Kaurane diterpenes from Isodon japonicus inhibit nitric oxide and prostaglandin E2 production and NF-kappaB activation in LPS-stimulated macrophage RAW264.7 cells

Planta Med. 2001 Jul;67(5):406-10. doi: 10.1055/s-2001-15808.


A methanolic extract of the whole plant of Isodon japonicus (Labiatae) showed potent inhibition on the LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production in RAW264.7 cells. Four known kaurane diterpenes were isolated by activity-guided fractionation and their structures were identified as kamebanin (1), kamebacetal A (2), kamebakaurin (3), excisanin A (4). All compounds also inhibited the LPS-induced NF-kappaB activation as assessed by NF-kappaB reporter assay and electrophoretic mobility shift assay (EMSA). Compounds 2-4 showed comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability. These results suggest that kaurane diterpenes could exert their inhibitory effects on the production of NO and PGE2 through the suppression of NF-kappaB activation, and be partially responsible for the anti-inflammatory activities of the genus Isodon.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Line
  • Dinoprostone / metabolism
  • Diterpenes / chemistry
  • Diterpenes / isolation & purification
  • Diterpenes / pharmacology*
  • Electrophoresis
  • Free Radical Scavengers / metabolism
  • Lamiaceae / chemistry*
  • Lipopolysaccharides / antagonists & inhibitors
  • Lipopolysaccharides / metabolism
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Molecular Structure
  • NF-kappa B / metabolism*
  • Nitric Oxide / metabolism*
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plants, Medicinal


  • Anti-Inflammatory Agents, Non-Steroidal
  • Diterpenes
  • Free Radical Scavengers
  • Lipopolysaccharides
  • NF-kappa B
  • Plant Extracts
  • Nitric Oxide
  • Dinoprostone