Details

Autor(en) / Beteiligte

• Ragàs, Xavier
• Sánchez-García, David
• Ruiz-González, Rubén
• Dai, Tianhong
• Agut, Montserrat
• Hamblin, Michael R
• Nonell, Santi

Titel

Cationic Porphycenes as Potential Photosensitizers for Antimicrobial Photodynamic Therapy

Ist Teil von

• Journal of medicinal chemistry, 2010-11, Vol.53 (21), p.7796-7803

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• Structures of typical photosensitizers used in antimicrobial photodynamic therapy are based on porphyrins, phthalocyanines, and phenothiazinium salts, with cationic charges at physiological pH values. However, derivatives of the porphycene macrocycle (a structural isomer of porphyrin) have barely been investigated as antimicrobial agents. Therefore, we report the synthesis of the first tricationic water-soluble porphycene and its basic photochemical properties. We successfully tested it for in vitro photoinactivation of different Gram-positive and Gram-negative bacteria, as well as a fungal species (Candida) in a drug-dose and light-dose dependent manner. We also used the cationic porphycene in vivo to treat an infection model comprising mouse third degree burns infected with a bioluminescent methicillin-resistant Staphylococcus aureus strain. There was a 2.6-log10 reduction (p < 0.001) of the bacterial bioluminescence for the PDT-treated group after irradiation with 180 J·cm−2 of red light.