Soncin M, Busetti A, Reddi E, Jori G, Rither B D, Kenney M E, Rodgers M A
Department of Biology, University of Padova, Italy.
J Photochem Photobiol B. 1997 Sep;40(2):163-7. doi: 10.1016/s1011-1344(97)00044-4.
Three Si(IV)-tetradibenzobarreleno-octabutoxyphthalocyanines (TDiBOPcs) bearing different axial ligands on the metal ion were studied for their tumour-localizing and-photosensitizing properties after i.v. injection via a Cremophor emulsion (0.35 mumol kg-1 b.w.) to Balb/c mice bearing an intramuscularly implanted MS-2 fibrosarcoma. In all cases, the maximum tumour accumulation of the photosensitizer (0.8-1.9 nmol g-1 of tissue) was found at 24 h after injection. The efficiency and selectivity of tumour targeting appeared to be dependent on the nature of the axial ligands; optimal values of these parameters were obtained in the case of the bis(trihexyl-siloxy)-substituted Si(IV)-TDiBOPc, which gave a 7-9 tumour/muscle ratio of phthalocyanine concentration at 24-48 h after injection. The extent of tumour response to PDT treatment was correlated with the concentration of the photosensitizer in the tumour tissue: upon 740 nm irradiation (180 mW cm-2, 200 J cm-2) at 48 h after injection of 0.35 mumol kg-1 of Si(IV)-TDiBOPc-C6H13, the tumour growth exhibited a delay of about 7 days.
研究了三种在金属离子上带有不同轴向配体的硅（IV）-四二苯并巴烯并八丁氧基酞菁（TDiBOPc），通过聚氧乙烯蓖麻油乳剂（0.35 μmol kg-1体重）静脉注射给患有肌肉内植入MS-2纤维肉瘤的Balb/c小鼠后，它们的肿瘤定位和光敏特性。在所有情况下，注射后24小时发现光敏剂在肿瘤中的最大积累量（0.8-1.9 nmol g-1组织）。肿瘤靶向的效率和选择性似乎取决于轴向配体的性质；在双（三己基硅氧基）取代的硅（IV）-TDiBOPc的情况下获得了这些参数的最佳值，在注射后24-48小时，其酞菁浓度的肿瘤/肌肉比为7-9。肿瘤对光动力疗法（PDT）治疗的反应程度与肿瘤组织中光敏剂的浓度相关：在注射0.35 μmol kg-1的硅（IV）-TDiBOPc-C6H13后48小时，在740 nm照射（180 mW cm-2，200 J cm-2）下，肿瘤生长延迟约7天。
