Multidrug resistance reversal agent from Jatropha elliptica

Bioassay-guided fractionation of Jatropha elliptica extract led to 2,6-dimethyl-4-phenyl-pyridine-3,5-dicarboxylic acid diethyl ester ( 8). This compound acts as an inhibitor of the NorA efflux pump found in a multidrug resistant strain of Staphylococcus aureus. As part of an ongoing project to iden...

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Veröffentlicht in:Phytochemistry (Oxford) 2005-08, Vol.66 (15), p.1804-1811
Hauptverfasser: Marquez, Béatrice, Neuville, Luc, Moreau, Nicole J., Genet, Jean-Pierre, dos Santos, Aldenir Feitosa, Caño de Andrade, Maria Cristina, Goulart Sant’Ana, Antônio Euzébio
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container_end_page 1811
container_issue 15
container_start_page 1804
container_title Phytochemistry (Oxford)
container_volume 66
creator Marquez, Béatrice
Neuville, Luc
Moreau, Nicole J.
Genet, Jean-Pierre
dos Santos, Aldenir Feitosa
Caño de Andrade, Maria Cristina
Goulart Sant’Ana, Antônio Euzébio
description Bioassay-guided fractionation of Jatropha elliptica extract led to 2,6-dimethyl-4-phenyl-pyridine-3,5-dicarboxylic acid diethyl ester ( 8). This compound acts as an inhibitor of the NorA efflux pump found in a multidrug resistant strain of Staphylococcus aureus. 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.
doi_str_mv 10.1016/j.phytochem.2005.06.008
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Psychology</subject><subject>General pharmacology</subject><subject>Jatropha</subject><subject>Jatropha elliptica</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>medicinal plants</subject><subject>Microbial Sensitivity Tests</subject><subject>multiple drug resistance</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacology. 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Psychology</topic><topic>General pharmacology</topic><topic>Jatropha</topic><topic>Jatropha elliptica</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>medicinal plants</topic><topic>Microbial Sensitivity Tests</topic><topic>multiple drug resistance</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacology. 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This compound acts as an inhibitor of the NorA efflux pump found in a multidrug resistant strain of Staphylococcus aureus. 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.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>16051285</pmid><doi>10.1016/j.phytochem.2005.06.008</doi><tpages>8</tpages></addata></record>
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subjects 2,6-dimethyl-4-phenylpyridine-3,5-dicarboxylic acid diethyl ester
Anti-Bacterial Agents - pharmacology
antibacterial properties
Antifungal Agents - pharmacology
Biological and medical sciences
Biological Factors
Chemical constitution
chemical structure
Drug Resistance, Multiple - drug effects
Efflux pump inhibitor
Fluoroquinolone
Fundamental and applied biological sciences. Psychology
General pharmacology
Jatropha
Jatropha elliptica
Kinetics
Medical sciences
medicinal plants
Microbial Sensitivity Tests
multiple drug resistance
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
phytochemicals
plant extracts
Plant Extracts - pharmacology
Plant physiology and development
pyridines
Resistance
spectral analysis
Staphylococcus aureus
title Multidrug resistance reversal agent from Jatropha elliptica
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