Abstract

Objective: The species Chrysobalanus icaco L., popularly known as abajurú, abajeru, has frequently been associated with antiangiogenic, anti-inflammatory and antirheumatic effects. The 2α-3β-6β-23-tetrahydro-olean-12-en-28-oic acid (THOA) was isolated from the methanolic extract of Chrysobalanus icaco leaves. Thus, the aim of the study was to evaluate the antinociceptive and anti-inflammatory activities of THOA.Methods: Acetic acid-induced abdominal writhing, formalin, von frey and open field tests were performed in mice. The number of writhes, licking time, mechanical threshold and walked squares by animals were the evaluation parameters applied, respectively. In addition, quantification of IL-1β and TNF-α were also performed. The THOA was administered orally at doses of 1–10 mg/kg in male mice. In addition, water, vehicle, morphine (5.01 mg/kg), acetylsalicylic acid (100 mg/kg), and dexamethasone (2.25 mg/kg) were administered.Results: The THOA showed effect with 5 and 10 mg/kg in the acute pain induced by acetic acid (49% and 62% contortion inhibition), carrageenan (150% and 188% increase in mechanical threshold) and formalin (36% and 60% licking inhibition), respectively. These results indicate an inhibition of hyper nociception, while the reduction in the production of cytokines (TNF-α inhibition–64% and 88%; IL-1β inhibition–48% and 55%, respectively) confirmed the inflammatory inhibition by carrageenan. The THOA did not induce motor impairment. The THOA was not toxic after oral administration (LD50>50 mg/kg).Conclusion: These data provide initial evidence that THOA decreases the inflammatory hyper nociception probably by inhibition of IL-1β and TNF-α production, proving to be effective in reducing pain and inflammation.

Highlights

  • Inflammation is a natural defence mechanism of the body against cells or tissues injury either due to chemical, mechanical or thermal stimuli or infections [1]

  • The previous administration of L-NAME and L-arginine did not reduce the antinociceptive effect produced by the tetrahydro-olean-12-en-28-oic acid (THOA) in the 2nd phase on the formalin test

  • The present study aimed to evaluate the inflammatory hypernociception in models of acute pain and inflammation in mice subjected to oral administration of THOA

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Summary

Introduction

Inflammation is a natural defence mechanism of the body against cells or tissues injury either due to chemical, mechanical or thermal stimuli or infections [1]. Inflammatory hyperalgesia results from the sensitization of primary afferent neurons which is better described as hyper nociception in animal models. It is induced by inflammatory mediators, such as prostaglandins and sympathetic amines, which directly sensitize peripheral nociceptive neurons [4]. The release of these directacting hyper nociceptive mediators is generally preceded by a cascade of cytokines [5]. New approaches are considered for the development of new anti-inflammatory agents, with less adverse effects than the current ones [7]

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