Anti-tumor activity evaluation of novel chrysin-organogermanium(IV)
complex in MCF-7 cells
Bioorg Med Chem Lett, 2013 Aug 19. pii:
S0960-894X(13)00995-5
Chrysin (5,7-dihydroxylflavone, Chry) is a natural product
extracted from plants, honey, and propolis. In this work, a novel
chrysin-organogermanium(IV) complex (Chry-Ge) with enhanced anticancer
activities was synthesized, and its potential anticancer effects against cancer
cells were measured using various methods.
MTT results showed that Chry-Ge 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 Chry-Ge. These
results suggested that Chry-Ge 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 Chry-Ge treatment.
Besides, atomic force microscopy (AFM) was applied to detect the changes of
ultrastructural and biomechanical properties of MCF-7 cellular membrane induced
by Chry-Ge.
The AFM data indicated that Chry-Ge 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 Chry-Ge in
MCF-7 cells. Moreover, the fluorescence-based flow cytometric analysis
demonstrated that Chry-Ge could induce apoptosis in MCF-7 cells in
ROS-dependent mitochondrial pathway.
All results collectively showed that Chry-Ge could be as a
promising anticancer drug for cancer therapy.
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