RESUMEN
BACKGROUND: Aqueous extracts of Tridax procumbens (TP) (Compositae) and Phyllanthus amarus (PA) (Euphorbiaceae) are used in traditional medicine in Ghana to treat malaria. Previous studies have demonstrated the anti-trypanosoma, anti-bacterial and anti-HIV effects of TP and PA. OBJECTIVE: To assess the antiplasmodial activity of extracts of TP and PA. METHOD: Aqueous extracts of TP and PA were prepared. A portion of each was freeze-dried and the remaining extracted sequentially with ethyl acetate and chloroform. Ethanolic extracts were also prepared. The antiplasmodial activity of the extracts was assessed with the 3H-hypoxanthine assay using chloroquine-resistant (Dd2) Plasmodium falciparum parasites. Chloroquine was used as the reference drug. The modified tetrazolium-based colorimetric assay was also used to evaluate the red blood cell (RBC)-protective/antiplasmodial activities and cytotoxicities of the extracts. RESULTS: Results showed that TP and PA have antiplasmodial activities. The aqueous and ethanolic extracts of PA were the most active, yielding EC50 values of 34.9 µg/ml and 31.2 µg/ml, respectively in the tetrazolium-based assay. The TP and PA produced and IC50 values of 24.8 µg/ml and 11.7 µg/ml, respectively in the hypoxanthine assay. Protection of human RBCs against P. falciparum damage by the extracts highly correlated with their antiplasmodial activities. None of the extracts, within the concentration range (1.9-500 µg/ml) studied produced any overt toxicity to human RBCs. CONCLUSION: The results indicate that both PA and TP have activities against chloroquine-resistant P. falciparum (Dd2) parasites. The antiplasmodial principles extracted into water and ethanol but not chloroform or ethyl acetate.
Asunto(s)
Antimaláricos/farmacología , Asteraceae , Phyllanthus , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Cloroquina/farmacología , Colorimetría , Resistencia a Medicamentos , Eritrocitos/efectos de los fármacos , Eritrocitos/parasitología , Humanos , Componentes Aéreos de las PlantasAsunto(s)
Plasmodium falciparum/efectos de los fármacos , Pirimetamina/farmacología , Tetrahidrofolato Deshidrogenasa/genética , Triazinas/farmacología , Animales , Secuencia de Bases , Resistencia a Medicamentos , Datos de Secuencia Molecular , Mutación , Plasmodium falciparum/enzimología , Plasmodium falciparum/genética , Reacción en Cadena de la Polimerasa , ProguanilRESUMEN
An acid peptidase that degrades hemoglobin optimally at pH 3.5, a neutral aminopeptidase and an alkaline endopeptidase that acts on an alpha-N-blocked synthetic substrate have been demonstrated in Plasmodium falciparum in culture. The enzymes were shown to be distinct by anion exchange chromatography, gel filtration on Sephadex G-200 and isoelectric focusing. The activities of the acid peptidase and the aminopeptidase were inhibited by antimalarial compounds.