title: KHC-4 anti-cancer effects on human PC3 prostate cancer cell line.
abstract: A bicyclic chemical structure, such as that found in flavonoids, was discovered to have anti-cancer activity. Further synthetic structural modification created a series of 2-phenyl-4-quinolone analogs, especially KHC-4, with the same bicyclic chemical structure. This new structure was reported to have stronger anti-cancer activity. In KHC-4 treatments for 72 h on human prostate cancer PC3 cells, cytotoxic effects (IC(50) =0.1 μM) increased dose dependently, causing Cdk1/cyclin B1 complex activity mannered cell cycle and proliferation. KHC-4 treatments suppressed Bcl-2 and Bcl-xL protein levels and upregulated Bax. At the same concentration, pro-caspase 9 protein was cleaved to an activated form, leading to cell apoptosis. Furthermore, the MMP-2 protein levels also decreased through KHC-4 treatment in PC3. In conclusion, KHC-4 presents great prostate cancer therapeutic effects for cell proliferation inhibition, induction of apoptosis and protection against tumor migration.
authors.affiliation: School of Applied Chemistry, Chung Shan Medical University, Taichung,  Taiwan , Institute of Medicine, Chung Shan Medical University, Taichung,  Taiwan.
authors.forename: Jin-Ming
authors.initials: JM
authors.lastname: Hwang
authors.forename: Wei-Jen
authors.initials: WJ
authors.lastname: Ting
authors.forename: Hsi-Chin
authors.initials: HC
authors.lastname: Wu
authors.forename: Yi-Jyun
authors.initials: YJ
authors.lastname: Chen
authors.forename: Fu-Jenn
authors.initials: FJ
authors.lastname: Tsai
authors.forename: Po-Yuan
authors.initials: PY
authors.lastname: Chen
authors.forename: Chin-Yu
authors.initials: CY
authors.lastname: Liu
authors.forename: Li-Chen
authors.initials: LC
authors.lastname: Chou
authors.forename: Sheng-Chu
authors.initials: SC
authors.lastname: Kuo
authors.forename: Chih-Yang
authors.initials: CY
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D053453:Caspase 9 / Q000378:metabolism; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056744:Cyclin B1 / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000737:chemistry*; D006801:Humans; D008297:Male; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D009025:Morpholines / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D051028:bcl-2-Associated X Protein / Q000378:metabolism; D051020:bcl-X Protein / Q000378:metabolism
chemical_list: C577043:2'-fluoro-6-morpholinyl-2-phenyl-4-quinolone; D000970:Antineoplastic Agents; D056744:Cyclin B1; D005419:Flavonoids; D009025:Morpholines; D019253:Proto-Oncogene Proteins c-bcl-2; D015363:Quinolones; D051028:bcl-2-Associated X Protein; D051020:bcl-X Protein; D053453:Caspase 9; C522361:MMP2 protein, human; D020778:Matrix Metalloproteinase 2