title: Anti-tumor activity evaluation of novel chrysin-organogermanium(IV) complex in MCF-7 cells.
abstract: 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.
authors.affiliation: Department of Chemistry of Jinan University, Guangzhou 510632, China.
authors.forename: Fen
authors.initials: F
authors.lastname: Yang
authors.forename: Hua
authors.initials: H
authors.lastname: Jin
authors.forename: Jiang
authors.initials: J
authors.lastname: Pi
authors.forename: Jin-huan
authors.initials: JH
authors.lastname: Jiang
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.forename: Hai-hua
authors.initials: HH
authors.lastname: Bai
authors.forename: Pei-hui
authors.initials: PH
authors.lastname: Yang
authors.forename: Ji-Ye
authors.initials: JY
authors.lastname: Cai
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D020169:Caspases / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D005419:Flavonoids / Q000737:chemistry*; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D005857:Germanium / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D020782:Matrix Metalloproteinases / Q000378:metabolism; D018625:Microscopy, Atomic Force; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D005419:Flavonoids; D017382:Reactive Oxygen Species; D005857:Germanium; C043561:chrysin; D020169:Caspases; D020782:Matrix Metalloproteinases
keywords: Atomic force microscopy (AFM); Chrysin; Chry–Ge; MCF-7