Inhibition by tectorigenin and tectoridin of prostaglandin E2 production and cyclooxygenase-2 induction in rat peritoneal macrophages

Biochim Biophys Acta. 1999 Jun 10;1438(3):399-407. doi: 10.1016/s1388-1981(99)00067-0.

Abstract

Tectorigenin and tectoridin, isolated from the rhizomes of Korean Belamcanda chinensis (Iridaceae) which are used as Chinese traditional medicine for the treatment of inflammation, suppressed prostaglandin E2 production by rat peritoneal macrophages stimulated by the protein kinase C activator, 12-O-tetradecanoylphorbol 13-acetate (TPA), or the endomembrane Ca2+-ATPase inhibitor, thapsigargin. Tectorigenin inhibited prostaglandin E2 production more potently than tectoridin. Neither compound inhibited the release of radioactivity from [3H]arachidonic acid-labeled macrophages stimulated by TPA or thapsigargin. In addition, activities of isolated cyclooxygenase (COX)-1 and COX-2 were not inhibited by the two compounds. Western blot analysis revealed that the induction of COX-2 by TPA or thapsigargin was inhibited by the two compounds in parallel with the inhibition of prostaglandin E2 production. These findings suggest that one of the mechanisms of the anti-inflammatory activities of the rhizomes of Belamcanda chinensis is the inhibition of prostaglandin E2 production by tectorigenin and tectoridin due to the inhibition of the induction of COX-2 in the inflammatory cells.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Arachidonic Acid / metabolism
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Dinoprostone / metabolism*
  • Drugs, Chinese Herbal / pharmacology*
  • Enzyme Induction / drug effects
  • Isoenzymes / analysis
  • Isoenzymes / biosynthesis*
  • Isoenzymes / metabolism
  • Isoflavones / pharmacology*
  • Macrophages, Peritoneal / drug effects*
  • Macrophages, Peritoneal / metabolism
  • Male
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / analysis
  • Prostaglandin-Endoperoxide Synthases / biosynthesis*
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Tetradecanoylphorbol Acetate / antagonists & inhibitors
  • Thapsigargin / antagonists & inhibitors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drugs, Chinese Herbal
  • Isoenzymes
  • Isoflavones
  • Membrane Proteins
  • Arachidonic Acid
  • Thapsigargin
  • tectorigenin
  • tectoridin
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, rat
  • Dinoprostone
  • Tetradecanoylphorbol Acetate