A marine sponge Fascaplysinopsis sp. derived alkaloid fascaplysin inhibits the HepG2 hepatocellular carcinoma cell

Recently, marine sponge drug fascaplysin has been found to have the potential to overcome cancer, particularly those of hepatocellular carcinoma. In this study, the decreased cell viability of HepG2 cells treated by fascaplysin was identified by MTT assay at very low IC₅₀ concentration (1 µmolL⁻¹). The morphological evidence of both acridine orange/ethidium bromide (AO/EB) and Hoechst 33342 staining assays confirmed the increased cell death of the treated HepG2 cells and the red nucleus of the cells noticed that the chromatin condensation of apoptosis also occurred at IC₅₀ concentration of fascaflycin. Consequently, the HepG2 cell apoptosis induced by fascaplysin was proved by the translocation of phosphatidylserine exhaustion of DNA fragmentation, the activation of caspase-3, caspase-8 and caspase-9, and poly (ADP-ribose) polymerase cleavage. The results of western blot and quantitative PCR methods suggested that fascaplysin down-regulated the expression of BCL-2, up-regulated expression of p53, increased cleavage of caspase-3, caspase-8 and caspase-9 to activate caspase dependent apoptosis in HCC cells and cleared the induction of G0/G1 cell cycle arrest. Furthermore, fascaplysin inhibited migration and invasion of HepG2 cells by suppressing expression of MMP-2 and MMP-9 were clearly stated, the selected drug was potent anticancer activity against HepG2 cells. Hence, it is concluded in this study that marine sponge derived fascaplysin has the excellent inhibitory ability against HepG2 cancer cells.