Anti-inflammatory effects of a bioavailable compound, Artepillin C, in Brazilian propolis

Eur J Pharmacol. 2008 Jun 10;587(1-3):296-301. doi: 10.1016/j.ejphar.2008.02.067. Epub 2008 Feb 29.


Artepillin C is the major compound in the Brazilian green propolis from Baccharis dracunculifolia. Our aim in this study was to investigate the anti-inflammatory effects, absorption, and bioavailability of Artepillin C in mice. The animals used were male Swiss mice subjected to: paw oedema by carrageenan (300 microg/paw), carrageenan-induced peritonitis, and prostaglandin E(2) determination. We also measured in vitro nitric oxide production by RAW 264.7 cells and NF-kappaB activity in HEK 293 cells. Finally, we measured the absorption and bioavailability of Artepillin C in plasma from mice by means of GC-MS after a single oral dose (10 mg/kg). In vivo, Artepillin C produced a maximal inhibition of 38% after 360 min on paw oedema. Artepillin C also decreased the number of neutrophils during peritonitis (IC(50): 0.9 (0.5-1.4) mg/kg). Treatment with Artepillin C decreased prostaglandin E(2) by 29+/-3% and 58+/-5% at 1 and 10 mg/kg, respectively, with a mean ID(50) of 8.5 (8.0-8.7) mg/kg). Similarly, in in vitro models, Artepillin C (3, 10, or 100 microM) decreased nitric oxide production by RAW 264.7 cells with a mean IC(50) of 8.5 (7.8-9.2) microM. In HEK 293 cells, Artepillin C reduced NF-kappaB activity with a mean IC(50) of 26 (22-30) mug/ml), suggesting anti-inflammatory activity, particularly during acute inflammation. Lastly, Artepillin C was absorbed after an oral dose (10 mg/kg) with maximal peaks found at 1 h (22 microg/ml). Collectively, Artepillin C showed anti-inflammatory effects mediated, at least in part, by prostaglandin E(2) and nitric oxide inhibition through NF-kappaB modulation, and exhibited bioavailability by oral administration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents*
  • Biological Availability
  • Carrageenan
  • Cell Survival / drug effects
  • Cells, Cultured
  • Dinoprostone / metabolism
  • Edema / chemically induced
  • Edema / prevention & control
  • Indicators and Reagents
  • Indomethacin / pharmacology
  • Intestinal Absorption
  • Leupeptins / pharmacology
  • Male
  • Mice
  • NF-kappa B / metabolism
  • Nitric Oxide / metabolism
  • Nitrites / metabolism
  • Phenylpropionates / chemistry
  • Phenylpropionates / pharmacokinetics
  • Phenylpropionates / pharmacology*
  • Propolis / chemistry*
  • Transcriptional Activation


  • Anti-Inflammatory Agents
  • Indicators and Reagents
  • Leupeptins
  • NF-kappa B
  • Nitrites
  • Phenylpropionates
  • Nitric Oxide
  • artepillin C
  • Carrageenan
  • Propolis
  • Dinoprostone
  • benzyloxycarbonylleucyl-leucyl-leucine aldehyde
  • Indomethacin