A novel pyrazolone complex P-FAH-Cu-bpy induces death of Escherichia coli and Staphylococcus aureus by disrupting cell structure and blocking energy.

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 Ca2+-Mg2+-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. [ABSTRACT FROM AUTHOR]