RESUMO
The anti-inflammatory activity of the petroleum ether, dichloromethane and methanol extracts from Heterotheca subaxillaris var. latifolia were assayed using 12-O-tetradecanoyl phorbol acetate (TPA) induced ear edema test in mice and carrageenan-induced paw edema test in rats. The dichloromethane extract showed a significant anti-inflammatory activity (91 percent of inhibition) in TPA-induced ear edema test (topical administration at 1 mg/ear). No effects were seen on carragenan-induced edema. Bio-guided fractionation deal to the isolation of the major flavonoids santin, pectolinaringenin, 3,6-dimethoxy-5,7,4'-trihydroxyflavone and hispidulin present in the active fractions.
A atividade antiinflamatória de extratos éter petróleo, diclorometânico e metanólico de Heterotheca subaxillaris var. latifolia, foi testada pelo método de edema induzido pelo 12-O-tetradecanoil phorbol acetato (TPA) na orelha do camundongos e pelo método do edema de pata induzido por carragenina em ratos. O extrato diclorometânico mostrou atividade antiinflamatória significativa (91 por cento inibição) no edema de orelha induzido por TPA (administração tópica de 1 mg/orelha). Não houve efeitos significativos no teste do edema induzido pela carragenina. O fracionamento bioguiado das frações ativas levou ao isolamento dos flavonoides majoritários santina, pectolinaringenina, 3,6-dimetoxi-5, 7,4 '-trihidroxiflavona e hispidulina.
RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia. THE AIM OF THE STUDY: We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators. MATERIAL AND METHODS: The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis. RESULTS: The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5mg/ear) inhibited the oedema by 66% (4.2+/-0.6 mg vs. 12.3+/-1.4 mg, P<0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5mg/ear x 7 applications (7.5+/-0.6 mg vs. 11.9+/-1.3mg, P<0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 microg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 microg/mL, the flavonoid-enriched fraction had no effect on TNF-alpha production. In addition, at 22.30 microg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively. CONCLUSION: These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.
Assuntos
Anti-Inflamatórios/farmacologia , Cucurbitaceae/química , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Brasil , Linhagem Celular , Colômbia , Ciclo-Oxigenase 2/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Modelos Animais de Doenças , Feminino , Flavonoides/isolamento & purificação , Inflamação/tratamento farmacológico , Inflamação/fisiopatologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Medicina Tradicional , Camundongos , Óxido Nítrico Sintase Tipo II/efeitos dos fármacos , Óxido Nítrico Sintase Tipo II/metabolismo , Peru , Extratos Vegetais/química , Raízes de PlantasRESUMO
Dichloromethane, methanol and aqueous extracts of the aerial parts of Terminalia australis were evaluated for their antifungal activity. The methanol and aqueous extracts were found to be effective against the tested Aspergillus and Candida strains.