Anti-tumor activity evaluation of novel chrysinaorganogermanium(IV) complex in MCF-7 cells

Chrysin (5,7-dihydroxylflavone, Chry) is a natural product extracted from plants, honey, and propolis. In this work, a novel chrysinaorganogermanium(IV) complex (ChryaGe) with enhanced anticancer activities was synthesized, and its potential anticancer effects against cancer cells were measured using various methods. MTT results showed that ChryaGe had significant inhibition effects on the proliferation of MCF-7, HepG2 and Colo205 human cancer cell lines in a dose-dependent manner while had little cytotoxic effects on MCF-10A human normal cells (MCF-10A cells) with the same treatment of ChryaGe. These results suggested that ChryaGe possessed enhanced anticancer effects and high selectivity between cancer cells and normal cells. The immuno-staining results showed that the nuclei of MCF-7 cells represented a total fragmented morphology and a disorganized cytoskeletal network in MCF-7 cells after ChryaGe treatment. Besides, atomic force microscopy (AFM) was applied to detect the changes of ultrastructural and biomechanical properties of MCF-7 cellular membrane induced by ChryaGe. The AFM data indicated that ChryaGe treatment directly caused the decrease of cell rigidity and adhesion force of MCF-7 cells, suggesting that membrane toxicity might be one of the targets for ChryaGe in MCF-7 cells. Moreover, the fluorescence-based flow cytometric analysis demonstrated that ChryaGe could induce apoptosis in MCF-7 cells in ROS-dependent mitochondrial pathway. All results collectively showed that ChryaGe could be as a promising anticancer drug for cancer therapy.