Comparative study of photo-induced activity of di- and tri-sulfonated derivatives of metal-free phthalocyanine and Photosens

摘要

Di- and tri-sulfonated derivatives of metal-free phthalocyanine and Photosens have been compared in this study. In vitro phototoxicity was studied on HEp2, A549, and Colo26 cell cultures. It has been shown that phototoxicity of di- and tri-sulfonated derivatives of metal-free phthalocyanine exceeds phototoxicity of Photosens 5- and 8-times on HEp2 cell line, 8- and 6-times on A549 cell line, and 22-times on Colo26 cell line, respectively. In vivo photo-induced antitumor activity of metal-free phthalocyanine and Photosens was evaluated on mice with transplanted P388 lymphocytic leukemia. Dependence of photodynamic therapy efficiency on photosensitizer dose and time interval between preparation administration and irradiation was studied. It has been shown that Photosens is the most efficient in 5 mg/kg of animal body weight dose and at 24-hour interval between injection and irradiation (tumor growth inhibition (TGI) - 82.2-95.6%). Metal-free phthalocyanine is the most efficient in 0.5 mg/kg dose which is 10-times lower than Photosens dose and when irradiated 4 hours later the injection (TGI - 78.6-100%). Metal-free di- and tri-sulfonated phthalocyanines are promising photosensitizers for photodynamic therapy. Taking into account its physical and chemical properties metal-free tri-sulfonated phthalocyanine named "Phthalosens" has been chosen for further thorough study.