Synthesis and effects on cell viability of flavonols and 3-methyl ether derivatives on human leukemia cells

Flavonoids are polyphenolic compounds which display an array of biological activities and are considered potential antitumor agents. Here we evaluated the antiproliferative activity of selected synthetic flavonoids against human leukemia cell lines. We found that 4′-bromoflavonol (flavonol 3) was the most potent. This compound inhibited proliferation in a concentration-dependent manner, induced apoptosis and blocked cell cycle progression at the S phase. Cell death was found to be associated with the cleavage and activation of multiple caspases, the activation of the mitogen-activated protein kinase pathway and the up-regulation of two death receptors (death receptor 4 and death receptor 5) for tumor necrosis factor-related apoptosis-inducing ligand. Moreover, combined treatments using 4′-bromoflavonol and TRAIL led to an increased cytotoxicity compared to single treatments. These results provide a basis for further exploring the potential applications of this combination for the treatment of cancer.

Bibliographic Details

Main Authors:	Burmistrova, Olga, Marrero, María Teresa, Estévez, Sara, Welsch, Isabel, Brouard, Ignacio, Quintana, José, Estévez, Francisco
Other Authors:	Ministerio de Ciencia e Innovación (España)
Format:	artículo biblioteca
Published:	Elsevier 2014-09-12
Subjects:	Death receptors, Flavonoids, Apoptosis, Cytotoxicity, Cell cycle, Caspases,
Online Access:	http://hdl.handle.net/10261/179981 http://dx.doi.org/10.13039/501100000780 http://dx.doi.org/10.13039/501100003339 http://dx.doi.org/10.13039/501100004837
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