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.

Antinociceptive properties of 25‐methoxy hispidol A, a triterpinoid isolated from Poncirus trifoliata (Rutaceae) through inhibition of NF‐κB signalling in mice

“…Following, the first phase or early phase, there is the beginning of the late or secondary phase, which results from local inflammation and release of inflammatory mediators. This phase is referred to as the inflammatory phase and lasts between 20 and 30 min (de Oliveira et al, ). Thirty animals were randomly divided into five groups such as negative control (only formalin treated), positive control (piroxicam 5 mg/kg, i.p), and treatment control administering 25‐MHA at the doses of 1, 5, and 10 mg/kg, and each group treated was assigned six animals.…”

“…The antinociceptive potential of 25‐MHA (10 mg/kg, i.p) was also investigated against the acetic acid‐induced visceral pain, known as the writhing test. The acetic acid following administration into the peritoneum of the mice produces writhing movement characterised by abdominal contraction with hind paw extension (de Oliveira et al, ). Eighteen mice were randomly divided into three groups ( n = 6 per group) such as negative control (administered with acetic acid only), positive control (piroxicam 5 mg/kg, i.p), and treatment control that received 25‐MHA (10 mg/kg, i.p).…”

“…The tissue samples from all the treated groups such as normal control (normal saline 2% DMSO), negative control (CFA treated, i.pl), positive control (dexamethasone 5 mg/kg, i.p), and 25‐MHA (10 mg/kg, i.p) groups for IL‐1β and TNF‐α determination were prepared according to the method described by (de Lima et al, ; de Oliveira et al, ; Khan et al, ). At Day 6 of the CFA administration (i.pl), the skin tissue from the paw was removed, and the tissue proteins were extracted from 100 mg tissue/ml PBS to which 0.4‐M NaCl, 0.05% Tween 20, and protease inhibitors were added.…”

Pyrano-isochromanones as IL-6 Inhibitors: Synthesis, in Vitro and in Vivo Antiarthritic Activity

“…2 Our finding of bergenin and its derivatives as potent IL-6 inhibitors is in agreement with the recent report on antinociception activity of bergenin. 25 Because RA is a chronic inflammatory disease and the joint pain is one of the key pathological symptoms, the antinociceptive agents will have additional beneficial effects in disease management. On the basis of this, we decided to investigate antiarthritic effect of bergenin and potent derivatives 4e and 4f in animal models.…”

Structure-activity Relationships for Bergenin Analogues as ^|^beta;-Secretase (BACE1) Inhibitors

“…It exhibits various biological activities, such as antioxidant 27,28 , anti-inflammatory 29 , anti-arthritis 30 , hypolipidemic 31 , anti-HIV 32 , antiarrhythmic 33 , hepatoprotective 34 , and antinociceptive effects 35 . Bergenin contains 5 hydroxyl groups, which are considered to be potentially active.…”