4.5 Article

Porphyrin - Apidaecin Conjugate as a New Broad Spectrum Antibacterial Agent

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 1, Pages 35-38

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ml900021y

Keywords

Antimicrobial PDT; antimicrobial peptides; porphyrin; apidaecin; photosensitizer-peptide conjugate

Funding

  1. Italian Minister dell'Istruzione, dell'Universita e della Ricerca

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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 (15-15 mu M) the conjugate was able to reduce the survival of Escherichia coli cells by 3-4 log(10), and most notably, it resulted photoactive also against hard-to-treat Pseudomonas aeruginosa. although at higher concentration (60 mu M) 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

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