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Título: | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
Autor: | Mosolygó, Tímea; Kincses, Annamária; Csonka, Andrea; Tönki, Ádám Szabó; Witek, Karolina; Sanmartín, Carmen; Marć, Małgorzata Anna; Handzlik, Jadwiga; Kieć-Kononowicz, Katarzyna; Domínguez-Álvarez, Enrique CSIC ORCID ; Spengler, Gabriella | Palabras clave: | Selenocompounds Selenoesters AcrAB-TolC efflux pump Chlamydia trachomatis D Escherichia coli K-12 AG100 Staphylococcus aureus |
Fecha de publicación: | 16-abr-2019 | Editor: | Multidisciplinary Digital Publishing Institute | Citación: | Molecules 24(8): 1487 (2019) | Resumen: | Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in <i>Staphylococcus aureus</i>, methicillin resistant <i>S. aureus</i> (MRSA), <i>Enterococcus faecalis, Escherichia coli</i>, and <i>Chlamydia trachomatis</i> D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens. | Versión del editor: | http://dx.doi.org/10.3390/molecules24081487 | URI: | http://hdl.handle.net/10261/180727 | DOI: | 10.3390/molecules24081487 | ISSN: | 1420-3049 |
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