Inhibitors of the NF-κB Activation Pathway from Cryptocarya rugulosa

The nuclear factor-κB (NF-κB) signaling pathway is constitutively active in many types of cancers and is a potential therapeutic target. Using a cell-based assay for stability of inhibitor of kappa B (IκB), a critical regulator of NF-κB activity, we found that an organic solvent extract of the plant...

Full description

Saved in:
Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2009-03, Vol.72 (3), p.336-339
Main Authors: Meragelman, Tamara L, Scudiero, Dominic A, Davis, R. Eric, Staudt, Louis M, McCloud, Thomas G, Cardellina, John H, Shoemaker, Robert H
Format: Article
Language:English
Subjects:
alpha-pyrone
carcinogenesis
Cryptocarya
Cryptocarya rugulosa
cryptocaryone
humans
rugulactone
signal transduction
transcription factors
transcriptional activation
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The nuclear factor-κB (NF-κB) signaling pathway is constitutively active in many types of cancers and is a potential therapeutic target. Using a cell-based assay for stability of inhibitor of kappa B (IκB), a critical regulator of NF-κB activity, we found that an organic solvent extract of the plant Cryptocarya rugulosa inhibited constitutive NF-κB activity in human lymphoma cell lines. The active components were identified as rugulactone, a new α-pyrone (1), and the known cryptocaryone (2). Rugulactone was the more active compound, exhibiting up to 5-fold induction of IκB at 25 μg/mL; maximal activity was observed with 10 h exposure of test cells to 1 or 2.
ISSN:0163-3864
1520-6025
DOI:10.1021/np800350x