Abstract
The activities of two naturally occurring compounds, isobavachalcone and diospyrone, against documented strains and multidrug-resistant (MDR) Gram-negative bacterial isolates were evaluated. The results indicated that the two compounds exhibited intrinsic antibacterial activity against several Gram-negative bacteria, and their activities were significantly improved in the presence of an efflux pump inhibitor (MIC values decreased to below 10 microg/ml). In addition, the activities of isobavachalcone and diospyrone against various strains exhibiting deletions of the major efflux pump components (AcrAB, TolC) were significantly increased. The overall results indicate that isobavachalcone and diospyrone could be candidates for the development of new drugs against MDR strains and that their use in combination with efflux pump inhibitors reinforces their activity.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Bacterial Proteins / metabolism
-
Carrier Proteins / metabolism
-
Chalcones / chemistry
-
Chalcones / pharmacology*
-
Diospyros
-
Drug Discovery
-
Drug Resistance, Bacterial
-
Drug Resistance, Multiple
-
Enterobacter aerogenes / drug effects
-
Enterobacter aerogenes / metabolism
-
Enterobacter cloacae / drug effects
-
Enterobacter cloacae / metabolism
-
Escherichia coli / drug effects
-
Escherichia coli / metabolism
-
Gram-Negative Bacteria / drug effects*
-
Gram-Negative Bacteria / metabolism*
-
Klebsiella pneumoniae / drug effects
-
Klebsiella pneumoniae / metabolism
-
Membrane Transport Proteins / metabolism*
-
Plant Proteins / chemistry
-
Plant Proteins / pharmacology*
-
Pseudomonas aeruginosa / drug effects
-
Pseudomonas aeruginosa / metabolism
Substances
-
Bacterial Proteins
-
Carrier Proteins
-
Chalcones
-
Membrane Transport Proteins
-
Plant Proteins
-
isobavachalcone