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Molecules 2015, 20(1), 863-878;

Inhibition of the NF-κB Signaling Pathway by a Novel Heterocyclic Curcumin Analogue

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece
Laboratory of Protein Chemistry, Proteomics and Epigenetic Signaling (PPES), Department of Biomedical Sciences, University of Antwerp, Wilrijk 2610, Belgium
Laboratory of Eukaryotic Gene Expression and Signal Transduction (LEGEST), Department of Physiology, University of Ghent, Ghent 9000, Belgium
Author to whom correspondence should be addressed.
Academic Editor: Bharat B. Aggarwal
Received: 30 September 2014 / Accepted: 16 December 2014 / Published: 8 January 2015
(This article belongs to the Special Issue Curcumin, Inflammation, and Chronic Diseases: How are They Linked?)
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In this study a series of curcumin analogues were evaluated for their ability to inhibit the activation of NF-κΒ, a transcription factor at the crossroads of cancer-inflammation. Our novel curcumin analogue BAT3 was identified to be the most potent NF-κB inhibitor and EMSA assays clearly showed inhibition of NF-κB/DNA-binding in the presence of BAT3, in agreement with reporter gene results. Immunofluorescence experiments demonstrated that BAT3 did not seem to prevent nuclear p65 translocation, so our novel analogue may interfere with NF-κB/DNA-binding or transactivation, independently of IKK2 regulation and NF-κB-translocation. Gene expression studies on endogenous NF-κB target genes revealed that BAT3 significantly inhibited TNF-dependent transcription of IL6, MCP1 and A20 genes, whereas an NF-κB independent target gene heme oxygenase-1 remained unaffected. In conclusion, we demonstrate that BAT3 seems to inhibit different cancer-related inflammatory targets in the NF-κB signaling pathway through a different mechanism in comparison to similar analogues, previously reported. View Full-Text
Keywords: curcumin analogue; NF-κB; TNF; cancer; inflammation curcumin analogue; NF-κB; TNF; cancer; inflammation

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Katsori, A.-M.; Palagani, A.; Bougarne, N.; Hadjipavlou-Litina, D.; Haegeman, G.; Vanden Berghe, W. Inhibition of the NF-κB Signaling Pathway by a Novel Heterocyclic Curcumin Analogue. Molecules 2015, 20, 863-878.

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