Porphyrin-apidaecin conjugate as a new broad spectrum antibacterial agent

ACS Med Chem Lett. 2010 Feb 1;1(1):35-8. doi: 10.1021/ml900021y. eCollection 2010 Apr 8.

Abstract

The conjugation of the cationic antimicrobial peptide, apidaecin Ib, to the anionic photosensitizer, 5(4'-carboxyphenyl)-10,15,20-triphenylporphyrin (cTPP), afforded a new antibacterial agent effective, under light activation, against both Gram-positive and Gram-negative bacteria. At low concentrations (1.5-15 μM) the conjugate was able to reduce the survival of Escherichia coli cells by 3-4 log10, and most notably, it resulted photoactive also against hard-to-treat Pseudomonas aeruginosa, although at higher concentration (60 μM). Under similar conditions, the photosensitizer alone was only photoactive against Staphylococcus aureus while the unconjugated peptide was inactive against all the bacterial strains tested. This study shows the possibility of obtaining new broad-spectrum apidaecin-photosensitizer conjugates with potent antibacterial activity.

Keywords: Antimicrobial PDT; antimicrobial peptides; apidaecin; photosensitizer−peptide conjugate; porphyrin.