Meso-tetraphenylporphyrin dimer derivative as a potential photosensitizer in photodynamic therapy.
Studies on the synthesis, preliminary in vivo biological activity, singlet oxygen and fluorescence yields of a dimeric porphyrin (D1) are described. The pharmacokinetic behavior and photodynamic properties of the dimer D1 were examined in Balb/c mice bearing an MS-2 fibrosarcoma. Compound D1 shows a high selectivity for tumor localization (tumor/peritumoral tissue ratios of dye concentration ranging between ca 100 and 140 at 24 h after drug administration of 5.0-1.0 mg kg-1 into DL-alpha-dipalmitoylphosphatidylcholine liposomes). The phototherapeutic efficiency of dimer D1 was evaluated by following the growth curves of fibrosarcoma irradiated with red light (600-700 nm) with a total dose of 400 J cm-2, at 24 h after intravenous injection. Photodynamic therapy-treated tumors showed a significant delay in growth as compared to untreated control mice. The results obtained suggest that the porphyrin dimer D1 may be a promising candidate for further use in PDT experiments.
Faustino
M A
MA
Department of Chemistry, University of Aveiro, Portugal.
Neves
M G
MG
Vicente
M G
MG
Cavaleiro
J A
JA
Neumann
M
M
Brauer
H D
HD
Jori
G
G
D000818:Animals; D015195:Drug Design; D005260:Female; D005354:Fibrosarcoma / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D010777:Photochemistry; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
D017319:Photosensitizing Agents; D011166:Porphyrins