Synthesis, Characterization, and Photoinduced Antibacterial Activity of Porphyrin-Type Photosensitizers Conjugated to the Antimicrobial Peptide Apidaecin 1b
| Autor: | Rubén Ruiz-González, Ryan Dosselli, Elena Reddi, David Sánchez-García, Santi Nonell, Cristiano Tampieri, Sonia De Munari, Montserrat Agut, Xavier Ragàs, Marina Gobbo |
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| Rok vydání: | 2013 |
| Předmět: |
Porphyrins
medicine.medical_treatment Photodynamic therapy Peptide Microbial Sensitivity Tests Mass Spectrometry chemistry.chemical_compound Gram-Negative Bacteria Drug Discovery medicine Chromatography High Pressure Liquid chemistry.chemical_classification Photosensitizing Agents Singlet Oxygen biology Singlet oxygen Photosensitizing Agent Photochemical Processes Antimicrobial biology.organism_classification Porphyrin Combinatorial chemistry Anti-Bacterial Agents Spectrometry Fluorescence chemistry Biochemistry Molecular Medicine Spectrophotometry Ultraviolet Antibacterial activity Bacteria Antimicrobial Cationic Peptides |
| Zdroj: | Journal of Medicinal Chemistry. 56:1052-1063 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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