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MSG: A POTENT AND HIGHLY SELECTIVE BACTERIAL BETA-GLUCURO-NIDASE INHIBITOR
Wei, Bin1; Yang, Wei2; Yan, Ru3
2017-01
Source PublicationDRUG METABOLISM AND PHARMACOKINETICS
ISSN1347-4367
Volume32Issue:1Pages:S57-S57
Abstract

Gut bacterial beta-glucuronidases play important roles in generating many endogenous molecules of biological significance and enterohepatic recirculation of xenobiotics. Recent studies showed that selective inhibition of gut bacterial beta-glucuronidases could alleviate gastrointestinal toxicity in mice caused by irinotecan[1] and diclofenac[2]. Although largely similar in structure, beta-glucuronidases from different gut bacteria may exhibit markedly different priorities for inhibition[3]. In this study, we screened beta-glucuronidase inhibitors from constituents originated from some commonly used Chinese medicines using a cell-free assay which measures p-nitrophenol production from p-nitrophenol-beta-D-glucopyranoside by proteins of human gut microbiota or bacterial isolates. The effect of the compounds on the growth of the gut microbiota was evaluated by measuring OD600. Amoxapine, a recently reported beta-glucuronidase inhibitor[4], was used as a control. Among tens of compounds tested, only MSG showed potent inhibitory effect towards beta-glucuronidase from human gut microbiota with an IC50 of 13.65 μM, comparing to 70.91 μM of amoxapine. Moreover, MSG only slightly inhibited the growth of human gut microbiota (<20% inhibition at 64 μM). More interestingly, MSG (100 μM) completely inhibited beta-glucuronidases from Helix pomatia and Streptococcus gallolyticus 53, partially inhibited beta-glucuronidases from Streptococcus agalactiae 136 and Staphylococcus xylosus 171, while not inhibited beta-glucuronidase from Escherichia coli 39. In contrast, amoxapine (100 μM) completely inhibited the beta-glucuronidase activity of Escherichia coli 39, but not affected that of Helix pomatia and other tested bacterial isolates. Taken together, MSG shows potent inhibitory effects towards microbial beta-glucuronidase activity without significantly affecting bacterial growth. The application of this compound in reducing drug-related gastrointestinal toxicity warrants further study.

DOI10.1016/j.dmpk.2016.10.231
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000397013800189
PublisherJAPANESE SOC STUDY XENOBIOTICS
The Source to ArticleWOS
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Cited Times [WOS]:0   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Zhejiang University of Technology
2.Hong Kong Baptist University
3.University of Macau
Recommended Citation
GB/T 7714
Wei, Bin,Yang, Wei,Yan, Ru. MSG: A POTENT AND HIGHLY SELECTIVE BACTERIAL BETA-GLUCURO-NIDASE INHIBITOR[J]. DRUG METABOLISM AND PHARMACOKINETICS,2017,32(1):S57-S57.
APA Wei, Bin,Yang, Wei,&Yan, Ru.(2017).MSG: A POTENT AND HIGHLY SELECTIVE BACTERIAL BETA-GLUCURO-NIDASE INHIBITOR.DRUG METABOLISM AND PHARMACOKINETICS,32(1),S57-S57.
MLA Wei, Bin,et al."MSG: A POTENT AND HIGHLY SELECTIVE BACTERIAL BETA-GLUCURO-NIDASE INHIBITOR".DRUG METABOLISM AND PHARMACOKINETICS 32.1(2017):S57-S57.
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