2-Hydroxy-3,4-naphthochalcone (2H-NC) inhibits TNFα-induced tumor invasion through the downregulation of NF-κB-mediated MMP-9 gene expression

Bioorg Med Chem Lett. 2015 Jan 1;25(1):128-32. doi: 10.1016/j.bmcl.2014.10.086. Epub 2014 Nov 1.

Abstract

The control of tumor metastasis is important for the successful prevention and treatment of cancer. Emerging evidence indicates that various natural and synthetic chalcones exhibit antimetastatic activity through the inhibition of nuclear factor-κB (NF-κB), although the precise mechanism by which this occurs is currently unclear. In this study, 2-hydroxy-3,4-naphthochalcone (2H-NC) was found to reduce tumor necrosis factor alpha (TNFα)-induced MMP-9 mRNA expression and gelatinolytic enzyme activity. These actions were associated with inhibition of RelA/p65 NF-κB activity. In addition, 2H-NC inhibited TNFα-induced invasion of MDA-MB-231 breast cancer cells, as assessed using a three-dimensional spheroid invasion assay. Taken together, these data demonstrate that 2H-NC prevents TNFα-induced tumor cell invasion through downregulation of NF-κB-mediated MMP-9 gene expression, and thereby identify naphthochalcones as a potentially effective class of molecules to use as a platform for the development of antimetastatic agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Chalcones / chemistry*
  • Chalcones / pharmacology
  • Down-Regulation / drug effects
  • Down-Regulation / physiology
  • Female
  • Humans
  • Matrix Metalloproteinase 9 / biosynthesis*
  • NF-kappa B / metabolism*
  • Naphthalenes / chemistry*
  • Naphthalenes / pharmacology
  • Neoplasm Invasiveness / prevention & control
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*
  • Tumor Necrosis Factor-alpha / toxicity

Substances

  • Chalcones
  • NF-kappa B
  • Naphthalenes
  • Tumor Necrosis Factor-alpha
  • MMP9 protein, human
  • Matrix Metalloproteinase 9