一种新型吡唑啉酮配合物 P-FAH-Cu-bpy 通过破坏细胞结构和阻断能量来诱导大肠杆菌和金黄色葡萄球菌死亡。
A novel pyrazolone complex P-FAH-Cu-bpy induces death of Escherichia coli and Staphylococcus aureus by disrupting cell structure and blocking energy.
机构信息
College of Life Sciences, Xinjiang Normal University, Urumqi, 830017, Xinjiang, China.
Institute of Applied Chemistry, College of Chemistry, Xinjiang University, Urumqi, 830046, Xinjiang, China.
出版信息
Arch Microbiol. 2023 Nov 8;205(12):376. doi: 10.1007/s00203-023-03714-6.
A novel pyrazolone-based copper complex [Cu(L)(bpy)]∙CH3OH (P-FAH-Cu-bpy) was synthesized and previously characterized to have antitumor properties. This study aimed to investigate its antibacterial properties and action modes against Escherichia coli and Staphylococcus aureus. By agar diffusion assay, P-FAH-Cu-bpy showed strong antibacterial activity against E. coli and S. aureus with the diameter of inhibition zone of 10.17-12.50 mm and 11.83-14 mm, respectively. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the complex were 1.5 and 3 μM, respectively. Destroyed bacteria cells and debris were clearly observed by SEM. At 2 MIC and 4 MIC of P-FAH-Cu-bpy, 1.1683 and 1.9083 pg copper per cell was taken by E. coli, and 4.5670 and 8.5250 pg per cell by S. aureus, respectively. Multi-step resistance selection showed both bacteria were sensitive to P-FAH-Cu-bpy without induction of resistance within 30 generations. With P-FAH-Cu-bpy treatment, the release of nucleotides and proteins and alkaline phosphatase was increased, but the activity of K-Na-ATPase and Ca-Mg-ATPase and membrane conductivity were decreased in both pathogens. In conclusion, P-FAH-Cu-bpy induced death of both bacteria by destroying the cell membrane structure and blocking energy and exhibited strong antibacterial activity against E. coli and S. aureus without inducing microbial resistance.
一种新型吡唑酮铜配合物[Cu(L)(bpy)]·CH3OH (P-FAH-Cu-bpy) 已被合成并进行了先前的抗肿瘤特性研究。本研究旨在探讨其对大肠杆菌和金黄色葡萄球菌的抗菌特性和作用模式。琼脂扩散试验表明，P-FAH-Cu-bpy 对大肠杆菌和金黄色葡萄球菌具有较强的抗菌活性，抑菌圈直径分别为 10.17-12.50mm 和 11.83-14mm。该配合物的最低抑菌浓度（MIC）和最低杀菌浓度（MBC）分别为 1.5 和 3μM。SEM 观察到明显的细菌细胞破坏和碎片。在 2 MIC 和 4 MIC 的 P-FAH-Cu-bpy 作用下，大肠杆菌分别摄取 1.1683 和 1.9083pg 铜/细胞，金黄色葡萄球菌分别摄取 4.5670 和 8.5250pg 铜/细胞。多步耐药性选择表明，在 30 代内，两种细菌对 P-FAH-Cu-bpy 均敏感，没有诱导耐药性。用 P-FAH-Cu-bpy 处理后，两种病原体的核苷酸和蛋白质以及碱性磷酸酶释放增加，而 K-Na-ATPase 和 Ca-Mg-ATPase 的活性以及膜电导率降低。综上所述，P-FAH-Cu-bpy 通过破坏细胞膜结构和阻断能量来诱导两种细菌死亡，并对大肠杆菌和金黄色葡萄球菌表现出较强的抗菌活性，而不会诱导微生物耐药性。
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