The activity of 16 new hydantoin compounds on the intrinsic and overexpressed efflux pump system of Staphylococcus aureus

Anna Dymek, Ana Armada, Jadwiga Handzlik, Miguel Viveiros, Gabriella Spengler, Joseph Molnar, Katarzyna Kieć-Kononowicz, Leonard Amaral

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Aim: To evaluate a new series of 16 hydantoin derivatives for activity against the intrinsic and overexpressed efflux pumps of the ATTC 25923 Staphylococcus aureus and the clinical Staphylococcus aureus HPV-107 strain, respectively. Materials and Methods: The hydantoin compounds were evaluated for activity against the efflux pumps of the ATTC 25923 S. aureus and the clinical S. aureus HPV-107 strains by the aid of the automated ethidium bromide method. Compounds that inhibited the efflux pumps of either strain were evaluated for ability to reduce or reverse resistance of these strains to oxacillin. Results: Although most of the hydantoins inhibited the efflux pumps of the ATTC strain, none reduced the resistance of this strain to oxacillin. In contrast, the inhibition of the Qac efflux pump present in HPV-107 was inhibited to some degree, by much higher concentrations of the hydantoin compounds than that needed for similar activity against the ATTC strain; only hydantoin PI8a significantly reduced the minimum inhibitory concentration of oxacillin against the HPV-107 strain. Conclusion: Hydantoin compound PI8a may have potential for therapy of a methicillin-resistant S. aureus infection whose multidrug-resistant phenotype is due to overexpression of an efflux pump.

Original languageEnglish
Pages (from-to)223-229
Number of pages7
JournalIn Vivo
Volume26
Issue number2
Publication statusPublished - Mar 1 2012

Keywords

  • Hydantoin derivatives
  • Inhibition of efflux pumps
  • Intrinsic efflux pump
  • Oxacillin
  • Qac efflux pump
  • Reversal of resistance to oxacillin
  • Staphylococcus aureus ATCC 25923 wild-type
  • Staphylococcus aureus HPV-107

ASJC Scopus subject areas

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

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    Dymek, A., Armada, A., Handzlik, J., Viveiros, M., Spengler, G., Molnar, J., Kieć-Kononowicz, K., & Amaral, L. (2012). The activity of 16 new hydantoin compounds on the intrinsic and overexpressed efflux pump system of Staphylococcus aureus. In Vivo, 26(2), 223-229.