Zn(II)-phthalocyanines as phototherapeutic agents for cutaneous diseases. Photosensitization of fibroblasts and keratinocytes

Two tetrasubstituted (RLP024 and RLP040) and one monosubstituted (MRLP101) Zn-phthalocyanines were readily accumulated by three skin-derived cell lines (HT-1080 transformed human fibroblasts, 3T3 mouse embryo fibroblasts and HaCaT human keratinocytes) upon 1 h-incubation with 0.5–5 μM phthalocyanine...

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Published in:Journal of photochemistry and photobiology. B, Biology Biology, 2006-04, Vol.83 (1), p.48-54
Main Authors: Fabris, Clara, Soncin, Marina, Miotto, Giovanni, Fantetti, Lia, Chiti, Giacomo, Dei, Donata, Roncucci, Gabrio, Jori, Giulio
Format: Article
Language:English
Subjects:
3T3 Cells
Animals
Benzimidazoles - pharmacology
Caspase 3
Caspases - drug effects
Caspases - metabolism
Caspases - radiation effects
Cell Line
Fibroblasts
Fibroblasts - drug effects
Fibroblasts - radiation effects
Humans
Indoles - therapeutic use
Keratinocytes
Keratinocytes - drug effects
Keratinocytes - radiation effects
Mice
Microscopy, Fluorescence
Organometallic Compounds - therapeutic use
Photodynamic therapy
Photosensitization
Photosensitizing Agents - therapeutic use
Phthalocyanine
Radiation-Sensitizing Agents - pharmacology
Skin Diseases - radiotherapy
Structure-Activity Relationship
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Summary:Two tetrasubstituted (RLP024 and RLP040) and one monosubstituted (MRLP101) Zn-phthalocyanines were readily accumulated by three skin-derived cell lines (HT-1080 transformed human fibroblasts, 3T3 mouse embryo fibroblasts and HaCaT human keratinocytes) upon 1 h-incubation with 0.5–5 μM phthalocyanine concentrations. The affinity was markedly larger for the tetra- as compared with the mono-substituted phthalocyanine, even though smaller phthalocyanine amounts were generally recovered from keratinocytes. As a consequence, the two tetra-substituted phthalocyanines exhibited a higher phototoxicity against all the three cell lines. Typically, the cell survival decreased by at least 80% after 1 min irradiation with 600–700 nm light at a fluence-rate of 50 mW/cm 2 in the presence of 5 μM phthalocyanine. Fluorescence microscopy and caspase-3 activation studies indicate that cell death of fibroblasts largely occurred by a random-necrotic process while the keratinocytes underwent cell death predominantly via apoptosis in spite of a very similar pattern of subcellular distribution of the phthalocyanines.
ISSN:1011-1344
1873-2682
DOI:10.1016/j.jphotobiol.2005.12.006