Antimicrobial photodynamic therapy with decacationic monoadducts and bisadducts of [70]fullerene: in vitro and in vivo studies

Nanomedicine (Lond). 2014 Feb;9(2):253-66. doi: 10.2217/nnm.13.22. Epub 2013 Jun 5.

Abstract

Background: Antimicrobial photodynamic therapy uses photosensitizers designed to bind to microorganisms and generate reactive oxygen species when illuminated with visible light.

Materials & methods: We synthesized a highly water-soluble [70]fullerene monoadduct, C70[>M(C3N6(+)C3)2]-(I(-))10 (LC17), and bisadduct, C70[>M(C3N6(+)C3)2][>M(C3N6C3)2] (LC18), both with a well-defined decacationic quaternary ammonium iodide moiety with ten positive charges per C70 to give water solubility and bacterial binding. We determined the antimicrobial effects against human pathogens, Gram-positive (Staphylococcus aureus) and Gram-negative species (Escherichia coli and Acinetobacter baumannii) when activated by UVA or white light.

Results: White light was more effective with LC17, while UVA light was more effective with LC18. Both compounds were effective in a mouse model of Gram-negative third-degree burn infections determined by bioluminescence imaging.

Discussion & conclusion: We propose that the attachment of an additional deca(tertiary-ethylenylamino)malonate arm to C70 allowed the moiety to act as a potent electron donor and increased the generation yield of hydroxyl radicals under UVA illumination.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acinetobacter baumannii / drug effects
  • Animals
  • Anti-Infective Agents / therapeutic use*
  • Escherichia coli / drug effects
  • Female
  • Fluorescent Dyes
  • Fullerenes / chemistry*
  • Mice
  • Mice, Inbred BALB C
  • Microbial Sensitivity Tests
  • Photochemotherapy*
  • Reactive Oxygen Species / metabolism

Substances

  • Anti-Infective Agents
  • Fluorescent Dyes
  • Fullerenes
  • Reactive Oxygen Species