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Updated: Jun 29, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
Phenolic constituents of Amorpha fruticosa that inhibit NF-kappaB activation and related gene expression
Nguyen Tien Dat1, Jeong-Hyung Lee, Kyeong Lee
1Molecular Cancer Research Center, Korean Research Institute of Biosciences and Biotechnology, Daejeon, Korea.
Abstract:
NF-kappaB is known to play a crucial role in the regulation of genes controlling the immune system, apoptosis, tumor cell growth, and tissue differentiation. Bioassay-guided fractionation of the n-hexane-soluble fraction of a methanol extract of Amorpha fruticosa afforded four new compounds, 5, 7, 8, and 9, and eight known compounds. Their structures were elucidated by spectroscopic methods. All compounds inhibited NF-kappaB activity, and tephrosin (1), 11-hydroxytephrosin (2), and deguelin (3) were the most active, with IC50 values of 0.11, 0.19, and 0.22 microM, respectively, in TNF-alpha-stimulated HeLa cell-based reporter gene assays. Further investigations showed that compounds 1, 5, and 6 blocked NF-kappaB/DNA binding activity and suppressed the expression of NF-kappaB target genes.
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