Abstract
Photodynamic Therapy (PDT) is a promising treatment for various types of cancer and other non-oncological diseases. This technique uses a photosensitizer (PS) that generates reactive oxygen species (ROS), which lead cells to death in the presence of light and molecular oxygen. In this study, we evaluated the photoactivity of four chlorins that presented an L-type structure conformation (6a, 6b, 8a, and 8b) in two tumoral (HEp-2 and HeLa) and one non-tumoral (Vero) cell line under PDT conditions. Intracellular accumulation and subcellular localization were determined by confocal microscopy, showing that these chlorins exhibited an excellent (120 min) internalization through the plasmatic membrane with mitochondria and lysosome localization. The chlorins 6a-b were two and three-fold more selective than the chlorins 8a-b to HEp-2 and HeLa compared to Vero at 3 and 6 J cm−2 doses, respectively. The fluorescence microscopy and flow cytometry analysis showed that the four chlorin derivatives lead tumor cells to death predominantly by apoptosis during the treatment with light. Considering that the chlorins 6a-b exhibited good water solubility and high phototoxicity to the tumor cells, we suggested that these tetrapyrrolic molecules have the potential for clinical treatment in cancer by PDT.
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