AIE-Active Antibiotic Photosensitizer with Enhanced Fluorescence in Bacteria Infected Cells and Better Therapy Effect toward Drug-Resistant Bacteria.

It is well-known that bacterial infections will induce a variety of diseases in the clinic. In particular, the emergence of drug-resistant bacteria has increased the threat to human health. The development of multiple modes of therapy will effectively fight against drug-resistant bacterial infections. In this work, we covalently attached an AIE photosensitizer to the antibiotic of moxifloxacin hydrochloride (MXF-HCl) and synthesized an antibiotic derivative, MXF-R, with pharmacological activity and photodynamic activation. In infected cells, MXF-R showed enhanced fluorescence after it specifically binds to bacteria; thus, in situ visualization of the bacteria was realized. Notably, through chemo- and photodynamic therapy, MXF-R exhibited better antibacterial activity than its parent antibiotic in rapid sterilization, and it achieved effective killing for moxifloxacin resistant bacteria. In addition, MXF-R shows a broad-spectrum antibacterial effect and could be used in the recovery therapy of infected wounds in mice, demonstrative of a significant therapeutic effect and good biological safety. Thus, as a promising multifunctional antibacterial agent, MXF-R will have tremendous potential in in situ visualization study and killing of drug-resistant bacteria. This work provides an innovative strategy for solving critical disease through the combination of materials and biomedical sciences.