Inhibition of UDP-glucuronosyltransferases (UGTs) by bromophenols (BPs).

Catalysis Glucuronosyltransferase / antagonists & inhibitors Humans Hydrocarbons, Brominated / pharmacology Hydrophobic and Hydrophilic Interactions Kinetics Molecular Docking Simulation Phenols / pharmacology Protein Isoforms / metabolism Structure-Activity Relationship
Bromine substituent Bromophenols (BPs) Human UDP-Glucuronosyltransferases (UGTs) Inhibition In vitro-in vivo extrapolation (IVIVE)

Journal

Chemosphere
ISSN: 1879-1298
Titre abrégé: Chemosphere
Pays: England
ID NLM: 0320657

Informations de publication

Date de publication:
Jan 2020
Historique:
received: 24 06 2019
revised: 18 08 2019
accepted: 21 08 2019
pubmed: 1 9 2019
medline: 29 1 2020
entrez: 1 9 2019
Statut: ppublish

Résumé

Bromophenols (BPs) are important organic compounds which have become dominant pollutants during these years. Our present study investigated the potential inhibition behaviour of BPs on the activity of one of the most important phase II drug-metabolizing enzymes (DMEs), UDP-glucuronosyltransferases (UGTs). Recombinant UDP-glucuronosyltransferases (UGTs)-catalyzed glucuronidation of 4-methylumbelliferone (4-MU) was utilized as the probe reaction. 100 μM of BPs was utilized as the inhibition screening concentrations, and the complete inhibition profile of UGT isoforms by BPs was obtained. UGT1A7 was the most vulnerable UGT isoform towards BPs. Some structure-activity relationship for the inhibition of UGTs by BPs was found, and this relationship can be furtherly explained by the hydrophobic contacts of BPs with the activity cavity of UGTs using in silico docking method. The inhibition kinetics determination showed that the inhibition kinetic parameter K

Identifiants

DOI: 10.1016/j.chemosphere.2019.124645 PMID: 31472352
pubmed: 31472352
pii: S0045-6535(19)31869-7
doi: 10.1016/j.chemosphere.2019.124645
pii:
doi:

Substances chimiques

Hydrocarbons, Brominated 0
Phenols 0
Protein Isoforms 0
Glucuronosyltransferase EC 2.4.1.17

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

124645

Informations de copyright

Copyright © 2019 Elsevier Ltd. All rights reserved.

Auteurs

Feige Wang (F)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China.

Shang Wang (S)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China.

Kai Yang (K)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China; Tianjin Key Laboratory of Environment, Nutrition and Public Health, Tianjin, China; National Demonstration Center for Experimental Preventive Medicine Education, Tianjin Medical University, Tianjin, 300070, China; Tianjin Center for International Collaborative Research in Environment, Nutrition and Public Health, Tianjin, China.

Yong-Zhe Liu (YZ)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China; Tianjin Key Laboratory of Environment, Nutrition and Public Health, Tianjin, China; National Demonstration Center for Experimental Preventive Medicine Education, Tianjin Medical University, Tianjin, 300070, China; Tianjin Center for International Collaborative Research in Environment, Nutrition and Public Health, Tianjin, China.

Kun Yang (K)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China; Tianjin Key Laboratory of Environment, Nutrition and Public Health, Tianjin, China; National Demonstration Center for Experimental Preventive Medicine Education, Tianjin Medical University, Tianjin, 300070, China; Tianjin Center for International Collaborative Research in Environment, Nutrition and Public Health, Tianjin, China.

Yao Chen (Y)

Shenyang Mental Health Center, Shenyang, Liaoning Province, China.

Zhong-Ze Fang (ZZ)

Department of Toxicology and Sanitary Chemistry, School of Public Health, Tianjin Medical University, Tianjin, 300070, China; Tianjin Key Laboratory of Environment, Nutrition and Public Health, Tianjin, China; National Demonstration Center for Experimental Preventive Medicine Education, Tianjin Medical University, Tianjin, 300070, China; Tianjin Center for International Collaborative Research in Environment, Nutrition and Public Health, Tianjin, China. Electronic address: fangzhongze@tmu.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Catalyse › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Glycosyltransferase › Hexosyltransferases › Glucuronosyltransferase › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures halogénés › Hydrocarbures bromés › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Phénomènes chimiques › Interactions hydrophobes et hydrophiles › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures cycliques › Hydrocarbures aromatiques › Dérivés du benzène › Phénols › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Isoformes de protéines › Inhibition of UDP-glucuronosyltransferases...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Inhibition of UDP-glucuronosyltransferases...