Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue 3, Pages 1052-1063Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm301509n
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Funding
- University of Padova, Progetto di Ateneo [2009 CPDA090338]
- Spanish Ministerio de Economia y Competitividad [CTQ2010-20870-C03-01, IT2009-0033]
- Italian Ministero dell'Istruzione dell'Universita e della Ricerca [IT10H5E13A]
- Generalitat de Catalunya (DURSI)
- Fons Social Europeu
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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.
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