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Enhancement of the antibiotic activity by quercetin against Staphylococcus aureus efflux pumps

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Abstract

The objective of this work was to evaluate the inhibitory effect of quercetin on S. aureus Efflux Pumps. The MIC of Quercetin was evaluated through the broth microdilution method, as well as the Efflux Pump inhibition assay through the method of reducing the antibiotic minimum inhibitory concentration as well as that of ethidium bromide. The in silico approach through bioinformatics was performed to demonstrate the molecular mechanism of interaction of the substrate and the binding cavity. The Quercetin inhibition concentration was not clinically relevant. With respect to the reversal of bacterial resistance effect by efflux pump inhibition, this effect was observed with the strains carrying the TetK and NorA pumps. Regarding the interaction between the Quercetin complex and the NorA pump, the extra stability was provided by hydrogen bonds produced by the hydroxyl group.

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Acknowledgements

We are grateful to the Regional University of Cariri - URCA, for providing equipment, materials and laboratory space for conducting the experiments. We also thank the Fundação Cearense de Apoio ao Desenvolvimento Científico e Tecnológico - FUNCAP for funding graduate scholarships and other resources, through the project BP3-0172-00168.01.00/20 SPU 09673071/2020.

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Authors and Affiliations

  1. Laboratory of Semi-Arid Bioprospecting (Lab-Bioprospec), Department of Biological Chemistry, DQB/URCA, Crato, Ceará, Brazil

    Joycy F. S. dos Santos, Cristina R. dos S. Barbosa, Jackelyne R. Scherf, Zildene de S. Silveira, Luiz J. de Lacerda Neto, Luiz M. Barros & Francisco A.B. Cunha

  2. Laboratory of Microbiology and Molecular Biology (LMBM), Department of Biological Chemistry, DQB/URCA, Crato, Ceará, Brazil

    Saulo R. Tintino, Ana R. P. da Silva, Thiago S. de Freitas & Henrique D.M. Coutinho

  3. Laboratory of Pharmacology and Molecular Chemistry (LFQM), Department of Biological Chemistry, DQB/URCA, Crato, Ceará, Brazil

    Irwin Rose de A. Menezes

  4. Department of Biological Chemistry, Microbiology and Molecular Biology Laboratory (LMBM), Regional University of Cariri, DQB/ URCA, Av. Cel. Antonio Luiz, 1161. Pimenta, Crato, Ceará, CEP: 63105-000, Brazil

    Henrique D.M. Coutinho

  5. Department of Molecular Biology, Federal University of Paraíba, João Pessoa, Paraíba, CEP: 58051-900, Brazil

    José P. Siqueira-Júnior

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  1. Joycy F. S. dos Santos
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Correspondence to Henrique D.M. Coutinho.

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dos Santos, J.F.S., Tintino, S.R., da Silva, A.R.P. et al. Enhancement of the antibiotic activity by quercetin against Staphylococcus aureus efflux pumps. J Bioenerg Biomembr 53, 157–167 (2021). https://doi.org/10.1007/s10863-021-09886-4

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