Novel anthraquinone derivatives: Synthesis via click chemistry approach and their induction of apoptosis in BGC gastric cancer cells via reactive oxygen species(ROS)-dependent mitochondrial pathway

Three water soluble anthraquinone derivatives were designed and synthesized employing click chemistry to prepare novel and potent antitumor drugs. An MTT assay indicated that all compounds had significant inhibitory activity against BGC gastric cancer cells in vitro. Apoptosis induced by these compounds was observed by flow cytometry and laser confocal microscopy. Mechanistic analysis showed that these compounds induced the generation of several reactive oxygen species, the loss of mitochondrial membrane potential (Δψm), the transition of mitochondrial permeability, and the release of cytochrome C from the mitochondrion to cytoplasm. These results suggest that the anthraquinones might be potential lead compounds for the cancer chemotherapy.

Graphical abstractThree water soluble anthraquinone derivatives were synthesized via employing click chemistry and the mechanistic study of the apoptotic induction was conducted in this paper.Figure optionsDownload full-size imageDownload as PowerPoint slide