Effects of 4',7-dimethoxyflavanone on cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.

The present study was designed to investigate the anticancer activity of 4,7-dimethoxyflavanone in vitro. When human breast cancer MCF-7 cells were treated with 4',7-dimethoxyflavanone at various concentrations (1-200 μM) for 24 h, antiproliferative effects were first observed at 1 μM and the IC(50) was 115.62 μM. Conversely, 4',7-dimethoxyflavanone was not cytotoxic (measured as lactate dehydrogenase release in CHO-K1 cells) under the same conditions. MCF-7 cells exposed to the 4',7-dimethoxyflavanone at the IC(50) concentration showed cell cycle arrest and apoptosis. Compared to the respective control level, exposure to 4',7-dimethoxyflavanone resulted in a remarkable increase of small DNA fragments at the sub-G1 phase and an increase in the G2/M phase cell population. Moreover, when 4',7-dimethoxyflavanone treatment caused G2/M phase arrest, an increase in CDK1 together with an increase in cyclin B was observed. Based on these results, 4',7-dimethoxyflavanone may be a useful anticancer agent.