Abstract
Porphyrin-polyamine conjugates bearing two (cis or trans position) or four spermidine or spermine units were synthesized. We studied the photostability, the hydrophilic/lipophilic balance of porphyrin-polyamine derivatives and the production of singlet oxygen. All these compounds possess physicochemical features required for their use in PDT. Then, we investigated the photocytotoxic efficacy of these porphyrin-polyamine derivatives and the cell death pathway implicated. All compounds appear to be more efficient than Photofrin® to induce HaCat and MCF7 cell death, essentially by apoptosis. Collectively, these data show that porphyrin-polyamine conjugates could be promising phototherapeutic agents.
2011 Elsevier B.V. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Apoptosis / drug effects*
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Apoptosis / radiation effects
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cell Line
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Cell Line, Tumor
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Female
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Humans
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Keratinocytes / cytology
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Keratinocytes / metabolism
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Photochemistry / methods*
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Photosensitizing Agents / chemical synthesis
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Photosensitizing Agents / chemistry
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Photosensitizing Agents / pharmacology*
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Phototherapy / methods
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Polyamines / chemical synthesis
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Polyamines / chemistry
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Polyamines / pharmacology*
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Porphyrins / chemical synthesis
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Porphyrins / chemistry
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Porphyrins / pharmacology*
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Spermidine / chemistry
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Spermidine / pharmacology
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Spermine / chemistry
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Spermine / pharmacology
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Stereoisomerism
Substances
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Photosensitizing Agents
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Polyamines
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Porphyrins
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Spermine
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Spermidine