30(1),25-30.
MLA Zhang, Qian,et al."Strong Specific Inhibition of UDP-glucuronosyltransferase 2B7 by Atractylenolide I and III".PHYTOTHERAPY RESEARCH 30.1(2016):25-30.
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