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Article

Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria

1
Laboratory of Organic and Pharmaceutical Chemistry (LQOF), Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
2
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4450-208 Matosinhos, Portugal
3
Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Faculty of Medicine, University of Szeged, Semmelweis utca 6, 6725 Szeged, Hungary
*
Authors to whom correspondence should be addressed.
Academic Editor: Françoise Van Bambeke
Received: 1 April 2021 / Revised: 28 April 2021 / Accepted: 17 May 2021 / Published: 19 May 2021
(This article belongs to the Special Issue The Role of Efflux Pump Inhibitor in Bacterial Multidrug Resistance)
The emergence of multidrug and extensively drug-resistant pathogenic bacteria able to resist to the action of a wide range of antibiotics is becoming a growing problem for public health. The search for new compounds with the potential to help in the reversion of bacterial resistance plays an important role in current medicinal chemistry research. Under this scope, bacterial efflux pumps are responsible for the efflux of antimicrobials, and their inhibition could reverse resistance. In this study, the multidrug resistance reversing activity of a series of xanthones was investigated. Firstly, docking studies were performed in the AcrAB-TolC efflux pump and in a homology model of the NorA pump. Then, the effects of twenty xanthone derivatives on bacterial growth were evaluated in Staphylococcus aureus 272123 and in the acrA gene-inactivated mutant Salmonella enterica serovar Typhimurium SL1344 (SE03). Their efflux pump inhibitory properties were assessed using real-time fluorimetry. Assays concerning the activity of these compounds towards the inhibition of biofilm formation and quorum sensing have also been performed. Results showed that a halogenated phenylmethanamine xanthone derivative displayed an interesting profile, as far as efflux pump inhibition and biofilm formation were concerned. To the best of our knowledge, this is the first report of xanthones as potential efflux pump inhibitors. View Full-Text
Keywords: xanthones; efflux pump; multidrug resistance; antibacterial activity; biofilm inhibition; quorum sensing xanthones; efflux pump; multidrug resistance; antibacterial activity; biofilm inhibition; quorum sensing
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MDPI and ACS Style

Durães, F.; Resende, D.I.S.P.; Palmeira, A.; Szemerédi, N.; Pinto, M.M.M.; Spengler, G.; Sousa, E. Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria. Antibiotics 2021, 10, 600. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10050600

AMA Style

Durães F, Resende DISP, Palmeira A, Szemerédi N, Pinto MMM, Spengler G, Sousa E. Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria. Antibiotics. 2021; 10(5):600. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10050600

Chicago/Turabian Style

Durães, Fernando, Diana I.S.P. Resende, Andreia Palmeira, Nikoletta Szemerédi, Madalena M.M. Pinto, Gabriella Spengler, and Emília Sousa. 2021. "Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria" Antibiotics 10, no. 5: 600. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10050600

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