Publication Type:

Journal Article


Bioorganic and Medicinal Chemistry Letters, Pergamon, Volume 24, Issue 19, p.4735-4742 (2014)



2, 3 dihydrochrysoeriol, 3 dihydroisorhamnetin, 5, 5 deoxychrysoeriol, 7 dideoxychrysoeriol, acacetin, apigenin, apoptosis, article, breast cancer cell line, cell cycle, cell proliferation, chrysoeriol, controlled study, diosmetin, flavone, flavone derivative, G2 phase cell cycle checkpoint, galangin, gene expression, gossypetin, immunoglobulin enhancer binding protein, isorhamnetin, kaempferide, kaempferol, luteolin, metastasis, quercetagetin, quercetin, signal transduction, structure activity relation, tamarixetin, unclassified drug


<p>Seventeen flavonoids with different substitutions were evaluated for inhibition of nuclear factor-κB (NF-κB) signaling in the invasive breast cancer cell line MDA-MB-231. They were screened using an engineered MDA-MB-231 cell line reporting NF-κB activation. The modulation of expression of two NF-κB regulated genes involved in tumorigenesis, matrix metalloproteinase-9 (MMP-9), and cyclooxygenase-2 (COX-2) were also analyzed in these cells. Among the compounds tested, all except gossypetin and quercetagetin inhibited the activation of NF-κB, and the expression of MMP-9 and COX-2 to different degree. Methylated flavone, chrysoeriol (luteolin-3′-methylether), was found to be the most potent inhibitor of MMP-9 and COX-2 expressions. The effect of chrysoeriol on cell proliferation, cell cycle, apoptosis and metastasis was analyzed by established methods. Chrysoeriol caused cell cycle arrest at G2/M and inhibited migration and invasion of MDA-MB-231 cells. The structure-activity relations amongst the flavonoids as NF-κB signaling inhibitors was studied. The study indicates differences between the actions of various flavonoids on NF-κB activation and on the biological activities of breast cancer cells. Flavones in general, were more active than the corresponding flavonols. © 2014 Elsevier Ltd. All rights reserved.</p>


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Cite this Research Publication

Ka Amrutha, Pandurangan Nanjan, Shaji, S. Ka, Sunilkumar, Da, Subhalakshmi, Ka, Rajakrishna, Lb, and Dr. Asoke Banerji, “Discovery of lesser known flavones as inhibitors of NF-κB signaling in MDA-MB-231 breast cancer cells-A SAR study”, Bioorganic and Medicinal Chemistry Letters, vol. 24, no. 19, pp. 4735-4742, 2014.