期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 28, 期 1, 页码 83-86出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.28.83
关键词
C-benzylated dihydrochalcone; cytotoxicity against HL-60 cell; apoptosis; uvaretin; diuvaretin; isouvaretin
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 G(1) phase and the appearance of a sub-G(1) 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.
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