ABSTRACT
Cell-selective activity regulation of therapeutics is necessary for efficient personalized treatments with minimal off-target effects. Here, the first example of a structurally simple, pyridinium BODIPY-based, tyrosinase activatable photosensitizer is developed and the cytotoxic singlet oxygen generation capacity is analysed. Singlet oxygen quantum yields of active and inactive forms are determined to be 0.64 and 0.02, respectively. Selective photo-induced cell death in mouse melanoma cells over mammary and hepatocellular carcinoma proved the potential of the photosensitizer in tissue-selective therapies.
Subject(s)
Antineoplastic Agents , Melanoma , Photochemotherapy , Mice , Animals , Photosensitizing Agents/pharmacology , Photosensitizing Agents/therapeutic use , Singlet Oxygen , Melanoma/drug therapy , Antineoplastic Agents/pharmacologyABSTRACT
Two novel, self-reporting distyryl BODIPY-based photodynamic therapy agents functionalized with singlet oxygen responsive imidazole and tertiary amine moieties are developed. Heavy atom-free photosensitizers are demonstrated to have efficient photodynamic action in MCF7 cells. The fluorescence intensity of the photosensitizers is shown to be reduced as a result of 1O2 generation without any significant change in photodynamic activity.