Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 14, Pages 4514-4521Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.05.025
Keywords
Chalcones; Staphylococcus aureus; MRSA; Antibiotic resistance; Antibiotics; Natural compounds
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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 IC50-values of 9.0 and 7.7 mu M, 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. (C) 2012 Elsevier Ltd. All rights reserved.
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