Chemical Research in Chinese Universities ›› 2021, Vol. 37 ›› Issue (1): 137-142.doi: 10.1007/s40242-021-0379-0

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Mitochondrion-anchoring AIEgen with Large Stokes Shift for Imaging-guided Photodynamic Therapy

FANG Fang1, GAO Yuting1, LUO Liang1,2   

  1. 1. National Engineering Research Center for Nanomedicine, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, P. R. China;
    2. Hubei Key Laboratory of Bioinorganic Chemistry and Materia Medica, School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan 430074, P. R. China
  • Received:2020-11-20 Revised:2020-12-28 Online:2021-02-01 Published:2020-12-29
  • Contact: LUO Liang E-mail:liangluo@hust.edu.cn
  • Supported by:
    This work was supported by the National Natural Science Foundation of China(Nos.22077038, 21702070), the Postdoctoral Research Foundation of China(No.2017M612461) and the Huazhong University Startup Fund of China.

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 aggregationinduced emission characteristics for image-guided photodynamic therapy. TPC-Py possessed an efficient production of 1O2, with a quantum yield of 11.65%, upon mild white light irradiation (6 mW/cm2). TPC-Py exhibited good biocompatibility under dark condition, but showed remarkable cytotoxicity towards human cervical carcinoma(HeLa) cells with a half maximal inhibitory concentration(IC50) of 3.2 μmol/L when exposed to white light irradiation(14.4 J/cm2). 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.

Key words: Photodynamic therapy, Photosensitizer, Aggregation-induced emission, Mitochondria, Imaging-guided