TargetRx Atlas

MRNA basic information

  • mRNA ID:ENST00000226574
  • Gene Name:NFKB
  • mRNA database:Ensembl
  • mRNA expression :down-regulated
  • mRNA Method:RT-PCR
  • mRNA Pathway:NFKB signaling pathway
  • Evidence:validated
  • (mRNA-drug)

Drug basic information

  • Drug ID:NA
  • Drug Name:DA-6034
  • Drug Method:down-regulated the gene expression

Disease basic infommation

  • Disease:inflammatory bowel disease
  • Tissue:patients tissues

Other information

  • Title:The effects of DA-6034 on NF-kappaB activity induced by lipopolysaccharide or tumor necrosis factor alpha in a human colonic epithelial cell line.
  • Journal:Hepatogastroenterology
  • Published:2008
  • PubMed ID:19260477
  • Abstract:Background/aims:DA-6034, a synthetic derivative of eupatilin, has shown a potent anti-inflammatory effect in experimental rat models with inflammatory bowel disease (IBD). Nuclear factor kappaB (NF-kappaB) is known to play a central role in regulating inflammatory responses in patients with IBD, and is an important target for therapeutic intervention. We, therefore, examined the effects of DA-6034 on NF-kappaB activity and proinflammatory cytokines production in the human colonic cell line. Methodology:HT-29 cells were stimulated with either lipopolysaccharide (LPS) or tumor necrosis factor alpha (TNF-alpha). After pretreatment with different doses of DA-6034, the influence of DA-6034 on NF-kappaB activity was determined by an electrophoretic mobility shift assay (EMSA). The effect of DA-6034 on inhibitory protein kappaBalpha (IkappaBalpha) activity was determined by immunoblotting. TNF-alpha and interlukin 8 (IL-8) messenger RNA expression, which are regulated by NF-kappaB, were assayed by RT-PCR. The production of TNF-alpha or IL-8 proteins was measured by ELISA. Results:DA-6034 inhibited NF-kappaB activity and prevented IkappaBalpha degradation in HT-29 cells after stimulation with either LPS or TNF-alpha. Furthermore, the production of TNF-alpha or IL-8 proteins decreased significantly after DA-6034 pretreatment. Conclusions:These observations suggest that DA-6034 produces an anti-inflammaotory effect through inhibition of NF-kappaB activity by the prevention of I B degradation.
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