Abstract

Photosensitizers that can target and accumulate in mitochondria are expected to achieve good therapeutic effects in photodynamic therapy, as mitochondria are the energy generation factory in cells. Herein, we designed and synthesized a novel mitochondrion-targeting photosensitizer TPC-Py with aggregation-induced emission characteristics for image-guided photodynamic therapy. TPC-Py possessed an efficient production of 1 O 2 , with a quantum yield of 11.65%, upon mild white light irradiation (6 mW/cm 2 ). TPC-Py exhibited good biocompatibility under dark condition, but showed remarkable cytotoxicity towards human cervical carcinoma(HeLa) cells with a half maximal inhibitory concentration(IC 50 ) of 3.2 µmol/L when exposed to white light irradiation(14.4 J/cm 2 ). In addition, the Stokes shift of TPC-Py was as high as 150 nm, so that it could prevent self-absorption and increase the signal-to-noise ratio of fluorescence imaging. The excellent performance of TPC-Py makes it a promising candidate in imaging-guided clinical PDT for cancer in the near future.