RESUMO
This study describes the antinociceptive activity of extracts (methanolic (ME) and acetonic (AE)) and two phenolic compounds, 3,4,3'-trimethoxyflavellagic acid (1) and 3,4,3'-trimethoxy flavellagic acid 4'-O-glucoside (2), from Plinia glomerata leaves, against different experimental models of pain in mice. When evaluated against writhing test, by i.p. route, ME and AE presented calculated ID(50) values (and respective confidence interval) of 3.28 (1.63-6.61) and 24.79 (16.57-37.09) mg/kg, respectively. Given by the oral route at 500 mg/kg, AE and ME extracts inhibited the abdominal constrictions by 60.5% and 35.3%, respectively. In the formalin test (10 mg/kg, i.p.), AE inhibited both phases of pain (45.6% in the first phase; 99.8% in the second phase) whereas ME inhibited 47.8% the first phase, and 92.6% the second phase. In the capsaicin test both extracts showed activity, with calculated ID(50) values of 6.56 (5.69-7.56) and 7.68 (4.94-11.93) mg/kg for AE and ME, respectively. When evaluated against the hot-plate test, both extracts demonstrated activity, but only in high doses. Compound 2, when evaluated against the formalin test (10 mg/kg, i.p.), inhibited both phases of pain (77.6%, first phase; 62%, second phase) whereas 1 inhibited only the first phase, with inhibition of 70%. When tested in the capsaicin and glutamate tests, at 10 mg/kg, i.p., 1 and 2 caused inhibitions of 41.5% and 37.9%, and 37.7% and 54.5%, respectively. These results confirm previous studies carried out by our research group regarding the antinociceptive properties of P. glomerata, stimulating other studies on mechanism of action as well as the determination of additional active principles in this plant.
Assuntos
Analgésicos/farmacologia , Ácido Elágico/análogos & derivados , Myrtaceae/química , Fenóis/farmacologia , Ácido Acético , Acetona , Analgésicos/isolamento & purificação , Analgésicos Opioides/farmacologia , Animais , Capsaicina , Ácido Elágico/isolamento & purificação , Ácido Elágico/farmacologia , Formaldeído , Ácido Glutâmico , Temperatura Alta , Injeções Intraperitoneais , Masculino , Metanol , Camundongos , Morfina/farmacologia , Medição da Dor/efeitos dos fármacos , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , SolventesRESUMO
The present work describes the antinociceptive properties and chemical composition of the aerial parts of Plinia glomerata (Myrtaceae). Both of the extracts evaluated, acetonic and methanolic, showed potent antinociceptive action, when analyzed against acetic acid-induced abdominal constrictions in mice, with calculated ID50 (mg/kg, i. p.) values of 24.8 and 3.3, respectively. Through usual chromatographic techniques with an acetonic extract, the following compounds were obtained: 3,4,3'-trimethoxy flavellagic acid (1), 3,4,3'-trimethoxy flavellagic acid 4'-O-glucoside (3) and quercitrin (4), which were identified based on spectroscopic data. Compounds 1 (ID50 = 3.9 mg/kg, i. p., or 10.8 micromol/kg) and 3 (ID50 = 1.3 mg/kg or 2.5 micromol/kg) were notably more active than some well-known analgesic drugs used here for comparison.
Assuntos
Analgésicos/farmacologia , Myrtaceae/química , Fenóis/farmacologia , Componentes Aéreos da Planta/química , Acetaminofen/farmacologia , Analgésicos/química , Analgésicos/isolamento & purificação , Animais , Aspirina/farmacologia , Brasil , Diclofenaco/farmacologia , Dipirona/farmacologia , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Modelos Moleculares , Fenóis/química , Fenóis/isolamento & purificaçãoRESUMO
Applanoxidic acids and sterols, isolated from Ganoderma spp., were acetylated and/or methylated. The antibacterial activity against Escherichia coli and Staphylococcus aureus and the antifungal activity against Candida albicans and Trichophyton mentagrophytes of the derivatives were investigated by a microdilution method, and compared with those of the natural products. Both natural and modified compounds exhibited comparable antibacterial and antifungal activities in a range of 1.0 to > 2.0 mg/ml minimal inhibitory concentration.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Ganoderma/química , Esteróis/isolamento & purificação , Triterpenos/farmacologia , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Arthrodermataceae/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Ganoderma/isolamento & purificação , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos , Esteróis/farmacologia , Trichophyton/efeitos dos fármacos , Triterpenos/isolamento & purificaçãoRESUMO
From the resinous exudate of leaves of Haplopappus multifolius two new coumarins were isolated and assigned the structures 6-hydroxy-7-(5'-hydroxy-3',7'-dimethylocta-2',6'-dien)-oxycoumarin (1) and 6-hydroxy-7-(7'-hydroxy-3',7'-dimethylocta-2',5'-dien)-oxy coumarin (2).
Assuntos
Cumarínicos/química , Haplopappus , Fitoterapia , Extratos Vegetais/química , Humanos , Espectroscopia de Ressonância Magnética , Folhas de PlantaRESUMO
A chemical study of aerial parts of Haplopappus illinitus afforded five labdane diterpenoids whose structures were elucidated by high field NMR spectroscopy and 2D techniques. Four of them are dicarboxylic acids previously reported as the corresponding dimethyl ester derivatives and the fifth is a new compound.