Downregulation of microglial activation by achillolide A

Planta Med. 2015 Feb;81(3):215-21. doi: 10.1055/s-0034-1396204. Epub 2015 Feb 5.


Chronic inflammation has been implicated in the pathogenesis of various neurodegenerative diseases. During the neuroinflammatory process, microglial cells release neurotoxic and proinflammatory mediators. In the present study, using activity-guided fractionation, we have purified an anti-inflammatory compound determined by spectroscopic methods to be a sesquiterpene lactone named achillolide A from Achillea fragrantissima (Forsk.) Sch. Bip. In primary cultures of lipopolysaccharide-activated microglial cells, achillolide A inhibited the lipopolysaccharide-induced levels of proinflammatory and toxic mediators including glutamate, nitric oxide, matrix metalloproteinase-9, cyclooxygenase-2, induced nitric oxide synthase, interleukin-1β, and tumor necrosis factor-α. Achillolide A also exhibited an antioxidant capacity, as was shown in a cell free system as well as by its ability to reduce intracellular reactive oxygen species levels in microglial cells. Thus, achillolide A might have therapeutic potential for treatment of neurodegenerative diseases and deserves further studies.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Achillea / chemistry*
  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / therapeutic use
  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use
  • Down-Regulation
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Inflammation Mediators / metabolism*
  • Lactones / pharmacology*
  • Lactones / therapeutic use
  • Microglia / drug effects*
  • Microglia / metabolism
  • Neurodegenerative Diseases / drug therapy
  • Neurodegenerative Diseases / metabolism
  • Phytotherapy
  • Plant Extracts / pharmacology*
  • Plant Extracts / therapeutic use
  • Rats
  • Reactive Oxygen Species / metabolism
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use


  • Anti-Inflammatory Agents
  • Antioxidants
  • Inflammation Mediators
  • Lactones
  • Plant Extracts
  • Reactive Oxygen Species
  • Sesquiterpenes