Inhibitors Of The Nf-Kappa B Activation Pathway From Cryptocarya Rugulosa

The nuclear factor-kappa B (NF-kappa B) 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 (I kappa B), a critical regulator of NF-kappa B activity, we found that an organic solvent extract of the plant Cryptocarya rugulosa inhibited constitutive NF-kappa B activity in human lymphoma cell lines. The active components were identified as rugulactone, a new alpha-pyrone (1), and the known cryptocaryone (2). Rugulactone was the more active compound, exhibiting up to 5-fold induction of I kappa B at 25 mu g/mL; maximal activity was observed with 10 h exposure of test cells to 1 or 2.