Identification of 11(13)-dehydroivaxillin as a potent therapeutic agent against non-Hodgkin's lymphoma

Cell Death Dis. 2017 Sep 14;8(9):e3050. doi: 10.1038/cddis.2017.442.

Abstract

Despite great advancements in the treatment of non-Hodgkin lymphoma (NHL), sensitivity of different subtypes to therapy varies. Targeting the aberrant activation NF-κB signaling pathways in lymphoid malignancies is a promising strategy. Here, we report that 11(13)-dehydroivaxillin (DHI), a natural compound isolated from the Carpesium genus, induces growth inhibition and apoptosis of NHL cells. Multiple signaling cascades are influenced by DHI in NHL cells. PI3K/AKT and ERK are activated or inhibited in a cell type dependent manner, whereas NF-κB signaling pathway was inhibited in all the NHL cells tested. Applying the cellular thermal shift assay, we further demonstrated that DHI directly interacts with IKKα/IKKβ in NHL cells. Interestingly, DHI treatment also reduced the IKKα/IKKβ protein level in NHL cells. Consistent with this finding, knockdown of IKKα/IKKβ inhibits cell proliferation and enhances DHI-induced proliferation inhibition. Overexpression of p65, p52 or RelB partially reverses DHI-induced cell growth inhibition. Furthermore, DHI treatment significantly inhibits the growth of NHL cell xenografts. In conclusion, we demonstrate that DHI exerts anti-NHL effect in vitro and in vivo, through a cumulative effect on NF-κB and other pathways. DHI may serve as a promising lead compound for the therapy of NHL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Enzyme Activation / drug effects
  • Gene Knockdown Techniques
  • Humans
  • I-kappa B Kinase / metabolism
  • Lymphoma, Non-Hodgkin / drug therapy*
  • Lymphoma, Non-Hodgkin / genetics
  • Lymphoma, Non-Hodgkin / pathology
  • Mice, SCID
  • NF-kappa B / genetics
  • NF-kappa B / metabolism
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / pharmacology
  • Sesquiterpenes / therapeutic use*
  • Transcription, Genetic / drug effects
  • Tumor Necrosis Factor-alpha / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • 11(13)-dehydroivaxillin
  • NF-kappa B
  • Sesquiterpenes
  • Tumor Necrosis Factor-alpha
  • I-kappa B Kinase