Orlikova, B., Tasdemir, D., Golais, F., Dicato, M. and Diederich, M. (2011) The aromatic ketone 4'-hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. Biochemical pharmacology, 82 (6). pp. 620-631. 10.1016/j.bcp.2011.06.012.
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Chalcones are aromatic ketones, known to exhibit anti-microbial, anti-inflammatory and anti-cancer activities. The aim of this study was to investigate the anti-inflammatory and anti-cancer activity of 4'-hydroxychalcone. Here, we report that 4'-hydroxychalcone inhibits TNFα-induced NF-κB pathway activation in a dose-dependent manner. To investigate the underlying molecular mechanisms we demonstrate that 4'-hydroxychalcone inhibits proteasome activity in a dose-dependent manner but has no effect on IKK activity. Results show that 4'-hydroxychalcone inhibits TNFα-dependent degradation of IκBα and subsequently prevents p50/p65 nuclear translocation leading to 4'-hydroxychalcone-inhibited expression of NF-κB target genes. Most importantly, inhibition of NF-κB activation by 4'-hydroxychalcone is not leukemia cell-type specific and has no significant effect on non-transformed cell viability, thus highlighting the compound's potential in both prevention and treatment.
|Uncontrolled Keywords:||Cancer; Chalcone; Inflammation; NF-κB; Polyphenol|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||Biochemical pharmacology|
|Deposited By:||Library Staff|
|Deposited On:||09 Mar 2012 16:12|
|Last Modified:||09 Mar 2012 16:12|
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