KHC-4 anti-cancer effects on human PC3 prostate cancer cell line.

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.