Biological activity of twenty-three hydantoin derivatives on intrinsic efflux pump system of Salmonella enterica serovar enteritidis NCTC 13349

Lisa Machado, Gabriella Spengler, Miguel Evaristo, Jadwiga Handzlik, Joseph Molnár, Miguel Viveiros, Katarzyna Kiec-Kononowicz, Leonard Amaral

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Background: Hydantoin derivatives have important biochemical and pharmacological properties. In the present study, 23 hydantoin compounds were evaluated for their efflux-modulating effects in Salmonella enterica serovar Enteritidis NCTC 13349 using real-time fluorimetry based on the intracellular accumulation of ethidium bromide (EB), a universal substrate of efflux pumps. Materials and Methods: Twenty-three hydantoin derivatives were tested for intrinsic efflux pump modulation in S. enterica Enteritidis NCTC 13349 by an automated real-time fluorimetric method that monitors the intracellular accumulation of ethidium bromide. Results: None of the compounds were found to have antibacterial activities at concentrations as high as 200 mg/l. Among the hydantoin derivatives tested in our study, only compound SZ7 showed efflux modulating activity on S. enterica Enteritidis NCTC 13349 in the assays that contained or omitted glucose as the singular source of metabolic energy. Conclusion: SZ7 is shown to be non-toxic and it could be evaluated to cure an efflux mediated MDR Salmonella infection, furthermore a quantitative activity-structural relationship is also planned in order to determine the site of the SZ7 molecule responsible for its efflux pump inhibitory activity.

Original languageEnglish
Pages (from-to)769-772
Number of pages4
JournalIn Vivo
Volume25
Issue number5
Publication statusPublished - Sep 1 2011

Keywords

  • Automated real-time fluorimetry
  • Efflux pumps
  • Hydantoin compounds
  • Inhibition
  • Metabolic dependent
  • Salmonella enterica serovar enteritidis NCTC 13349

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology

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