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Exp Parasitol ; 263-264: 108807, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39043327

RESUMO

African trypanosomiasis and malaria are among the most severe health challenges to humans and livestock in Africa and new drugs are needed. Leaves of Hyptis suaveolens Kuntze (Lamiaceae) and Momordica charantia L. (Cucurbitaceae) were extracted with hexane, ethyl acetate, and then methanol, and subjected to silica gel column chromatography. Structures of six isolated compounds were elucidated through NMR and HR-EIMS spectrometry. Callistrisic acid, dehydroabietinol, suaveolic acid, suaveolol, and a mixture of suaveolol and suaveolic acid (SSA) were obtained from H. suaveolens, while karavilagenin D and momordicin I acetate were obtained from M. charantia. The isolated biomolecules were tested against trypomastigotes of Trypanosoma brucei brucei and T. congolense, and against Plasmodium falciparum. The most promising EC50 values were obtained for the purified suaveolol fraction, at 2.71 ± 0.36 µg/mL, and SSA, exhibiting an EC50 of 1.56 ± 0.17 µg/mL against T. b. brucei trypomastigotes. Suaveolic acid had low activity against T. b. brucei but displayed moderate activity against T. congolense trypomastigotes at 11.1 ± 0.5 µg/mL. Suaveolol and SSA were also tested against T. evansi, T. equiperdum, Leishmania major and L. mexicana but the antileishmanial activity was low. Neither of the active compounds, nor the mixture of the two, displayed any cytotoxic effect on human foreskin fibroblast (HFF) cells at even the highest concentration tested, being 200 µg/mL. We conclude that suaveolol and its mixture possessed significant and selective trypanocidal activity.


Assuntos
Hyptis , Momordica charantia , Extratos Vegetais , Folhas de Planta , Plasmodium falciparum , Trypanosoma brucei brucei , Trypanosoma brucei brucei/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Plasmodium falciparum/efeitos dos fármacos , Momordica charantia/química , Folhas de Planta/química , Hyptis/química , Tripanossomíase Africana/tratamento farmacológico , Tripanossomíase Africana/parasitologia , Animais , Trypanosoma congolense/efeitos dos fármacos , Triterpenos/farmacologia , Triterpenos/química , Triterpenos/isolamento & purificação , Humanos , Tripanossomicidas/farmacologia , Tripanossomicidas/química , Tripanossomicidas/isolamento & purificação
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