Polylysine-porphycene conjugates as efficient photosensitizers for the inactivation of microbial pathogens.
Porphycenes are electronic isomers of porphyrins which, when neutral, display no appreciable photosensitizing action towards Gram-negative bacteria. The covalent binding of oligomeric polylysine moieties, which are cationic at physiological pH values, endows porphycenes with a significant phototoxic activity against Gram-negative bacteria while retaining their photoefficiency against a variety of microbial pathogens, including Gram-positive bacteria, fungi and mycoplasmas. The effect of the polylysine moiety is dependent on both the polylysine concentration and the degree of oligomerization. A suitable interplay among the various parameters opens the possibility to obtain either a broad spectrum of antimicrobial activity or a selective action toward a specific pathogen while minimizing the damage to human fibroblasts.
Polo
L
L
Department of Biology, University of Padova, Italy.
Segalla
A
A
Bertoloni
G
G
Jori
G
G
Schaffner
K
K
Reddi
E
E
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects / Q000254:growth & development; D002478:Cells, Cultured; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D005347:Fibroblasts / Q000166:cytology; D006801:Humans; D015394:Molecular Structure; D017319:Photosensitizing Agents / Q000737:chemistry / Q000494:pharmacology*; D011107:Polylysine / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development
C438955:2,7,12,17-tetrakis(2-methoxyethyl)-9-glutaramidoporphycene; C438956:2,7,12,17-tetrakis(2-methoxyethyl)-9-p-carboxybenzyloxyporphycene; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D017319:Photosensitizing Agents; D011166:Porphyrins; C051407:porphycene; D011107:Polylysine