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Antinociceptive properties of bergenin.

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.
AuthorsCristiane Metzker de Oliveira, Fabiana Regina Nonato, Flávia Oliveira de Lima, Ricardo David Couto, Juceni P David, Jorge M David, Milena Botelho Pereira Soares, Cristiane Flora Villarreal
JournalJournal of natural products (J Nat Prod) Vol. 74 Issue 10 Pg. 2062-8 (Oct 28 2011) ISSN: 1520-6025 [Electronic] United States
PMID21939182 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzopyrans
  • Tumor Necrosis Factor-alpha
  • 3,5-dihydroxy-4-methoxybenzoic acid
  • Interleukin-10
  • Gallic Acid
  • bergenin
Topics
  • Analgesics (chemistry, pharmacology)
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (chemistry, pharmacology)
  • Benzopyrans (chemistry, pharmacology)
  • Dose-Response Relationship, Drug
  • Edema (chemically induced, drug therapy)
  • Gallic Acid (analogs & derivatives, chemistry)
  • Interleukin-10 (antagonists & inhibitors, biosynthesis, genetics)
  • Male
  • Mice
  • Pain (chemically induced, drug therapy)
  • Pain Measurement
  • Tumor Necrosis Factor-alpha (antagonists & inhibitors, biosynthesis)

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