Journal
TOXICOLOGY IN VITRO
Volume 24, Issue 5, Pages 1347-1355Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tiv.2010.04.013
Keywords
Chalcones; Anti proliferative; Antiangiogenic
Categories
Funding
- Slovak Research and Development Agency [APVV-0325-07]
- Slovak Grant Agency for Science [1/4236/07]
- LABMED
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As flavonoids, chalcones possess a wide variety of biological activities including anticancer properties. In the present study we have investigated the in vitro antiproliferative and antiangiogenic effects of four synthetic chalcones. E-2-(4'-methoxybenzylidene)-1-benzosuberone (3) was the most active compound with IC50= 10(-7) mol l(-1) in Jurkat cells. In both Jurkat and HeLa chalcone 3-treated cells we found a significant increase in the proportion of cancer cells in the G(2)/M phase of the cell cycle as well as an increase in cells having sub-G(0)/G(1) DNA content which is considered to be a marker of apoptotic cell death. Apoptosis was also confirmed by annexin V staining and DNA fragmentation. These effects were associated with reduced expression of the anti-apoptotic gene, Bcl-2, and increased expression of the pro-apoptotic gene, Bax. Furthermore, chalcone 3 was selected to evaluate its effect on some angiogenic events. In non-toxic concentrations, chalcone 3 inhibited VEGF-induced migration of human umbilical vein endothelial cells. Moreover, it also decreased secretion of matrix metalloproteinase (mainly MMP-9) and vascular endothelial growth factor (VEGF). In conclusion, the present study has assessed the in vitro antiproliferative/antiangiogenic potential of chalcone 3. This results generate a rationale for in vivo efficacy studies with this compound in preclinical cancer models. (C) 2010 Elsevier Ltd. All rights reserved.
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