Multidrug resistance reversal agent from Jatropha elliptica
Multidrug resistance reversal agent from Jatropha elliptica
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DOI：
10.1016/j.phytochem.2005.06.008
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发表时间：
2005-08-01
期刊：
影响因子：
3.8
通讯作者：
Sant'Ana, AEG
中科院分区：
文献类型：
--
作者：
Marquez, B;Neuville, L;Sant'Ana, AEG
作为一个正在进行的项目的一部分，以确定植物天然产物作为抗性修饰剂，生物测定指导分馏的提取物的麻风树椭圆（波尔）Muell精氨酸。导致分离五取代的吡啶，即2，6-二甲基-4-苯基-吡啶-3，5-二羧酸二乙酯（8）。通过光谱方法确定结构。测定该已知化合物对具有MsrA和诺拉耐药外排机制的金黄色葡萄球菌菌株的体外抗菌和耐药修饰活性。抗生素外排研究表明，（8）作为诺拉外排泵的抑制剂，并恢复细胞内药物浓度的水平。(c)2005 Elsevier Ltd.保留所有权利。
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. (c) 2005 Elsevier Ltd. All rights reserved.