A triphenylphosphine-coordinated copper(I) complex with aggregation-induced emission characteristics for chemodynamic therapy.

Cu(I)-mediated Fenton-like catalytic performance has been extensively explored in chemodynamic therapy (CDT) due to its excellent reactive oxygen species (ROS) production. Integration of its specific Cu(I)-mediated CDT functions with customized aggregation-induced emission (AIE) luminogens to achieve efficient therapeutics and specific bioimaging of tumors is highly desirable but rarely studied. Herein, a novel triphenylamine (TPA)-modified AIE-active ligand and triphenylphosphine (TPP)-coordinated copper(I) complex (denoted as DPB-OD-Cu) was fabricated and accurately characterized. Owing to the restriction of the two rotatable parts of TPA and TPP units to motion in poor and high viscosity solvents, DPB-OD-Cu exhibits strong AIE behavior. Besides, the obtained DPB-OD-Cu exhibited high cytotoxicity and tumor suppression effect due to the conversion of intracellular hydrogen peroxide (H2O2) into cytotoxic hydroxyl radicals (˙OH) in the presence of Cu(I), thereby increasing oxidative stress, leading to the apoptosis of cancer cells. Furthermore, DPB-OD-Cu has shown specific mitochondrial imaging performance in NCI-H460 cancer cells. Therefore, the integration of Cu(I)'s Fenton-like reaction with functional AIEgens will advance the development of cell/subcellular-targeted CDT agents for image-guided therapy, opening new therapeutic opportunities.