Phenolic constituents of Amorpha fruticosa that inhibit NF-kappaB activation and related gene expression

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Title
Phenolic constituents of Amorpha fruticosa that inhibit NF-kappaB activation and related gene expression
Author(s)
N T Dat; J H Lee; Kyeong Lee; Young-Soo Hong; Y H Kim; Jung Joon Lee
Bibliographic Citation
Journal of Natural Products, vol. 71, no. 10, pp. 1696-1700
Publication Year
2008
Abstract
NF-κB 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-κB 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 μM, respectively, in TNF-α-stimulated HeLa cell-based reporter gene assays. Further investigations showed that compounds 1, 5, and 6 blocked NF-κB/DNA binding activity and suppressed the expression of NF-κB target genes.
ISSN
0163-3864
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/np800383q
Type
Article
Appears in Collections:
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
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