Inhibition by berberine of cyclooxygenase-2 transcriptional activity in human colon cancer cells

J Ethnopharmacol. 1999 Aug;66(2):227-33. doi: 10.1016/s0378-8741(98)00162-7.

Abstract

The enzyme cyclooxygenase-2 (COX-2) is abundantly expressed in colon cancer cells and plays a key role in colon tumorigenesis. Compounds inhibiting COX-2 transcriptional activity have therefore potentially a chemopreventive property against colon tumor formation. An assay method for estimating COX-2 transcriptional activity in human colon cancer cells was established using a beta-galactosidase reporter gene system, and examination was made of various medicinal herbs and their ingredients for an inhibitory effect on COX-2 transcriptional activity. We found that berberine, an isoquinoline alkaloid present in plants of the genera Berberis and Coptis, effectively inhibits COX-2 transcriptional activity in colon cancer cells in a dose- and time-dependent manner at concentrations higher than 0.3 microM. The present findings may further explain the mechanism of anti-inflammatory and anti-tumor promoting effects of berberine.

MeSH terms

  • Berberine / pharmacology*
  • Cell Division / drug effects
  • Colonic Neoplasms / enzymology*
  • Colonic Neoplasms / genetics
  • Cycloheximide / pharmacology
  • Cyclooxygenase 2
  • Genes, Reporter / drug effects
  • Humans
  • Isoenzymes / biosynthesis*
  • Isoenzymes / genetics
  • Membrane Proteins
  • Plasmids
  • Prostaglandin-Endoperoxide Synthases / biosynthesis*
  • Prostaglandin-Endoperoxide Synthases / genetics
  • Protein Synthesis Inhibitors / pharmacology
  • Transcription, Genetic / drug effects*
  • Transfection
  • Tumor Cells, Cultured

Substances

  • Isoenzymes
  • Membrane Proteins
  • Protein Synthesis Inhibitors
  • Berberine
  • Cycloheximide
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases