title: Anticancer effects of O-desmethylangolensin are mediated through cell             cycle arrest at the G2/M phase and mitochondrial-dependent apoptosis in Hep3B             human hepatocellular carcinoma cells.
abstract: In the present study, in order to investigate the anticancer effects of             O-desmethylangolensin (O-DMA) on human hepatocellular carcinoma Hep3B cells, we             first examined the antiproliferative effect of O-DMA. When Hep3B cells were treated             with O-DMA at various concentrations (5-200 µM) for 24, 48 or 72 h, cell proliferation             decreased significantly in a dose- and time-dependent manner. Moreover, O-DMA             exposure at the IC50 concentration for 72 h arrested cells at the G2/M phase,             which was accompanied by a reduction in CDK1, and an increase in cyclin A and B.             Under the same conditions, O-DMA significantly increased the number of sub-G1             phase cells. Additionally, an Annexin V assay revealed that exposure to O-DMA             affected the rate of cell apoptosis. O-DMA caused the downregulation of Bcl-2             and upregulation of Bax, which led to cytochrome c release from the mitochondria             and activation of caspase-3. Taken together, these data suggest that O-DMA exhibits             anticancer activity by arresting the cell cycle at G2/M phase and causing mitochondrial-dependent             apoptosis in Hep3B cells.
authors: Plant Resources Research Institute, Duksung Women's University, Tobong-ku, Seoul 132-714, Republic of Korea. ejchoi@duksung.ac.kr
authors: Eun Jeong
authors: EJ
authors: Choi
authors: Jae-In
authors: JI
authors: Lee
authors: Gun-Hee
authors: GH
authors: Kim
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D016203:CDC2 Protein Kinase / Q000096:biosynthesis; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019925:Cyclin A / Q000096:biosynthesis; D019926:Cyclin B / Q000096:biosynthesis; D045304:Cytochromes c / Q000378:metabolism; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects*; D006801:Humans; D007529:Isoflavones / Q000494:pharmacology*; D008113:Liver Neoplasms / Q000188:drug therapy*; D008928:Mitochondria / Q000378:metabolism; D048789:Phytoestrogens / Q000494:pharmacology; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000096:biosynthesis
chemical_list: D000970:Antineoplastic Agents; D019925:Cyclin A; D019926:Cyclin B; D007529:Isoflavones; D048789:Phytoestrogens; D019253:Proto-Oncogene Proteins c-bcl-2; D045304:Cytochromes c; D016203:CDC2 Protein Kinase; D053148:Caspase 3; C050052:O-desmethylangolensin