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Article Dans Une Revue Bioorganic Chemistry Année : 2020

Merulinic acid C overcomes gentamicin resistance in Enterococcus faecium

Fernanda Rodrigues-Costa
  • Fonction : Auteur
Juliano Slivinski
  • Fonction : Auteur
Laura Ióca
  • Fonction : Auteur
Ariane Bertonha
  • Fonction : Auteur
Rafael de Felício
  • Fonction : Auteur
Marcos Guilherme Da Cunha
  • Fonction : Auteur
Paulo Vinicius da Mata Madeira
  • Fonction : Auteur
Ana Cauz
  • Fonction : Auteur
Vítor Freire
  • Fonction : Auteur
Cristina Dislich Ropke
  • Fonction : Auteur
Frederico Gueiros-Filho
  • Fonction : Auteur
Roberto Berlinck
  • Fonction : Auteur
Andréa Dessen
  • Fonction : Auteur
  • PersonId : 739646
  • IdHAL : adessen

Résumé

Enterococci are gram-positive, widespread nosocomial pathogens that in recent years have developed resistance to various commonly employed antibiotics. Since finding new infection-control agents based on secondary metabolites from organisms has proved successful for decades, natural products are potentially useful sources of compounds with activity against enterococci. Herein are reported the results of a natural product library screening based on a whole-cell assay against a gram-positive model organism, which led to the isolation of a series of anacardic acids identified by analysis of their spectroscopic data and by chemical derivatizations. Merulinic acid C was identified as the most active anacardic acid derivative obtained against antibiotic-resistant enterococci. Fluorescence microscopy analyses showed that merulinic acid C targets the bacterial membrane without affecting the peptidoglycan and causes rapid cellular ATP leakage from cells. Merulinic acid C was shown to be synergistic with gentamicin against Enterococcus faecium, indicating that this compound could inspire the development of new antibiotic combinations effective against drug-resistant pathogens.
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Dates et versions

hal-02864630 , version 1 (11-06-2020)

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Citer

Fernanda Rodrigues-Costa, Juliano Slivinski, Laura Ióca, Ariane Bertonha, Rafael de Felício, et al.. Merulinic acid C overcomes gentamicin resistance in Enterococcus faecium. Bioorganic Chemistry, 2020, 100, pp.103921. ⟨10.1016/j.bioorg.2020.103921⟩. ⟨hal-02864630⟩
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