Inhibitory effects of scutellarein on proliferation of human lung cancer A549 cells through ERK and NFκB mediated by the EGFR pathway

Chin J Physiol. 2014 Aug 31;57(4):182-7. doi: 10.4077/CJP.2014.BAC200.

Abstract

High expression levels of cyclooxygenase-2 (COX-2) contribute a strong proliferative ability to human lung cancer cells, and this function is link to the epidermal growth factor receptor (EGFR) pathway, which was mediated by extracellular-signal-regulated kinase (ERK) and nuclear factor kappa B (NFκB). In this study, scutellarein, a flavonoid compound, was screened for proliferation inhibition at different concentrations (0, 5, 25 and 50 μM) at 24 h or 48 h in human lung cancer cell line A549. Results showed that A549 cell proliferation was inhibited by 50 μM scutellarein treatment in 24 h and 48 h of treatment. The expression levels of phosphorylated EGFR, phosphorylated ERK, phosphorylated NFκB and COX-2 were reduced in a dose-dependent manner after 24 h scutellarein treatments at different concentrations. Further, ERK inhibitor U0126 and NFκB inhibitor MG132 also inhibited A549 cell proliferation similar to 50 κM scutellarein treatment from 24 h to 48 h. The experimental results showed that scutellarein could inhibit proliferation of the human lung cancer cell line A549 through ERK and NFκB mediated by the EGFR pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apigenin / chemistry
  • Apigenin / pharmacology*
  • Butadienes / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Enzyme Inhibitors / pharmacology
  • ErbB Receptors / metabolism*
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Humans
  • Leupeptins / pharmacology
  • Lung Neoplasms / metabolism
  • Lung Neoplasms / pathology*
  • MAP Kinase Signaling System / drug effects*
  • MAP Kinase Signaling System / physiology
  • NF-kappa B / metabolism
  • Nitriles / pharmacology

Substances

  • Antineoplastic Agents
  • Butadienes
  • Enzyme Inhibitors
  • Leupeptins
  • NF-kappa B
  • Nitriles
  • U 0126
  • Apigenin
  • Egfr protein, rat
  • ErbB Receptors
  • Extracellular Signal-Regulated MAP Kinases
  • scutellarein
  • benzyloxycarbonylleucyl-leucyl-leucine aldehyde