title: 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.
authors.affiliation: Universidade Federal da Bahia, and Centro de Biotecnologia e Terapia Celular, Hospital São Rafael, Salvador, BA, Brazil.
authors.forename: Cristiane Metzker
authors.initials: CM
authors.lastname: de Oliveira
authors.forename: Fabiana Regina
authors.initials: FR
authors.lastname: Nonato
authors.forename: Flávia Oliveira
authors.initials: FO
authors.lastname: de Lima
authors.forename: Ricardo David
authors.initials: RD
authors.lastname: Couto
authors.forename: Juceni P
authors.initials: JP
authors.lastname: David
authors.forename: Jorge M
authors.initials: JM
authors.lastname: David
authors.forename: Milena Botelho Pereira
authors.initials: MB
authors.lastname: Soares
authors.forename: Cristiane Flora
authors.initials: CF
authors.lastname: Villarreal
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D001578:Benzopyrans / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005707:Gallic Acid / Q000031:analogs & derivatives / Q000737:chemistry; D016753:Interleukin-10 / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000235:genetics; D008297:Male; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010147:Pain Measurement; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D014409:Tumor Necrosis Factor-alpha; C024272:3,5-dihydroxy-4-methoxybenzoic acid; D016753:Interleukin-10; D005707:Gallic Acid; C006741:bergenin