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Bioorg Chem ; 73: 37-42, 2017 08.
Artículo en Inglés | MEDLINE | ID: mdl-28599132

RESUMEN

Quorum sensing (QS) is a cell-to-cell signaling communication system that controls the virulence behavior of a broad spectrum of bacterial pathogens, participating also in the development of biofilms, responsible of the antibiotic ineffectiveness in many infections. Therefore, QS system is an attractive target for antimicrobial therapy. In this study, we compare the effect of seven structurally related coumarins against bacterial growth, biofilm formation and elastase activity of Pseudomonas aeruginosa. In addition, the anti-pathogenic capacity of the seven coumarins was evaluated on the wild type and the biosensor strain of Chromobacterium violaceum. The comparative study of coumarins showed that molecules with hydroxyl groups on the aromatic ring displayed higher activity on the inhibition of biofilm formation of P. aeruginosa over coumarins with substituents in positions 3 and 4 or without the double 3,4-bond. These 3 or 4-hydroxylated positions caused a decrease in the anti-biofilm activity obtained for coumarin. However, the hydroxyl group in position 3 of the pyrone ring was important for the inhibition of C. violaceum QS and elastolytic activity of P. aeruginosa. The effects observed were active independently of any effect on growth. According to our results, coumarin and its hydroxylated derivatives represent an interesting group of compounds to use as anti-virulence agents against the human pathogen P. aeruginosa.


Asunto(s)
Antibacterianos/farmacología , Chromobacterium/efectos de los fármacos , Cumarinas/farmacología , Pseudomonas aeruginosa/efectos de los fármacos , Percepción de Quorum/efectos de los fármacos , Antibacterianos/síntesis química , Antibacterianos/química , Chromobacterium/química , Cumarinas/síntesis química , Cumarinas/química , Relación Dosis-Respuesta a Droga , Indoles/antagonistas & inhibidores , Indoles/metabolismo , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad
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