Apoptotic Induction of Mitochondria-Anchored Aggregation-Induced Emission Luminogens through the Intrinsic Mitochondrial Pathway.

Gastric cancer has the third highest mortality rate globally. Chemotherapy is the primary treatment used in advanced gastric cancer. Aggregation-induced emission luminogens (AIEgens) have been exploited as non-toxic and efficient chemotherapy agents for the treatment of cancer. Our previous research demonstrated that tetraphenylethene-substituted pyridinium salt (TPE-Py) is a kind of AIEgen that had the ability to lead to apoptosis in gastric cancer cells. However, it is currently unknown whether TPE-Py induced apoptosis in gastric cancer cells by the mitochondria-mediated pathway. This research confirmed that TPE-Py could target mitochondria and induce apoptotic cell death. In addition, several well-recognized indicators were detected to investigate the functional and morphological changes of mitochondria. We found that TPE-Py could diminish the mitochondrial membrane potential and increase the accumulation of reactive oxygen species and the discharge of cytochrome c , which was related to the mitochondrial apoptotic pathway. Meanwhile, morphological changes in mitochondria were also observed by transmission electron microscopy in gastric cancer cells after incubation with TPE-Py. In conclusion, we provided insights into the mechanism regulating apoptosis in gastric cancer cells and elucidated the mechanism of apoptosis induced by TPE-Py via the intrinsic mitochondrial pathway.