Identification of Escherichia coli β-glucuronidase inhibitors from Polygonum cuspidatum Siebold & Zucc.
نویسندگان
چکیده
Gut bacterial β-glucuronidase (GUS) can reactivate xenobiotics that exert enterohepatic circulation- triggered gastrointestinal tract toxicity. GUS inhibitors alleviate drug-induced enteropathy and improve treatment outcomes. We evaluated the inhibitory effect of Polygonum cuspidatum Siebold & Zucc. its major constituents against Escherichia coli (EcGUS), characterized mechanism each components. Trans-resveratrol 4’-O-β-D-glucopyranoside (HZ-1) (-)-epicatechin gallate (HZ-2) isolated from P. were identified as key components potent inhibitors. These two displayed strong to moderate effects on EcGUS, with Ki values 9.95 1.95 μM, respectively. Results molecular docking indicated HZ-1 HZ-2 could interact residues Asp163, Ser360, Ile 363, Glu413, Glu504, Lys 568 EcGUS via hydrogen bonding. Our findings demonstrate which supported further evaluation development active novel candidates for alleviating damage in mammalian gut.
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ژورنال
عنوان ژورنال: Brazilian Journal of Pharmaceutical Sciences
سال: 2022
ISSN: ['2175-9790', '1984-8250']
DOI: https://doi.org/10.1590/s2175-97902022e21394