Abstract
Antimicrobial photodynamic therapy (aPDT) is an emerging treatment for bacterial infections that is becoming increasingly more attractive because of its effectiveness against multi-antibiotic-resistant strains and unlikelihood of inducing bacterial resistance. Among the strategies to enhance the efficacy of PDT against Gram-negative bacteria, the binding to a cationic antimicrobial peptide offers the attractive prospect for improving both the water solubilty and the localization of the photoactive drug in bacteria. In this work we have compared a number of free and apidaecin-conjugated photosensitizers (PSs) differing in structure and charge. Our results indicate that the conjugation of per se ineffective highly hydrophobic PSs to a cationic peptide produces a photosensitizing agent effective against Gram-negative bacteria. Apidaecin cannot improve the phototoxic activity of cationic PSs, which mainly depends on a very high yield of singlet oxygen production in the surroundings of the bacterial outer membrane. Apidaecin-PS conjugates appear most promising for treatment protocols requiring repeated washing after sensitizer delivery.
Original language | English |
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Pages (from-to) | 1052-1063 |
Number of pages | 12 |
Journal | Journal of Medicinal Chemistry |
Volume | 56 |
Issue number | 3 |
DOIs | |
Publication status | Published - 14 Feb 2013 |
Keywords
- Singlet oxygen
- Photodynamic therapy
- Escherichia-coli
- Spectrum
- Luminescence
- Biodiversity
- Membrane