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Article

Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors

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Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
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CIIMAR-Interdisciplinary Centre of Marine and Environmental Research, University of Porto, Novo Edifício do Terminal de Cruzeiros do Porto de Leixões, Avenida General Norton de Matos, S/N, 4450-208 Matosinhos, Portugal
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UCIBIO-REQUIMTE, Laboratory of Toxicology, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
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ICBAS–Institute of Biomedical Sciences Abel Salazar, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
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Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Faculty of Medicine, University of Szeged, Semmelweis utca 6, 6725 Szeged, Hungary
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Department of Molecular Biology, ICBAS–Instituto de Ciências Biomédicas Abel Salazar, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
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Bioengineering & Synthetic Microbiology, I3S–Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal
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Authors to whom correspondence should be addressed.
Academic Editors: Eduarda M. P. Silva and Diana Cláudia Pinto
Pharmaceuticals 2021, 14(6), 572; https://doi.org/10.3390/ph14060572
Received: 31 May 2021 / Revised: 11 June 2021 / Accepted: 14 June 2021 / Published: 15 June 2021
The overexpression of efflux pumps is one of the causes of multidrug resistance, which leads to the inefficacy of drugs. This plays a pivotal role in antimicrobial resistance, and the most notable pumps are the AcrAB-TolC system (AcrB belongs to the resistance-nodulation-division family) and the NorA, from the major facilitator superfamily. In bacteria, these structures can also favor virulence and adaptation mechanisms, such as quorum-sensing and the formation of biofilm. In this study, the design and synthesis of a library of thioxanthones as potential efflux pump inhibitors are described. The thioxanthone derivatives were investigated for their antibacterial activity and inhibition of efflux pumps, biofilm formation, and quorum-sensing. The compounds were also studied for their potential to interact with P-glycoprotein (P-gp, ABCB1), an efflux pump present in mammalian cells, and for their cytotoxicity in both mouse fibroblasts and human Caco-2 cells. The results concerning the real-time ethidium bromide accumulation may suggest a potential bacterial efflux pump inhibition, which has not yet been reported for thioxanthones. Moreover, in vitro studies in human cells demonstrated a lack of cytotoxicity for concentrations up to 20 µM in Caco-2 cells, with some derivatives also showing potential for P-gp modulation. View Full-Text
Keywords: thioxanthones; antimicrobial resistance; efflux pumps; biofilm; quorum-sensing thioxanthones; antimicrobial resistance; efflux pumps; biofilm; quorum-sensing
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MDPI and ACS Style

Durães, F.; Palmeira, A.; Cruz, B.; Freitas-Silva, J.; Szemerédi, N.; Gales, L.; da Costa, P.M.; Remião, F.; Silva, R.; Pinto, M.; Spengler, G.; Sousa, E. Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors. Pharmaceuticals 2021, 14, 572. https://doi.org/10.3390/ph14060572

AMA Style

Durães F, Palmeira A, Cruz B, Freitas-Silva J, Szemerédi N, Gales L, da Costa PM, Remião F, Silva R, Pinto M, Spengler G, Sousa E. Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors. Pharmaceuticals. 2021; 14(6):572. https://doi.org/10.3390/ph14060572

Chicago/Turabian Style

Durães, Fernando, Andreia Palmeira, Bárbara Cruz, Joana Freitas-Silva, Nikoletta Szemerédi, Luís Gales, Paulo M. da Costa, Fernando Remião, Renata Silva, Madalena Pinto, Gabriella Spengler, and Emília Sousa. 2021. "Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors" Pharmaceuticals 14, no. 6: 572. https://doi.org/10.3390/ph14060572

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