J Pharm Pharmacol. 2001 Nov; 53(11): 1533-9.

New insights into the mechanism of action of the anti-inflammatory triterpene lupeol.

FernÃ¡ndez MA, de las Heras B, GarcÃa MD, SÃ¡enz MT, Villar A.

Departamento de Farmacologia, Facultad de Farmacia, Universidad de Sevilla.

The pentacyclic triterpene lupeol has been studied for its inhibitory effects on murine models of inflammation and peritoneal macrophage functions in-vitro. Lupeol (0.5 and 1 mg/ear) administered topically suppressed the mouse ear oedema induced by 12-0-tetradecanoyl-phorbol acetate (TPA), being less effective on ear oedema induced by arachidonic acid. Quantitation of the neutrophil specific marker myeloperoxidase demonstrated that its topical activity was associated with reduction in cell infiltration into inflamed tissues. When tested in-vitro, lupeol significantly reduced prostaglandin E2 (PGE2) production from A23187-stimulated macrophages, but failed to affect leukotriene C4 release. It was a weak inhibitor of nitrite release, but dose-dependently suppressed PGE2. Cytokine production (tumour necrosis factor-alpha and interleukin-1beta) was inhibited in the range 10-100 microM in lipopolysaccharide-treated macrophages. This study demonstrated that lupeol possessed anti-inflammatory activity which was likely to depend on its ability to prevent the production of some pro-inflammatory mediators.