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Inhibitory Activity of 4-O-Benzoyl-3′-O-(OMethylsinapoyl) Sucrose from Polygala tenuifolia on Escherichia coli β-Glucuronidase
- Source :
- Journal of Microbiology and Biotechnology. 31:1576-1582
- Publication Year :
- 2021
- Publisher :
- Journal of Microbiology and Biotechnology, 2021.
-
Abstract
- Bacterial β-glucuronidase in the intestine is involved in the conversion of 7-ethyl-10- hydroxycamptochecin glucuronide (derived from irinotecan) to 7-ethyl-10-hydroxycamptothecin, which causes intestinal bleeding and diarrhea (side effects of anti-cancer drugs). Twelve compounds (1-12) from Polygala tenuifolia were evaluated in terms of β-glucuronidase inhibition in vitro. 4-O-Benzoyl-3'-O-(O-methylsinapoyl) sucrose (C3) was highly inhibitory at low concentrations. C3 (an uncompetitive inhibitor) exhibited a ki value of 13.4 μM; inhibitory activity increased as the substrate concentration rose. Molecular simulation revealed that C3 bound principally to the Gln158-Tyr160 enzyme loop. Thus, C3 will serve as a lead compound for development of new β- glucuronidase inhibitors.
- Subjects :
- chemistry.chemical_classification
Sucrose
biology
General Medicine
medicine.disease_cause
biology.organism_classification
Applied Microbiology and Biotechnology
In vitro
Glucuronidase
chemistry.chemical_compound
Enzyme
chemistry
Biochemistry
Polygala tenuifolia
medicine
Uncompetitive inhibitor
Glucuronide
Escherichia coli
Biotechnology
Subjects
Details
- ISSN :
- 17388872 and 10177825
- Volume :
- 31
- Database :
- OpenAIRE
- Journal :
- Journal of Microbiology and Biotechnology
- Accession number :
- edsair.doi...........cdbc93a096d3e32a3995ea5d09529577