Single-Chromophore-Based Therapeutic Agent Enables Green-Light-Triggered Chemotherapy and Simultaneous Photodynamic Therapy to Cancer Cells

A new type of single-chromophore-based photoactivatable prodrug (B-Cbl-3) enabling green-light-triggered chemotherapy and simultaneous photodynamic therapy with superb therapeutic efficacy was developed by conjugating a photoactive BODIPY derivative with an antitumor chlorambucil moiety. The optimized BODIPY moiety markedly enabled high efficient photogeneration of 1O2 and fluorescence emission with distinct colors before and after photorelease of chlorambucil. The preliminary biological experiment results have verified the efficient photorelease of chlorambucil from B-Cbl-3 and the huge contrast in cytotoxicity between them, superior combined therapeutic performance based on extraordinary low doses of drug and light irradiation, and ratiometric fluorescence imaging for in situ monitoring drug release. The salient superiority of B-Cbl-3 regarding alleviating the attenuation of triggering light caused by optically turbid tissue that short-wavelength lights typically encounters has also been verified.