| Revista: | Brazilian Journal of Pharmaceutical Sciences |
| Base de datos: | PERIÓDICA |
| Número de sistema: | 000452218 |
| ISSN: | 1984-8250 |
| Autores: | Li, Jing Xin1 Wang, Yu2 Hao, Ying1 Huo, Xiao Kui1 Sun, Cheng Peng1 Zhao, Xiao Xia1 Wang, Jin Cheng1 Zhang, Jian Bin1 Ning, Jing1 Tian, Xiang Ge1 Wang, Chao1 Zhao, Wen Yu1 Lv, Xia1 Li, Ya Chen1 Ma, Xiao Chi1 |
| Instituciones: | 1Dalian Medical University, School of Public Health, Dalian, Liaoning. China 2The Second Hospital of Dalian Medical University, Department of Pharmacy, Dalian, Liaoning. China |
| Año: | 2022 |
| Volumen: | 58 |
| País: | Brasil |
| Idioma: | Inglés |
| Tipo de documento: | Artículo |
| Enfoque: | Aplicado, descriptivo |
| Resumen en inglés | Gut bacterial β-glucuronidase (GUS) can reactivate xenobiotics that exert enterohepatic circulation- triggered gastrointestinal tract toxicity. GUS inhibitors can alleviate drug-induced enteropathy and improve treatment outcomes. We evaluated the inhibitory effect of Polygonum cuspidatum Siebold & Zucc. and its major constituents against Escherichia coli GUS (EcGUS), and characterized the inhibitory mechanism of each of the components. Trans-resveratrol 4’-O-β-D-glucopyranoside (HZ-1) and (-)-epicatechin gallate (HZ-2) isolated from P. cuspidatum were identified as the key components and potent inhibitors. These two components displayed strong to moderate inhibitory effects on EcGUS, with Ki values of 9.95 and 1.95 μM, respectively. Results from molecular docking indicated that HZ-1 and HZ-2 could interact with the key residues Asp163, Ser360, Ile 363, Glu413, Glu504, and Lys 568 of EcGUS via hydrogen bonding. Our findings demonstrate the inhibitory effect of P. cuspidatum and its two components on EcGUS, which supported the further evaluation and development of P. cuspidatum and its two active components as novel candidates for alleviating drug-induced damage in the mammalian gut |
| Disciplinas: | Biología, Química |
| Palabras clave: | Fitoquímica, Briofitas y pteridofitas, Helechos, Inhibidores enzimáticos, Beta-glucuronidasa, Polygonum cuspidatum, Polygonaceae |
| Keyword: | Phytochemistry, Briophytes and pteridophytes, Ferns, Beta-glucuronidase, Enzyme inhibitors, Polygonum cuspidatum, Polygonaceae |
| Texto completo: | Texto completo (Ver HTML) Texto completo (Ver PDF) |
