Combination of vancomycin and guanidinium-functionalized helical polymers for synergistic antibacterial activity and biofilm ablation

万古霉素与胍基功能化螺旋聚合物联用,可产生协同抗菌活性并破坏生物膜。

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Abstract

The emergence of various resistant bacteria and overuse of antibiotics have led to severe side effects. Therefore, developing efficient and safe antibacterial systems is important. Herein, well-defined antimicrobial material-helical poly(phenyl guanidinium isocyanide) block copolymers with different conformations (l-P3-van, d-P3-van, and dl-P3-van) that connect vancomycin (van) to the polymer through a disulfide bond were synthesized. The prepared antimicrobial materials exhibit broad-spectrum antimicrobial activity, low bacterial resistance, and good proteolytic stability. They also overcome the intrinsic resistance of Gram-negative bacteria to van with a 100-fold increase in antimicrobial activity. Interestingly, the conformation of the material promotes its antimicrobial activity. The left-handed helix conformation shows five-fold more antimicrobial activity than the right-handed helical conformation, thereby opening a path for the application of nanochirality in the field of antibiotics.

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