RESUMO
Esenbeckia febrifuga (Rutaceae) is a plant traditionally used to treat malaria in the Brazilian Amazon region. Ethanol extract of stems displayed a good antiplasmodial activity against Plasmodium falciparum strains W-2 (IC(50) 15.5+/-0.71 microg/ml) and 3 D7 (IC(50) 21.0+/-1.4 microg/ml). Two coumarins (bergaptene 1 and isopimpinellin 2), five alkaloids (flindersiamine 3, kokusaginine 4, skimmiamine 5, gamma-fagarine 6 and 1-hydroxy-3-methoxy-N-methylacridone, 7), besides a limonoid (rutaevine 8), have been isolated for the first time from this species. Antiplasmodial activity of compounds 3, 5-8 has been evaluated in vitro against P. falciparum strains (W-2 and 3D7) and the furoquinolines 5 and 6 were the most potent displaying IC(50) values <50 microg/ml; flindersiamine (3) showed a weak activity while alkaloid 7 and rutaevine (8) were inactive (IC(50)>100 microg/ml).
Assuntos
Malária Falciparum/tratamento farmacológico , Fitoterapia , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Rutaceae/química , Animais , Antimaláricos/química , Antimaláricos/farmacologia , Brasil , Cloroquina/farmacologia , Resistência a Medicamentos , Eritrócitos/parasitologia , Etanol/química , Medicina Tradicional , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Caules de PlantaRESUMO
Esenbeckia febrifuga (Rutaceae) is a plant traditionally used to treat malaria in the Brazilian Amazon region. Ethanol extract of stems displayed a good antiplasmodial activity against Plasmodium falciparum strains W-2 (IC(50) 15.5+/-0.71mug/ml) and 3 D7 (IC(50) 21.0+/-1.4mug/ml). Two coumarins (bergaptene 1 and isopimpinellin 2), five alkaloids (flindersiamine 3, kokusaginine 4, skimmiamine 5, gamma-fagarine 6 and 1-hydroxy-3-methoxy-N-methylacridone, 7), besides a limonoid (rutaevine 8), have been isolated for the first time from this species. Antiplasmodial activity of compounds 3, 5-8 has been evaluated in vitro against P. falciparum strains (W-2 and 3D7) and the furoquinolines 5 and 6 were the most potent displaying IC(50) values <50mug/ml; flindersiamine (3) showed a weak activity while alkaloid 7 and rutaevine (8) were inactive (IC(50)>100mug/ml)...(AU)