Efflux pumps are involved in the defense of Gram-negative bacteria against the natural products isobavachalcone and diospyrone.
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.
Kuete
Victor
V
Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon.
Ngameni
Bathélémy
B
Tangmouo
Jean G
JG
Bolla
Jean-Michel
JM
Alibert-Franco
Sandrine
S
Ngadjui
Bonaventure T
BT
Pagès
Jean-Marie
JM
D001426:Bacterial Proteins / Q000378:metabolism; D002352:Carrier Proteins / Q000378:metabolism; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D029788:Diospyros; D055808:Drug Discovery; D024881:Drug Resistance, Bacterial; D018432:Drug Resistance, Multiple; D021902:Enterobacter aerogenes / Q000187:drug effects / Q000378:metabolism; D016972:Enterobacter cloacae / Q000187:drug effects / Q000378:metabolism; D004926:Escherichia coli / Q000187:drug effects / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000378:metabolism*; D007711:Klebsiella pneumoniae / Q000187:drug effects / Q000378:metabolism; D026901:Membrane Transport Proteins / Q000378:metabolism*; D010940:Plant Proteins / Q000737:chemistry / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000378:metabolism
D001426:Bacterial Proteins; D002352:Carrier Proteins; D047188:Chalcones; D026901:Membrane Transport Proteins; D010940:Plant Proteins; C468754:isobavachalcone