The cytotoxic effect of 2-acylated-1,4-naphthohydroquinones on leukemia/lymphoma cells

Here, we tested seven 2-acylated-1,4-hydronaphthoquinones for their cytotoxic effects on a panel of cancer lymphoma/leukemia cells and compared to a non-cancer origin cell line. Several naphthohydroquinones exhibited selective cytotoxic effects on lymphoma/leukemia cells with lowest activity on non-cancer cells. The mode of cell death induced by an acylated naphthohydroquinone, which has a long alkyl chain, was found to be via apoptosis. Furthermore, the naphthohydroquinone provoked mitochondria depolarization and activation of its downstream effector, caspase-3, thus implicating the intrinsic apoptotic pathway as its mechanism to exert cell death.

The toxicity against leukemia/lymphoma CEM/Jurkat/Nalm-6/Ramos cells is: IC50 = 5.99/6.56/5.80/0.98 μM. Significant less cytotoxicity was exerted on non-cancerous Hs27 cells: IC50 = 43.75 μM. The death program was initiated via mitochondria depolarization, implicating the intrinsic apoptotic pathway. The progression of the apoptosis was confirmed by the activation of its downstream effector, caspase-3.Figure optionsDownload as PowerPoint slide