Synthesis, characterization, and photoinduced antibacterial activity of porphyrin-type photosensitizers conjugated to the antimicrobial peptide apidaecin 1b

Ryan Dosselli, Cristiano Tampieri, Rubén Ruiz-González, Sonia De Munari, Xavier Ragàs, David Sánchez-García, Montserrat Agut, Santi Nonell, Elena Reddi, Marina Gobbo

Producción científica: Artículo en revista indizadaArtículorevisión exhaustiva

87 Citas (Scopus)

Resumen

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.

Idioma originalInglés
Páginas (desde-hasta)1052-1063
Número de páginas12
PublicaciónJournal of Medicinal Chemistry
Volumen56
N.º3
DOI
EstadoPublicada - 14 feb 2013

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