Faustino M A, Neves M G, Vicente M G, Cavaleiro J A, Neumann M, Brauer H D, Jori G
Department of Chemistry, University of Aveiro, Portugal.
Photochem Photobiol. 1997 Oct;66(4):405-12. doi: 10.1111/j.1751-1097.1997.tb03165.x.
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.
本文描述了一种二聚体卟啉（D1）的合成、初步体内生物活性、单线态氧和荧光产率的研究。在携带MS-2纤维肉瘤的Balb/c小鼠中检测了二聚体D1的药代动力学行为和光动力性质。化合物D1对肿瘤定位具有高选择性（在以5.0 - 1.0 mg kg-1的剂量将其注入DL-α-二棕榈酰磷脂酰胆碱脂质体后24小时，染料浓度的肿瘤/肿瘤周围组织比率在约100至140之间）。在静脉注射后24小时，通过跟踪用总剂量为400 J cm-2的红光（600 - 700 nm）照射的纤维肉瘤的生长曲线，评估了二聚体D1的光治疗效率。与未治疗的对照小鼠相比，光动力疗法治疗的肿瘤生长明显延迟。所得结果表明，卟啉二聚体D1可能是进一步用于光动力疗法实验的有前景的候选物。
