germanium and chrysin

Organogermanium(IV) (Ge) is considered to play an important role in the anti-oxidative activities of some Chinese medicines. Here, a new chrysin-organogermanium (Chry-Ge) complex was synthesized and investigated for its potential biological activities. The radicals-sensitive Ge-O bond was introduced to Chry-Ge complex to enhance bioactivities of organic Ge or Chry. Results showed that Chry-Ge complex possessed great anti-oxidative activities, showing stronger hydroxyl scavenging effects than their corresponding ligands. We also demonstrated Chry-Ge complex inhibited ROS-dependent oxidative damage in cells. Moreover, the morphological and biophysical recoveries in oxidation-damaged cells induced by Chry-Ge complex were characterized by atomic force microscopy. All these results collectively suggested that Chry-Ge complex has synergetic effect for radicals scavenging and could be served as promising pharmacologically active agent against anti-oxidative treatment.

Topics: Animals; Antioxidants; Cell Line; Coordination Complexes; Elastic Modulus; Flavonoids; Germanium; Hydroxyl Radical; Microscopy, Atomic Force; Oxidative Stress; Rats

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.

Topics: Antineoplastic Agents; Apoptosis; Caspases; Cell Line, Tumor; Cell Proliferation; Coordination Complexes; Flavonoids; G2 Phase Cell Cycle Checkpoints; Germanium; Hep G2 Cells; Humans; Matrix Metalloproteinases; MCF-7 Cells; Microscopy, Atomic Force; Reactive Oxygen Species