Anti-carcinogenic effect of a new analogue 4'-chloroflavanone from flavanone in human breast cancer cells.
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| Abstract |
We investigated the antiproliferative effects of synthetic flavanone derivatives using an MTT assay in MCF-7 and MDA-MB-453 cells. When cells were treated with synthetic flavanone derivatives in concentrations ranging from 1 to 200 microM for 48 h, cell growth decreased at concentrations >50 microM. 4'-Chloroflavanone is more potent than flavanone among the synthetic flavanone derivatives. Exposure to 4'-chloroflavanone at 50 microM for 48 h caused cell cycle arrest in both MCF-7 and MDA-MB-453 cells. In addition, when 4'-chloroflavanone caused G1/S phase arrest, a decrease in CDK4 and cyclin D, together with an increase in p21Cip1, was observed in the cells. The p21Cip1 is a downstream target of p53 that may be affected by the activation of p53 by 4'-chloroflavanone. These results indicate that activation of p53 played some role in 4'-chloroflavanone-induced cell cycle arrest of human breast cancer cells. 4'-Chloroflavanone increased cytochrome c expression and decreased the expression of caspase-3, but did not change the expression of Bcl-2 and Bax. Activation of cytochrome c and its downstream target, caspase-3, is suggested to be an important inducer of the apoptosis process by 4'-chloroflavanone. 4'-Chloroflavanone inhibits cell proliferation through G1/S phase disruption and may induce apoptosis. Based on our findings, we propose that 4'-chloro-flavanone is useful as an anticancer drug.
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| Authors | Eun Jeong Choi, Jae In Lee, Gun-Hee Kim |
| Journal | International journal of molecular medicine (Int J Mol Med) Vol. 25 Issue 2 Pg. 293-8 (Feb 2010) ISSN: 1791-244X [Electronic] Greece |
| PMID | 20043141 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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