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1.
Bioorg Chem ; 73: 37-42, 2017 08.
Artigo em Inglês | MEDLINE | ID: mdl-28599132

RESUMO

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.


Assuntos
Antibacterianos/farmacologia , Chromobacterium/efeitos dos fármacos , Cumarínicos/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Percepção de Quorum/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Chromobacterium/química , Cumarínicos/síntese química , Cumarínicos/química , Relação Dose-Resposta a Droga , Indóis/antagonistas & inibidores , Indóis/metabolismo , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
2.
Anaerobe ; 16(4): 345-54, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20451635

RESUMO

Different attempts have been made to improve the health status of humans and animals by increasing the intestinal production of short-chain fatty acids (SCFA) derived from non-digestible carbohydrates fermentation. In this paper we investigate the in vitro production of short-chain fatty acids (SCFA) after addition of inulin, propionibacteria or a combination of both in an experimental model of mice cecal slurries. The development of bacterial genera which are usually stimulated by inulin addition was also investigated. According to our experimental data, acetic acid and butyric acids concentrations increased after incubation in slurries that had no supplements. By contrast, butyric acid concentrations remained in the basal value when supplements were used. Fermentation of only inulin did not increase the concentration of total SCFA. Propionibacterium acidipropionici CRL1198 improved the production of propionic acid in cecal slurries when it was added alone, but the effect was more noticeable in the combination with inulin. A modulation of the global fermentative activity of the cecal microbiota was evidenced by the increase on the ratio propionic acid/SCFA in supplementations with propionibacteria. Statistical analysis of data demonstrated that samples from homogenates with propionibacteria alone or combined with inulin belong to the same cluster. The presence of propionibacteria limited the growth of Bacteroides fragilis and Clostridium hystoliticum groups in slurries with and without inulin. The growth of Bifidobacterium was not modified and the stimulating effect of inulin on lactobacilli disappeared in the presence of propionibacteria. In conclusion, dairy propionibacteria are potential candidates to develop new functional foods helpful to ensure the intestinal production of SCFA during inulin supplementation and to control the overgrowth of bacteria belonging to Bacteroides and Clostridium genera.


Assuntos
Bactérias/crescimento & desenvolvimento , Bactérias/metabolismo , Ceco/microbiologia , Ácidos Graxos Voláteis/metabolismo , Inulina/metabolismo , Animais , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Modelos Animais , Propionibacterium/crescimento & desenvolvimento , Propionibacterium/metabolismo
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