Department of Chemistry and Biochemistry, Concordia University, Montréal, Québec, Canada.
Department of Chemistry and Biochemistry, Concordia University, Montréal, Québec, Canada; Department of Biology, Concordia University, Montréal, Québec, Canada.
Bioorg Med Chem. 2024 Jan 1;97:117541. doi: 10.1016/j.bmc.2023.117541. Epub 2023 Dec 6.
Infections caused by antibiotic-resistant bacteria are a major threat to health, increasing mortality rates and straining health systems worldwide. Adjuvants targeted to beta-lactamase function are able to resensitize bacteria to beta-lactam antibiotics, but there is comparatively little research into the use of adjuvants against other resistance phenotypes. In this study, we performed a high-throughput screen of 74 natural products to identify adjuvants that synergized with antibiotics to eradicate resistant Gram-negative bacteria. From this, we identified six adjuvant hits which restored growth inhibition when combined with the relevant antibiotic, and pursued a lead candidate, perforone, which possessed selective adjuvant activity in combination with polymyxin B against polymyxin-resistant Escherichia coli cells. These results suggest that pairing adjuvants with antibiotics could be a useful general intervention against resistant bacteria, helping to mitigate the effects of antimicrobial resistance.
抗生素耐药菌引起的感染是对健康的主要威胁,它增加了全球的死亡率并使卫生系统不堪重负。针对β-内酰胺酶功能的佐剂能够使细菌重新对β-内酰胺类抗生素敏感,但针对其他耐药表型的佐剂研究相对较少。在这项研究中,我们对 74 种天然产物进行了高通量筛选,以鉴定与抗生素协同作用以消灭耐药革兰氏阴性菌的佐剂。由此,我们确定了六个佐剂,当与相关抗生素联合使用时,它们可以恢复生长抑制,我们进一步研究了先导候选物——穿孔素,发现其与多粘菌素 B 联合使用时,对多粘菌素耐药的大肠杆菌细胞具有选择性佐剂活性。这些结果表明,将佐剂与抗生素联合使用可能是对抗耐药菌的一种有用的一般干预措施,有助于减轻抗菌药物耐药性的影响。