Selenocompounds as Potent Efflux Pump Inhibitors on Gram‐positive Bacteria
Abstract: In recent years, selenocompounds have gained increasing attention as potential anticancer and antibacterial agents. Several selenoderivatives have been confirmed to act as MDR efflux pump inhibitors, based on their in vitro results against the bacterial AcrAB‐TolC system and the cancer MDR efflux pump P‐glycoprotein. Efflux pumps can contribute directly or indirectly to the virulence of bacteria, as they can reduce the intracellular concentration of antibacterial substances by expelling them out of the cell. The present work aims to study the antibacterial and efflux pump inhibiting properties of four families of selenoesters, namely aspirin‐selenoesters, phenone‐selenoesters, hydroxy‐selenoesters, and benzyl‐selenoesters. The real‐time ethidium bromide accumulation assay confirmed that these derivatives inhibited the efflux systems of methicillin‐resistant Staphylococcus aureus (MRSA) without exerting any antibacterial effect. The relative expression of efflux pump gene of NorA transporter was also monitored in the presence of the most potent derivatives on reference S. aureus, finding that these derivatives could change the expression of the tested efflux pump gene. Regarding the anti‐biofilm activity, aspirin‐selenoesters, benzyl‐selenoesters, and hydroxy‐selenoesters could efficiently inhibit the biofilm production of the MRSA strain. It can be concluded that selenocompounds could act as efflux pump inhibitors, thus reducing the virulence of biofilm‐producing bacteria.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Selenocompounds as Potent Efflux Pump Inhibitors on Gram‐positive Bacteria ; day:20 ; month:11 ; year:2024 ; extent:12
ChemMedChem ; (20.11.2024) (gesamt 12)
- Creator
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Kincses, Annamária
Szemerédi, Nikoletta
Benito‐Lama, Miguel
Dózsai, Dávid
Csonka, Ákos
Domínguez‐Álvarez, Enrique
Spengler, Gabriella
- DOI
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10.1002/cmdc.202400691
- URN
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urn:nbn:de:101:1-2411211309207.238571801586
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:23 AM CEST
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Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Kincses, Annamária
- Szemerédi, Nikoletta
- Benito‐Lama, Miguel
- Dózsai, Dávid
- Csonka, Ákos
- Domínguez‐Álvarez, Enrique
- Spengler, Gabriella
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Thymoquinone’ potent impairment of multidrug-resistant Staphylococcus aureus NorA efflux pump activity
Antibiotic Conjugates with an Artificial MECAM-Based Siderophore Are Potent Agents against Gram-Positive and Gram-Negative Bacterial Pathogens
The reproduction process of Gram-positive protocells
Potent synergy and sustained bactericidal activity of polymyxins combined with Gram-positive only class of antibiotics versus four Gram-negative bacteria
Efflux pump-mediated resistance to new beta lactam antibiotics in multidrug-resistant gram-negative bacteria
Gram-positive bacteria : vaccine vehicles for mucosal immunization
CSF inflammatory markers differ in gram-positive versus gram-negative shunt infections
The distinct translational landscapes of gram-negative Salmonella and gram-positive Listeria
Prognostic factors and monomicrobial necrotizing fasciitis: gram-positive versus gram-negative pathogens
Gram-negative bacteremia induces greater magnitude of inflammatory response than Gram-positive bacteremia
Zielstrukturen der gastrointestinalen Barriere für Gram-positive probiotische Bakterien
Cytokine induction by Gram-positive bacteria
Thymoquinone’ potent impairment of multidrug-resistant Staphylococcus aureus NorA efflux pump activity
Antibiotic Conjugates with an Artificial MECAM-Based Siderophore Are Potent Agents against Gram-Positive and Gram-Negative Bacterial Pathogens
The reproduction process of Gram-positive protocells
Potent synergy and sustained bactericidal activity of polymyxins combined with Gram-positive only class of antibiotics versus four Gram-negative bacteria
Efflux pump-mediated resistance to new beta lactam antibiotics in multidrug-resistant gram-negative bacteria
Gram-positive bacteria : vaccine vehicles for mucosal immunization
CSF inflammatory markers differ in gram-positive versus gram-negative shunt infections
The distinct translational landscapes of gram-negative Salmonella and gram-positive Listeria
Prognostic factors and monomicrobial necrotizing fasciitis: gram-positive versus gram-negative pathogens
Gram-negative bacteremia induces greater magnitude of inflammatory response than Gram-positive bacteremia