Aggregation-induced Emission-active Fluorescent Nanodot as a Potential Photosensitizer for Photodynamic Anticancer Therapy

Background: Photodynamic therapy (PDT) has become a very promising and effective strategy for the treatment of cancers and other malignant diseases. In recent years, photosensitizers (PS) with aggregation-induced emission (AIE) property have attracted great attention. Objective: A high-performance AIE-active PS, E- 1-allyl-3-(2-(5-(4-(diphenylamino)phenyl) thiophene- 2-yl)vinyl)quinoxalin-2 (1H)-one (SJ-1), was synthesized and its PDT effect was preliminarily tested in vitro. Methods: SJ-1 was designed using a quinoxalinone scaffold as the core chromophore. It could selfassembled into AIE-active nanoparticles with a mean size of 155 nm in aqueous medium and show maximum emission at 633 nm. Results: SJ-1 nanoparticles at a concentration of 20 μM showed effective reactive oxygen species (ROS) production and could induce almost 90% decrease of cell viability under laser irradiation in Hela and HT-29 cells, with negligible dark toxicity. Conclusion: In vitro results indicated that SJ-1 may be a potential PS for PDT.