- Discovery of lesser known flavones as inhibitors of NF-κB signaling in MDA-MB-231 breast cancer cells - A SAR study
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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.
- Amrutha,Nanjan, Pandurangan,Shaji, Sanu K.,Sunilkumar, Damu,Subhalakshmi,Rajakrishna, Lakshmi,Banerji, Asoke
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p. 4735 - 4742
(2015/01/08)
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- COMPOUNDS FOR IMMUNOPOTENTIATION
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Methods of stimulating an immune response and treating patients responsive thereto with 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-diones, staurosporine analogs, derivatized pyridazines, chromen-4-ones, indolinones, quinazolines, nucleoside analogs, and other small molecules are disclosed.
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Page/Page column 122
(2010/02/15)
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- Peroxidase from cell cultures of cassia didymobotrya: A review and comparison with horseradish peroxidase
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The catalytic activity on flavonoids and dibenzylbutanolides and the specificity of the peroxidase isolated from 29d-old cell cultures of Cassia didymobotrya are reported. Studies on several substrates in comparison with horseradish peroxidase revealed pe
- Botta, Bruno,Ricciardi, Paola,Vitali, Alberto,Vinciguerra, Vittorio,Garcia, Carlos,Delle Monache, Giuliano
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p. 757 - 766
(2007/10/03)
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- Flavonoids, 45 . A General and Efficient Synthesis of Hydroxyflavones and -chromones
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An efficient and versatile method for the synthesis of flavones hydroxylated in either ring A or B and of chromones hydroxylated in is described.This approach is based on the acidic resin-promoted cyclodehydration and simultaneous deprotection of methoxymethoxylated 1-(2-hydroxyphenyl)propane-1,3-diones easily available by either the Baker-Venkataraman rearrangement or the Claisen condensation. - Key words: Amberlyst 15 / Baker-Venkataraman rearrangement / Claisen condensation / hydroxychromone / hydroxyflavone / methoxymethyl protection
- Patonay, Tamas,Molnar, Denes,Muranyi, Zoltan
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p. 233 - 242
(2007/10/02)
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