Medicinal Plants Research Center, Federal University of Piaui, Teresina, Piaui, Brazil.
Laboratory of Research in Microbiology, Federal University of Piaui, Teresina, Piaui, Brazil.
Microb Pathog. 2019 May;130:242-246. doi: 10.1016/j.micpath.2019.03.012. Epub 2019 Mar 12.
The aim of this study was to evaluate the antimicrobial activity of ethanoic extract of P. amarus (PAEE) and its compound Phyllanthin, as well as, investigate if these natural products could modulate the fluoroquinolone-resistance in S. aureus SA1199-B by way of overexpression of the NorA efflux pump. Microdilution tests were carried out to determine the minimal inhibitory concentration (MIC) of the PAEE or Phyllanthin against several bacterial and yeast strains. To evaluate if PAEE or Phyllanthin were able to act as modulators of the fluoroquinolone-resistance, MICs for Norfloxacin and ethidium bromide were determined in the presence or absence of PAEE or Phyllanthin against S. aureus SA1199-B. PAEE showed antimicrobial activity against Gram-negative strains, meanwhile Phyllanthin was inactive against all strains tested. Addition of PAEE or Phyllanthin, to the growth media at sub-inhibitory concentrations enhanced the activity of the Norfloxacin as well as, Ethidium Bromide, against S. aureus SA1199-B. These results indicate that Phyllanthin is able to modulate the fluoroquinolone-resistance possibly by inhibition of NorA. This hypothesis was supported by in silico docking analysis which confirmed that Phyllantin is a NorA ligand. Thus, this compound could be used as a potentiating agent of the Norfloxacin activity in the treatment of infections caused by fluoroquinolone-resistant S. aureus.
本研究旨在评估相思豆(P. amarus)的乙酸乙酯提取物(PAEE)及其化合物叶素的抗菌活性,并研究这些天然产物是否可以通过过度表达 NorA 外排泵来调节金黄色葡萄球菌 SA1199-B 的氟喹诺酮耐药性。进行微量稀释试验以确定 PAEE 或叶素对几种细菌和酵母菌株的最小抑菌浓度(MIC)。为了评估 PAEE 或叶素是否能够作为氟喹诺酮耐药性的调节剂,在存在或不存在 PAEE 或叶素的情况下,确定了诺氟沙星和溴化乙锭对金黄色葡萄球菌 SA1199-B 的 MIC。PAEE 对革兰氏阴性菌株表现出抗菌活性,而叶素对所有测试菌株均无活性。在亚抑菌浓度下将 PAEE 或叶素添加到生长培养基中,增强了 Norfloxacin 以及溴化乙锭对金黄色葡萄球菌 SA1199-B 的活性。这些结果表明,叶素能够调节氟喹诺酮耐药性,可能是通过抑制 NorA。这一假设得到了计算机对接分析的支持,该分析证实叶素是 NorA 的配体。因此,该化合物可作为氟喹诺酮耐药性金黄色葡萄球菌引起感染的诺氟沙星活性的增强剂。