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Inhibitors of the NF-kappaB activation pathway from Cryptocarya rugulosa

  1. Author:
    Meragelman, T. L.
    Scudiero, D. A.
    Davis, R. E.
    Staudt, L. M.
    McCloud, T. G.
    Cardellina, J. H. 2nd.
    Shoemaker, R. H.

  2. Author Address

    Screening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, Maryland, USA.
    1. Year: 2009
    2. Date: Mar 27
    3. Epub Date: 12/20/2008
  2. Journal: Journal of Natural Products
    1. 72
    2. 3
    3. Pages: 336-9
  4. Type of Article: Article
  5. ISSN: 1520-6025 (Electronic);0163-3864 (Linking)
  1. Abstract:

    The nuclear factor-kappaB (NF-kappaB) 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 (IkappaB), a critical regulator of NF-kappaB activity, we found that an organic solvent extract of the plant Cryptocarya rugulosa inhibited constitutive NF-kappaB 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 IkappaB at 25 microg/mL; maximal activity was observed with 10 h exposure of test cells to 1 or 2.

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  2. DOI: 10.1021/np800350x
  3. PMID: 19093800

Library Notes

  1. Fiscal Year: FY2008-2009
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