UM  > 中華醫藥研究院
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 BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000397013800189
PublisherJAPANESE SOC STUDY XENOBIOTICS
The Source to ArticleWOS
Fulltext Access
Citation statistics
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.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Wei, Bin]'s Articles
[Yang, Wei]'s Articles
[Yan, Ru]'s Articles
Baidu academic
Similar articles in Baidu academic
[Wei, Bin]'s Articles
[Yang, Wei]'s Articles
[Yan, Ru]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Wei, Bin]'s Articles
[Yang, Wei]'s Articles
[Yan, Ru]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.