Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation

FEBS Lett. 2004 Jul 30;571(1-3):50-4. doi: 10.1016/j.febslet.2004.06.056.


4-Methyl-N1-(3-phenyl-propyl)-benzene-1,2-diamine (JSH-23) is a novel chemically synthetic compound. The aromatic diamine JSH-23 compound exhibited inhibitory effect with an IC(50) value of 7.1 microM on nuclear factor (NF)-kappaB transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7, and interfered LPS-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. This mechanism of action is very rare for controlling NF-kappaB activation. Furthermore, the compound inhibited not only LPS-induced expressions of tumor necrosis factor-alpha, interleukin (IL)-1beta, IL-6 and inducible nitric oxide synthase and cyclooxygenase-2 but also LPS-induced apoptosis of the RAW 264.7 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Cell Nucleus / drug effects
  • Cell Nucleus / metabolism*
  • Cell Survival / drug effects
  • Cytokines / genetics
  • Escherichia coli
  • Gene Expression Regulation / drug effects
  • I-kappa B Proteins / metabolism*
  • Inflammation
  • Kinetics
  • Lipopolysaccharides / pharmacology*
  • Macrophages / metabolism*
  • Mice
  • NF-KappaB Inhibitor alpha
  • NF-kappa B / metabolism*
  • Nitric Oxide Synthase / genetics
  • Nitric Oxide Synthase Type II
  • Protein Transport / drug effects
  • Reverse Transcriptase Polymerase Chain Reaction


  • Cytokines
  • I-kappa B Proteins
  • Lipopolysaccharides
  • NF-kappa B
  • Nfkbia protein, mouse
  • NF-KappaB Inhibitor alpha
  • Nitric Oxide Synthase
  • Nitric Oxide Synthase Type II
  • Nos2 protein, mouse