Antibacterial activity of ruthenium polypyridyl complexes against Staphylococcus aureusand biofilms

摘要

There is clearly a need for the development of new classes of antimicrobials to fight against multidrug-resistant bacteria. Here, we designed and synthesized of three ruthenium polypyridyl complexes: [Ru(bpy)(2)(BTPIP)](ClO4)(2)(Ru(II)-1), [Ru(bpy)(2)(ETPIP)](ClO4)(2)(Ru(II)-2) and [Ru(bpy)(2)(CAPIP)](ClO4)(2)(Ru(II)-3) (N-N = bpy = 2,2 '-bipyridine), their antimicrobial activities againstS. aureuswere assessed. The lead complexes of this set,Ru(II)-1(MIC = 0.016 mg/mL), was tested against biofilm. We also investigated whether bacteria can easily develop resistance toRu(II)-1. The result demonstrated thatS. aureuscould not easily develop resistance to the ruthenium complexes. In addition, aimed to test whether ruthenium complexes treatment could increase the susceptibility ofS. aureusto antibiotics, the synergism betweenRu(II)-1and common antibiotics againstS. aureuswere investigated using the checkerboard method. Interesting,Ru(II)-1could increased the susceptibility ofS. aureusto some aminoglycoside antibiotics(kanamycin and gentamicin). Finally, in vivo bacterial infection treatment studies were also conducted through murine skin infection model. These results confirmed ruthenium complexes have good antimicrobial activity in vitro and in vivo.