Shikimic acid inhibits LPS-induced cellular pro-inflammatory cytokines and attenuates mechanical hyperalgesia in mice

Int Immunopharmacol. 2016 Oct:39:97-105. doi: 10.1016/j.intimp.2016.07.016. Epub 2016 Jul 25.

Abstract

Background and aims: Shikimic acid (SA) is present in a wide variety of plants and microorganisms used in traditional and folk medicine and also is an essential starting material for the synthesis of the antiviral drug Oseltamivir (Tamiflu®). Some pharmacological actions observed in SA-enriched products include antioxidant and anti-inflammatory activities. Here, we investigated the anti-inflammatory and antinociceptive actions of isolated SA.

Methods: RAW 264.7 macrophage cells were treated with bacterial LPS (1μg/mL) and the effect of SA on the modulation of cell viability, nitric oxide (NO) production, TNF-α, and IL-1β content and MAPK (ERK1/2 and p38) activation was evaluated. Besides, the anti-hyperalgesic actions of SA on in vivo model of mechanical hyperalgesia induced by carrageenan (CG), dopamine (DA), TNF-α and prostaglandin (PGE2) were assessed.

Results: In RAW 264.7 cells, SA suppressed LPS-induced decrease in cell viability and nitrite accumulation to control values and inhibited up-regulation of TNF-α (65%) and IL-1β (39%). These effects may be mediated at least in part by inhibition of LPS-induced ERK 1/2 (22%) and p38 (17%) phosphorylation. In mice, SA at 50, 100, and 200mg/kg decreased formalin-induced nociceptive behavior (around 50%) and inhibited the inflammatory nociception induced by TNF-α and PGE2 (50 to 75% each). Moreover, SA (100 and 200mg/kg) significantly attenuated the mechanical hyperalgesia induced by CG and DA (25 to 40% each).

Conclusions: These results indicate that SA presents anti-inflammatory actions with potential for development of drugs to treat pro-inflammatory and painful conditions.

Keywords: Cytokines; Inflammation; Mechanical hyperalgesia; Nociception; Raw 264.7; Shikimic acid.

MeSH terms

  • Analgesics / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents / therapeutic use*
  • Antiviral Agents / therapeutic use
  • Cytokines / metabolism
  • Hyperalgesia / drug therapy*
  • Immunity, Cellular / drug effects
  • Inflammation Mediators / metabolism
  • Lipopolysaccharides / immunology
  • Macrophages / drug effects*
  • Macrophages / immunology
  • Male
  • Mice
  • Oseltamivir / therapeutic use
  • RAW 264.7 Cells
  • Shikimic Acid / therapeutic use*
  • Signal Transduction / drug effects
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • Analgesics
  • Anti-Inflammatory Agents
  • Antiviral Agents
  • Cytokines
  • Inflammation Mediators
  • Lipopolysaccharides
  • Oseltamivir
  • Shikimic Acid
  • p38 Mitogen-Activated Protein Kinases