A versatile fluorescent molecular probe endowed with singlet oxygen generation under white-light photosensitization

- Novel molecular cassette displaying dual fluorescence and singlet oxygen emission.
- Broadband light-activation of the halogen-free photosensitizer.
- Cell internalization and low cytotoxicity of the biocompatible photosensitizer.
- Tumoral cells are efficiently destroyed by the in situ generated oxygen singlet.
- Photosensitizer retains enough fluorescence signal as to be monitored by bioimaging.

Despite fluorescent photodynamic therapy (fluorescent-PDT) dyes are promising theranostic agents, current approaches unfortunately involve crucial shortcomings (such as, narrow absorption bands, high cost, low bio-compatibility and specificity, low dual efficiency) making difficult their clinical translation. Particularly, efficient fluorescent-PDT agents triggered under white-light, with potential application in topic solar treatments, are scarce. Here, we describe the rational development of a novel fluorescent-PDT molecular biomaterial based on BODIPY building blocks able to sustain, simultaneously, synthetic accessibility, high fluorescence and phototoxicity within a broad spectral window, biocompatibility, including low dark toxicity and high cell permeability with selective accumulation in lysosomes and, what is more important, excellent efficient activity triggered under white light. These all-in-one combined properties make the new dye a valuable ground platform for the development of future smarter theranostic agents.

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