Synthesis, acute toxicity and anti-inflammatory effect of bornyl salicylate, a salicylic acid derivative

Abstract

Bornyl salicylate (BS) is a salicylic derivative, obtained by sterification of salicylic acid and monoterpene (-)-borneol, and its topical use in inflammatory diseases was described in the early 20th century. It is also known that borneol presents neuroprotective, genoprotective and analgesic properties. The purpose of this study was to evaluate BS in experimental models of acute inflammation. The toxicity of BS was analyzed by measuring water and food intake, weight, mortality and weight of main organs. To assess its anti-inflammatory effect, BS-treated mice were challenged with carrageenan, prostaglandin E2 (PGE2), bradikynin (BK) or histamine (HIS)-induced paw edema, zymosan-induced peritonitis and vascular permeability induced by acetic acid. Nitric oxide (NO) production was analyzed in peritoneal macrophage cultures. There was no sign of acute toxicity of BS in male and female mice. Furthermore, treatment with BS was significantly (p < 0.05) effective in reducing paw edema induced by carrageenan in early and late phases; this effect was related to PGE2 and BK, but HIS independent. Neutrophil migration and cytokine release (TNF-α, IL-1β and IL-6) induced by zymosan and fluid leakage induced by acetic acid were also reduced in BS-treated animals. In vitro, BS (10 µg/mL) reduced NO production in LPS-stimulated macrophages. These data suggest that BS has an anti-inflammatory effect, which is related, at least in part, with decrease of mediators as PGE2, NO and pro-inflammatory cytokines. However, further studies should be done to explore its potential as an anti-inflammatory drug.

Keywords::

• Bornyl salicylate
• acute inflammation
• cytokines
• vascular permeability
• nitric oxide

Acknowledgments

The authors are indebted to Hermann Ferreira Costa, Gláucia Faheina, Adriano Alves, Anne Abreu, Laércia Paiva, Victor Brito, Priscila Jacob and José Crispim Duarte for the valuable technical assistance.

Declaration of interest

This work had financial support of Programa de Apoio a Núcleos de Excelência do Conselho Nacional de Desenvolvimento Científico e Tecnológico (PRONEX/CNPq MCT/Brasil) and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES/Brasil). The authors report no declarations of interest.