Neolignans from Piper kadsura and their anti-neuroinflammatory activity

Bioorg Med Chem Lett. 2010 Jan 1;20(1):409-12. doi: 10.1016/j.bmcl.2009.10.016. Epub 2009 Oct 8.

Abstract

Bioassay-guided column chromatographic separation of the methanolic extract of dried aerial parts of Piper kadsura (Piperaceae) led to the isolation of a new neolignan, piperkadsin C (1), together with eight known neolignans (2-9). The structures of the isolated compounds were elucidated by combined spectroscopic methods. The anti-neuroinflammatory activities of these compounds were evaluated by assessing nitric oxide (NO) production in LPS-activated BV-2 cells, a microglia cell line. Piperkadsin C (1) and futoquinol (2) potently inhibited NO production with an IC(50) value of 14.6 and 16.8microM in microglia cells, respectively. Compounds 3, 4, 5, 8, and 9 also exhibited moderate inhibition of NO production in BV-2 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Humans
  • Lignans / chemistry*
  • Lignans / isolation & purification
  • Lignans / pharmacology
  • Lipopolysaccharides / pharmacology
  • Magnetic Resonance Spectroscopy
  • Neurons / drug effects*
  • Nitric Oxide / metabolism
  • Piper / chemistry*
  • Plant Extracts / chemistry

Substances

  • Anti-Inflammatory Agents
  • Lignans
  • Lipopolysaccharides
  • Plant Extracts
  • futoquinol
  • piperkadsin C
  • Nitric Oxide