Chalcone Inhibitors of the NorA Efflux Pump in Staphylococcus Aureus Whole Cells and Enriched Everted Membrane Vesicles

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2012 Jun 12

PMID 22682300

Citations 25

Authors

Jes Gitz Holler

Hans-Christian Slotved

Per Molgaard

Carl Erik Olsen

Soren Brogger Christensen

Affiliations

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Abstract

A library of 117 chalcones was screened for efflux pump inhibitory (EPI) activity against NorA mediated ethidium bromide efflux. Five of the chalcones (5-7, 9, and 10) were active and two chalcones (9 and 10) were equipotent to reserpine with IC(50)-values of 9.0 and 7.7 μM, respectively. Twenty chalcones were subsequently proved to be inhibitors of the NorA efflux pump in everted membrane vesicles. Compounds 5, 7, and 9 synergistically increased the effect of ciprofloxacin on Staphylococcus aureus. Our results suggest that chalcones might be developed into drugs for overcoming multidrug resistance based on efflux transporters of microorganisms.

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