Antinociceptive properties of bergenin

J Nat Prod. 2011 Oct 28;74(10):2062-8. doi: 10.1021/np200232s. Epub 2011 Sep 22.

Abstract

Bergenin (1) is a C-glucoside of 4-O-methylgallic acid with known antiarthritic activity attributed to modulation of cytokine production. The present study was undertaken to evaluate whether 1 has antinociceptive properties in models of inflammatory pain and to investigate its possible mechanisms of action. Pretreatment with 1 (12.5-100 mg/kg, ip) produced a dose-related inhibition of acetic acid-induced writhing in mice. Furthermore, treatment with 1 (50 and 100 mg/kg) inhibited both the early and late phases in a formalin test. In addition, 1 (50 and 100 mg/kg, ip) inhibited mechanical hyperalgesia, edema, and paw production of hyperalgesic cytokines (TNF-α and IL-1β) induced by complete Freund's adjuvant. However, the local production of IL-10, an anti-inflammatory cytokine, was not altered by 1 (100 mg/kg, ip). Treatment with 1 produced a similar profile of antinociception in wild-type and IL-10-deficient mice. Mice treated with 1 did not show any motor performance alterations or apparent systemic toxicity. The results presented herein demonstrate that bergenin has consistent antinociceptive and anti-inflammatory properties, acting by the inhibition of IL-1β and TNF-α production, and suggest its potential for the control of inflammatory pain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Benzopyrans / chemistry
  • Benzopyrans / pharmacology*
  • Dose-Response Relationship, Drug
  • Edema / chemically induced
  • Edema / drug therapy
  • Gallic Acid / analogs & derivatives
  • Gallic Acid / chemistry
  • Interleukin-10 / antagonists & inhibitors
  • Interleukin-10 / biosynthesis
  • Interleukin-10 / genetics
  • Male
  • Mice
  • Pain / chemically induced
  • Pain / drug therapy*
  • Pain Measurement
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors
  • Tumor Necrosis Factor-alpha / biosynthesis

Substances

  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzopyrans
  • Tumor Necrosis Factor-alpha
  • 3,5-dihydroxy-4-methoxybenzoic acid
  • Interleukin-10
  • Gallic Acid
  • bergenin