Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
Food Chem Toxicol. 2012 Dec;50(12):4302-9. doi: 10.1016/j.fct.2012.09.001. Epub 2012 Sep 11.
A methanolic extract of Punica granatum (pomegranate) fruit pericarp (PGME) was tested in combination with ciprofloxacin against extended-spectrum β-lactamase (ESBL) producing Escherichia coli, Klebsiella pneumoniae, and metallo-β-lactamase (MBL) producing Pseudomonas aeruginosa, which were screened for their resistance profile against fluoroquinolone antibiotics. The minimum inhibitory concentrations (MIC) of ciprofloxacin and PGME, alone, were determined, and synergy of ciprofloxacin-PGME combinations evaluated by checkerboard assay and fractional inhibitory concentration (FIC). Nineteen out of forty-nine strains exhibited synergy with ciprofloxacin (FIC of 0.125-0.5 for ciprofloxacin) further verified by agar-well assay. This could be due to the bacterial efflux pump inhibitor (EPI) activity of the polyphenolic constituents of PGME. However, the isolates exhibiting a high level of ciprofloxacin resistance did not respond to ciprofloxacin-PGME combinations, which could be due to target site modification not influenced further by EPI activity of PGME. Again, some strains were sensitive or weakly resistant to ciprofloxacin, which exhibited 'indifference' to the combination, probably due to a lack of over-expressed efflux mechanism. Thus, a synergy of a ciprofloxacin-PGME combination was demonstrated for the first time against ESBL- and MBL-producing Gram-negative bacilli, and the efficacy of an existing drug improved with the help of an inexpensive alternative therapy.
石榴(石榴)果实果皮的甲醇提取物(PGME)与环丙沙星联合测试,以对抗产超广谱β-内酰胺酶(ESBL)的大肠杆菌、肺炎克雷伯菌和产金属β-内酰胺酶(MBL)的铜绿假单胞菌,这些细菌对氟喹诺酮类抗生素的耐药谱进行了筛选。单独测定了环丙沙星和 PGME 的最小抑菌浓度(MIC),并通过棋盘试验和部分抑菌浓度(FIC)评估了环丙沙星-PGME 组合的协同作用。在 49 株菌株中,有 19 株与环丙沙星表现出协同作用(环丙沙星的 FIC 为 0.125-0.5),琼脂孔试验进一步证实了这一点。这可能是由于 PGME 多酚成分具有细菌外排泵抑制剂(EPI)活性。然而,对环丙沙星表现出高水平耐药性的分离株对环丙沙星-PGME 组合没有反应,这可能是由于靶位修饰不受 PGME 的 EPI 活性进一步影响。同样,一些对环丙沙星敏感或弱耐药的菌株对该组合表现出“漠不关心”,可能是由于缺乏过度表达的外排机制。因此,首次证明了环丙沙星-PGME 联合治疗对产 ESBL 和 MBL 的革兰氏阴性杆菌具有协同作用,并通过廉价替代疗法提高了现有药物的疗效。