AI Article Synopsis

  • Bacterial resistance, particularly in Staphylococcus aureus, poses a serious global public health challenge, driving researchers to explore new solutions such as efflux pump inhibitors.
  • A newly synthesized chalcone was tested for its antibacterial properties, revealing it does not have direct antibacterial activity, but it can enhance the effectiveness of existing antibiotics like ciprofloxacin and ethidium bromide.
  • Molecular docking simulations indicate that the chalcone likely functions as a MepA efflux pump inhibitor, targeting the same binding site as known inhibitors.

Article Abstract

Bacterial resistance has become a global concern for public health agencies. Various resistance mechanisms found in Staphylococcus aureus strains grant this bacterium resistance to a wide range of antibiotics, contributing to the rise in human mortality worldwide. Resistance mediated by efflux pumps is one of the most prevalent mechanisms in multi-resistant bacteria, which has aroused the interest of several researchers in the search for possible efflux pump inhibitors. In view of the aforementioned considerations, it is important that new strategies, such as the synthesis of chalcones, be made available as a viable strategy in antimicrobial therapy. In this study, the synthesized chalcone (2E)-1-(3'-aminophenyl)-3-(4-dimethylaminophenyl)-prop-2-en-1-one was tested for its antibacterial activity, focusing on antibiotic modification and the inhibition of the MepA efflux pump present in S. aureus strain K2068. The broth microdilution method, using microdilution plates, was employed in microbiological tests to determine the minimum inhibitory concentration of the chalcone, antibiotics, and ethidium bromide. The results show that while the chalcone did not exhibit direct antibacterial activity, it synergistically enhanced the effects of ciprofloxacin and ethidium bromide, as evidenced by the reduction in MICs. In addition, computer simulations of molecular docking demonstrate that the tested chalcone acts on the same binding site as the efflux pump inhibitor chlorpromazine, interacting with essentially the same residues. These data suggest that the chalcone may act as a MepA inhibitor.

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Source
http://dx.doi.org/10.1007/s12223-024-01221-9DOI Listing

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