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Phenylpropanoids of Alpinia galanga as efflux pump inhibitors in Mycobacterium smegmatis mc(2) 155

机译:高良姜高良姜的苯丙烷类化合物作为耻垢分枝杆菌mc(2)155中的外排泵抑制剂

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摘要

The first and second line drugs used for the treatment of tuberculosis are now becoming ineffective due to emergence of resistant strains. Efflux pump provokes resistance in mycobacterium and hence could be explored as a new target for the discovery of anti-TB agents. In search of efflux pump inhibitors, MIC and modulation factor of phenylpropanoids isolated from A. galanga rhizome were determined prior to the accumulation and efflux assay. Phenylpropanoid compounds viz. 1′-S-1′-Acetoxychavicol acetate, trans-p-coumaryl diacetate and 1′-S-1′-acetoxyeugenol acetate were found to be potent modulators and decreased the MIC of ethidium bromide by 64 fold at the concentration of 2.5, 6.25 and 5.0 mg/L respectively. 1′-S-1′-Acetoxyeugenol acetate enhanced the accumulation and inhibited the efflux of EtBr in Mycobacterium smegmatis mc2 155 cells.
机译:由于耐药菌株的出现,用于治疗结核病的一线和二线药物现在变得无效。外排泵在分枝杆菌中引起耐药性,因此可以作为发现抗结核病药物的新靶标进行探索。为了寻找外排泵抑制剂,在蓄积和外排测定之前,测定了从高良姜根茎中分离出的苯基丙烷的MIC和调节因子。苯丙烷化合物即。发现1'-S-1'-乙酸乙酰丁香酚酯,反-对-香豆基双乙酸酯和1'-S-1'-乙酰氧基丁香酚乙酸酯是有效的调节剂,在2.5的浓度下,溴化乙锭的MIC降低了64倍,分别为6.25和5.0 mg / L。 1'-S-1'-乙酰丁香酚乙酸酯可增强耻垢分枝杆菌mc2 155细胞中EtBr的积累并抑制其流出。

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