Synthesis, acute toxicity and anti-inflammatory effect of bornyl salicylate, a salicylic acid derivative.
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.
Universidade Federal da Paraíba, Departamento de Fisiologia e Patologia, Laboratório de Imunofarmacologia, João Pessoa, Paraíba, Brasil.
Renata Marcia Costa
RM
Vasconcelos
Fagner Carvalho
FC
Leite
Jacqueline Alves
JA
Leite
Sandra
S
Rodrigues Mascarenhas
Luis Cezar
LC
Rodrigues
Marcia Regina
MR
Piuvezam
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001920:Bradykinin / Q000494:pharmacology; D002351:Carrageenan / Q000494:pharmacology; D002465:Cell Movement / Q000187:drug effects; D016207:Cytokines / Q000378:metabolism; D015232:Dinoprostone / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004435:Eating / Q000187:drug effects; D005260:Female; D008070:Lipopolysaccharides / Q000633:toxicity; D017737:Macrophages, Peritoneal / Q000378:metabolism / Q000473:pathology; D008297:Male; D051379:Mice; D009504:Neutrophils / Q000378:metabolism / Q000473:pathology; D009569:Nitric Oxide / Q000096:biosynthesis; D010120:Oxytocics / Q000494:pharmacology; D010538:Peritonitis / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D012459:Salicylates / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014665:Vasodilator Agents / Q000494:pharmacology; D015054:Zymosan / Q000633:toxicity
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016207:Cytokines; D008070:Lipopolysaccharides; D010120:Oxytocics; D012459:Salicylates; D014665:Vasodilator Agents; D009569:Nitric Oxide; D002351:Carrageenan; D015054:Zymosan; D015232:Dinoprostone; D001920:Bradykinin