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Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance
The emergence of drug-resistant pathogens leads to a gradual decline in the efficacy of many antibacterial agents, which poses a serious problem for proper therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules,...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763688/ https://www.ncbi.nlm.nih.gov/pubmed/33322639 http://dx.doi.org/10.3390/antibiotics9120896 |
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author | Szemerédi, Nikoletta Kincses, Annamária Rehorova, Katerina Hoang, Lan Salardón-Jiménez, Noemi Sevilla-Hernández, Clotilde Viktorová, Jitka Domínguez-Álvarez, Enrique Spengler, Gabriella |
author_facet | Szemerédi, Nikoletta Kincses, Annamária Rehorova, Katerina Hoang, Lan Salardón-Jiménez, Noemi Sevilla-Hernández, Clotilde Viktorová, Jitka Domínguez-Álvarez, Enrique Spengler, Gabriella |
author_sort | Szemerédi, Nikoletta |
collection | PubMed |
description | The emergence of drug-resistant pathogens leads to a gradual decline in the efficacy of many antibacterial agents, which poses a serious problem for proper therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules, drug inactivation, or release of the drug into the extracellular space by efflux pumps (EPs). In previous studies, selenoesters have proved to be promising derivatives with a noteworthy antimicrobial activity. On the basis of these results, two series of novel selenoesters were synthesized to achieve more potent antibacterial activity on Gram-positive and Gram-negative bacteria. Fifteen selenoesters (eight ketone-selenoesters and seven cyano-selenoesters) were investigated with regards to their efflux pump-inhibiting, anti-quorum-sensing (QS), and anti-biofilm effects in vitro. According to the results of the antibacterial activity, the ketone-selenoesters proved to be more potent antibacterial compounds than the cyano-selenoesters. With regard to efflux pump inhibition, one cyano-selenoester on methicillin-resistant S. aureus and one ketone-selenoester on Salmonella Typhimurium were potent inhibitors. The biofilm inhibitory capacity and the ability of the derivatives to disrupt mature biofilms were noteworthy in all the experimental systems applied. Regarding QS inhibition, four ketone-selenoesters and three cyano-selenoesters exerted a noteworthy effect on Vibrio campbellii strains. |
format | Online Article Text |
id | pubmed-7763688 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-77636882020-12-27 Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance Szemerédi, Nikoletta Kincses, Annamária Rehorova, Katerina Hoang, Lan Salardón-Jiménez, Noemi Sevilla-Hernández, Clotilde Viktorová, Jitka Domínguez-Álvarez, Enrique Spengler, Gabriella Antibiotics (Basel) Article The emergence of drug-resistant pathogens leads to a gradual decline in the efficacy of many antibacterial agents, which poses a serious problem for proper therapy. Multidrug resistance (MDR) mechanisms allow resistant bacteria to have limited uptake of drugs, modification of their target molecules, drug inactivation, or release of the drug into the extracellular space by efflux pumps (EPs). In previous studies, selenoesters have proved to be promising derivatives with a noteworthy antimicrobial activity. On the basis of these results, two series of novel selenoesters were synthesized to achieve more potent antibacterial activity on Gram-positive and Gram-negative bacteria. Fifteen selenoesters (eight ketone-selenoesters and seven cyano-selenoesters) were investigated with regards to their efflux pump-inhibiting, anti-quorum-sensing (QS), and anti-biofilm effects in vitro. According to the results of the antibacterial activity, the ketone-selenoesters proved to be more potent antibacterial compounds than the cyano-selenoesters. With regard to efflux pump inhibition, one cyano-selenoester on methicillin-resistant S. aureus and one ketone-selenoester on Salmonella Typhimurium were potent inhibitors. The biofilm inhibitory capacity and the ability of the derivatives to disrupt mature biofilms were noteworthy in all the experimental systems applied. Regarding QS inhibition, four ketone-selenoesters and three cyano-selenoesters exerted a noteworthy effect on Vibrio campbellii strains. MDPI 2020-12-11 /pmc/articles/PMC7763688/ /pubmed/33322639 http://dx.doi.org/10.3390/antibiotics9120896 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Szemerédi, Nikoletta Kincses, Annamária Rehorova, Katerina Hoang, Lan Salardón-Jiménez, Noemi Sevilla-Hernández, Clotilde Viktorová, Jitka Domínguez-Álvarez, Enrique Spengler, Gabriella Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title | Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title_full | Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title_fullStr | Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title_full_unstemmed | Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title_short | Ketone- and Cyano-Selenoesters to Overcome Efflux Pump, Quorum-Sensing, and Biofilm-Mediated Resistance |
title_sort | ketone- and cyano-selenoesters to overcome efflux pump, quorum-sensing, and biofilm-mediated resistance |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763688/ https://www.ncbi.nlm.nih.gov/pubmed/33322639 http://dx.doi.org/10.3390/antibiotics9120896 |
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