Multidrug resistance reversal agent from Jatropha elliptica.
As part of an ongoing project to identify plant natural products as resistance-modifying agents, bioassay-guided fractionation of an extract of Jatropha elliptica (Pohl) Muell Arg. led to the isolation of a penta-substituted pyridine, namely 2,6-dimethyl-4-phenyl-pyridine-3,5-dicarboxylic acid diethyl ester (8). The structure was established by spectroscopic methods. This known compound was assayed for in vitro antibacterial and resistance-modifying activities against strains of Staphylococcus aureus possessing the MsrA and NorA resistance efflux mechanisms. Antibiotic efflux studies indicated that (8) acts as an inhibitor of the NorA efflux pump and restores the level of intracellular drug concentration.
Marquez
Béatrice
B
Laboratoire de Synthèse Sélective Organique et Produits Naturels, Ecole Nationale Supérieure de Chimie de Paris, UMR CNRS 7573, 11 rue Pierre et Marie Curie, 75231 Paris Cedex 05, France.
Neuville
Luc
L
Moreau
Nicole J
NJ
Genet
Jean-Pierre
JP
dos Santos
Aldenir Feitosa
AF
Caño de Andrade
Maria Cristina
MC
Sant'Ana
Antônio Euzébio Goulart
AE
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000935:Antifungal Agents / Q000494:pharmacology; D001685:Biological Factors; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D031286:Jatropha; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D010936:Plant Extracts / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001685:Biological Factors; D010936:Plant Extracts