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Discovery of Lesser Known Flavones as Inhibitors of NF-κB Signaling in MDA-MB-231 Breast Cancer cells--A SAR Study

Discovery of Lesser Known Flavones as Inhibitors of NF-κB Signaling in MDA-MB-231 Breast Cancer cells--A SAR Study

K Amrutha, Pandurangan Nanjan, Sanu K Shaji, Damu Sunilkumar, K Subhalakshmi, Lakshmi Rajakrishna, Asoke Banerji

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4735-4742.

PMID: 25190466

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP86749511	Gossypetin 3-methylether		86749-51-1	Price

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