摘要：Uvaretin, isouvaretin and diuvaretin, cytotoxic C -benzylated dihydrochalcones isolated from Uvaria acuminata , displayed growth inhibitory effects against human promyelocytic leukemia HL-60 cells. We examined the mechanism of the cytotoxicity. From the morphological study by staining with Hoechst 33258, the cells treated with C -benzylated dihydrochalcones exhibited significant chromosomal condensation and nuclear degradation. The cell cycle analysis showed the accumulation of cells in the G1 phase and the appearance of a sub-G1 peak. These results suggest apoptotic cell death. Further, from the detection of DNA fragmentation and the activation of caspase-3, the biological hallmarks of apoptosis, these C -benzylated dihydrochalcones appeared to induce apoptosis against HL-60 cells. The cytotoxicity of uvaretin and diuvaretin was stronger than that of isouvaretin, which suggest that the 5′-substitution of the 2-hydroxybenzyl group increased the cytotoxicity.
关键词：C-benzylated dihydrochalcone;cytotoxicity against HL-60 cell;apoptosis;uvaretin;diuvaretin;isouvaretin
