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.
Subject(s)
Drug Discovery , Flavones/pharmacology , NF-kappa B/antagonists & inhibitors , Signal Transduction/drug effects , Apoptosis/drug effects , Cell Cycle/drug effects , Cell Line, Tumor , Cell Movement/drug effects , Dose-Response Relationship, Drug , Flavones/chemical synthesis , Flavones/chemistry , Humans , Molecular Structure , NF-kappa B/metabolism , Structure-Activity RelationshipABSTRACT
An alphasatellite DNA associated with Okra enation leaf curl virus (OELCuV) which causes enation and leaf curling in okra (Abelmoschus esculentus) plants was characterized. The full-length DNA comprises 1,350 nucleotides and shows typical genome organization of an alphasatellite. It shows the highest nucleotide sequence identity (79.7 %) to Hollyhock yellow vein virus-associated symptomless alphasatellite (HoYVSLA). This is the first report of the association of an alphasatellite with OELCuV from India.
Subject(s)
Abelmoschus/virology , Begomovirus/genetics , DNA, Satellite/chemistry , DNA, Satellite/genetics , Plant Diseases/virology , Cluster Analysis , DNA, Satellite/isolation & purification , India , Molecular Sequence Data , Phylogeny , Sequence Analysis, DNA , Sequence Homology, Nucleic AcidABSTRACT
N-(2-Methylphenyl)-2,2-dichloroacetamide (2MPA) and N-(4-methylphenyl)-2,2-dichloroacetamide (4MPA) of the configuration X(y)C(6)H(5-y)-NHCO-CHCl(2) (where, X=CH(3) and y=1) were synthesised and an extensive spectroscopic investigations have been carried out by recording the Fourier transform infrared (FTIR) and FT-Raman spectra and subjecting them to normal co-ordinate analysis, in an effort to provide mixing of the fundamental modes with the help of potential energy distribution (PED). The ab initio and DFT studies were carried out with 6-311++G(d,p) basis set to determine the structural, thermodynamical and vibrational characteristics of the compounds and also to understand the steric influence of methyl group on the characteristic frequencies of amide (-CONH-) group.
