4.3 Article

Potentiation of antibiotic activity, and efflux pumps inhibition by (2E)-1-(4-aminophenyl)-3-(4-fluorophenyl)prop-2-en-1-one

期刊

FUNDAMENTAL & CLINICAL PHARMACOLOGY
卷 36, 期 6, 页码 1066-1082

出版社

WILEY
DOI: 10.1111/fcp.12785

关键词

aminochalcone; Antibacterial activity; efflux pump; PA-Fluoride

资金

  1. Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior - CAPES [001]
  2. Fundacao Cearense de Apoio ao Desenvolvimento Cientifico e Tecnologico - FUNCAP [BP4-0172-00075.01.00/20]
  3. Conselho Nacional de Desenvolvimento Cientifico e Tecnologico - CNPq [308178/2021-1]

向作者/读者索取更多资源

In recent years, bacterial resistance to traditional drugs has increased, making it more important to find new effective antibiotics. This study found that PA-Fluorine enhances antibiotic activity and shows synergistic effects against certain resistant bacterial strains. Molecular docking studies showed that PA-Fluorine interacts with specific efflux pumps. ADMET studies also revealed the potential of PA-Fluorine as an efflux pump inhibitor.
In recent years, bacterial resistance to traditional drugs has increased, and the need to find new effective antibiotics to treat infections caused by multidrug-resistant bacteria has consequently become more important. The current study aimed to evaluate the potentiation of antibiotic activity and efflux pumps inhibition by (2E)-1-(4-aminophenyl)-3-(4-fluorophenyl)prop-2-en-1-one (PA-Fluorine) against the standard and resistant bacterial strains of Staphylococcus aureus and Escherichia coli. The association between PA-Fluorine and ampicillin reduced the minimum inhibitory concentration (MIC), showing a synergistic effect against S. aureus. For E. coli, PA-Fluorine did not show any significant results when associated with ampicillin. Ciprofloxacin and chlorpromazine showed synergy with PA-Fluorine on the two studied strains. An efflux pump mechanism was involved in the mechanism of action of chlorpromazine, norfloxacin, and ethidium bromide. PA-Fluorine synergistically modulated norfloxacin and bromide. It was thus concluded that PA-Fluorine has the potential to enhance antibacterial activity when combined with antibiotics. Molecular docking studies showed the effect of intermolecular interactions of PA-Fluorine on the NorA and MepA efflux pumps. Physicochemical and pharmacokinetic properties were also obtained by ADMET studies for this chalcone, which presents be a strong candidate as an efflux pump inhibitor.

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