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Article

Chalcones Isolated from Arrabidaea brachypoda Flowers as Inhibitors of NorA and MepA Multidrug Efflux Pumps of Staphylococcus aureus

1
Laboratory of Research in Microbiology, Federal University of Piaui, Teresina, Piaui 64049-550, Brazil
2
Laboratory of Advanced Studies in Phytomedicines, Federal University of Maranhão, São Luís, Maranhão 65080-805, Brazil
3
Laboratory of Organic Geochemistry, Federal University of Piaui, Teresina, Piauí 64049-550, Brazil
4
Laboratory of Genetics of Microorganisms, Federal University of Paraiba, Joao Pessoa, Paraiba 58051-900, Brazil
5
Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará 63105-010, Brazil
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Department of Medicine, Division of Infectious Diseases, Wayne State University School of Medicine, Detroit, MI 48201, USA
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Laboratory of Microbiology and Molecular Biology, Regional University of Cariri, Crato, Ceará 64049-550, Brazil
8
Faculty of Medicine, University of Porto, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
9
Institute for Research and Innovation in Health (i3S), University of Porto, 4200-135 Porto, Portugal
*
Authors to whom correspondence should be addressed.
Received: 20 May 2020 / Revised: 16 June 2020 / Accepted: 18 June 2020 / Published: 20 June 2020
(This article belongs to the Special Issue The Role of Efflux Pump Inhibitor in Bacterial Multidrug Resistance)
Bacterial resistance to antibiotics has become a public health issue around the world. The present study aimed to evaluate the antibacterial activity of chalcones isolated from flowers of Arrabidaea brachypoda, and their potential as efflux pump inhibitors of Staphylococcus aureus efflux pumps. Microdilution assays were performed with natural products from A. brachypoda. Chalcones 1, 3, 4, and 5 did not show intrinsic antimicrobial activity against all S. aureus strains tested, but they were able to potentiate the Norfloxacin action against the SA1199-B (norA) strain, with a better modulating action for the 4 trimethoxylated chalcone. All chalcones were also able to potentiate the action of EtBr against SA1199-B strain, suggesting a potential NorA inhibition. Moreover, chalcone 4 was able to interfere in the activity of MepA, and interfered weakly in the QacA/B activity. Molecular docking analyzes showed that tested chalcones are capable of binding in the hydrophobic cavity of NorA and MepA, in the same Norfloxacin binding site, indicating that chalcone 4 compete with the antibiotic for the same NorA and MepA binding sites. Association of chalcone 4 with Norfloxacin could be an alternative against multidrug resistant S. aureus over-productive of NorA or MepA. View Full-Text
Keywords: Arrabidaea brachypoda; Chalcone; antimicrobial activity; efflux pumps; efflux pump inhibitors; resistance to antibiotics Arrabidaea brachypoda; Chalcone; antimicrobial activity; efflux pumps; efflux pump inhibitors; resistance to antibiotics
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MDPI and ACS Style

Rezende-Júnior, L.M.; Andrade, L.M.d.S.; Leal, A.L.A.B.; Mesquita, A.B.d.S.; Santos, A.L.P.d.A.d.; Neto, J.d.S.L.; Siqueira-Júnior, J.P.; Nogueira, C.E.S.; Kaatz, G.W.; Coutinho, H.D.M.; Martins, N.; da Rocha, C.Q.; Barreto, H.M. Chalcones Isolated from Arrabidaea brachypoda Flowers as Inhibitors of NorA and MepA Multidrug Efflux Pumps of Staphylococcus aureus. Antibiotics 2020, 9, 351. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060351

AMA Style

Rezende-Júnior LM, Andrade LMdS, Leal ALAB, Mesquita ABdS, Santos ALPdAd, Neto JdSL, Siqueira-Júnior JP, Nogueira CES, Kaatz GW, Coutinho HDM, Martins N, da Rocha CQ, Barreto HM. Chalcones Isolated from Arrabidaea brachypoda Flowers as Inhibitors of NorA and MepA Multidrug Efflux Pumps of Staphylococcus aureus. Antibiotics. 2020; 9(6):351. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060351

Chicago/Turabian Style

Rezende-Júnior, Luís M., Leila M.d.S. Andrade, Antonio L.A.B. Leal, Avilnete B.d.S. Mesquita, Ana L.P.d.A.d. Santos, José d.S.L. Neto, José P. Siqueira-Júnior, Carlos E.S. Nogueira, Glenn W. Kaatz, Henrique D.M. Coutinho, Natália Martins, Cláudia Q. da Rocha, and Humberto M. Barreto 2020. "Chalcones Isolated from Arrabidaea brachypoda Flowers as Inhibitors of NorA and MepA Multidrug Efflux Pumps of Staphylococcus aureus" Antibiotics 9, no. 6: 351. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060351

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