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Regioselective glucuronidation of oxyresveratrol, a natural hydroxystilbene, by human liver and intestinal microsomes and recombinant ugts
Hu N.; Mei M.; Ruan J.; Wu W.; Wang Y.; Yan R.
2014
Source PublicationDrug Metabolism and Pharmacokinetics
Volume29Issue:3Pages:229
Abstract

Oxyresveratrol (OXY) is a natural hydroxystilbene that shows similar bioactivity but better water solubility than resveratrol. This study aims to characterize its glucuronidation kinetics in human liver (HLMs) and intestinal (HIMs) microsomes and identify the main UDP-glucuronosyltransferase (UGT) isoforms involved. Three and four mono-glucuronides of OXY were generated in HIMs and HLMs, respectively, with oxyresveratrol-2-O-β-D-glucuronosyl (G4) as the major metabolite in both organs. The kinetics of G4 formation fit a sigmoidal model in HLMs and biphasic kinetics in HIMs. Multiple UGT isoforms catalyzed G4 formation with the highest activity observed with UGT1A9 followed by UGT1A1. G4 formation by both isoforms followed substrate inhibition kinetics. Propofol (UGT1A9 inhibitor) effectively blocked G4 generation in HLMs (IC 50 63.7 ± 11.6 μM), whereas the UGT1A1 inhibitor bilirubin only produced partial inhibition in HLMs and HIMs. These findings shed light on the metabolic mechanism of OXY and arouse awareness of drug interactions. Copyright © 2014 by the Japanese Society for the Study of Xenobiotics (JSSX).

KeywordGlucuronidation Kinetics Oxyresveratrol Oxyresveratrol-2-o-β-d-glucuronosyl Regioselectivity Ugt1a9 Uridine Diphospho-glucuronosyltransferase (Ugts)
DOI10.2133/dmpk.DMPK-13-RG-102
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000337641200002
The Source to ArticleScopus
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Cited Times [WOS]:5   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, 999078, Macau
2.Department of Clinical Pharmacy, First People's Hospital of Changzhou, Changzhou, China
3.School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China
Recommended Citation
GB/T 7714
Hu N.,Mei M.,Ruan J.,et al. Regioselective glucuronidation of oxyresveratrol, a natural hydroxystilbene, by human liver and intestinal microsomes and recombinant ugts[J]. Drug Metabolism and Pharmacokinetics,2014,29(3):229.
APA Hu N.,Mei M.,Ruan J.,Wu W.,Wang Y.,&Yan R..(2014).Regioselective glucuronidation of oxyresveratrol, a natural hydroxystilbene, by human liver and intestinal microsomes and recombinant ugts.Drug Metabolism and Pharmacokinetics,29(3),229.
MLA Hu N.,et al."Regioselective glucuronidation of oxyresveratrol, a natural hydroxystilbene, by human liver and intestinal microsomes and recombinant ugts".Drug Metabolism and Pharmacokinetics 29.3(2014):229.
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