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Phytochemistry ; 72(11-12): 1424-30, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21570099

RESUMO

(±)-Licarin A (1) was obtained by oxidative coupling, and its enantiomers, (-)-licarin A (2) and (+)-licarin A (3), were resolved by chiral HPLC. Schistosomicidal and trypanocidal activities of these compounds were evaluated in vitro against Schistosoma mansoni adult worms and trypomastigote forms of Trypanosoma cruzi. The racemic mixture (1) displayed significant schistosomicidal activity with an LC50 value of 53.57 µM and moderate trypanocidal activity with an IC50 value of 127.17 µM. On the other hand, the (-)-enantiomer (2), displaying a LC50 value of 91.71 µM, was more active against S. mansoni than the (+)-enantiomer (3), which did not show activity. For the trypanocidal assay, enantiomer 2 showed more significant activity (IC50 of 23.46 µM) than enantiomer 3, which showed an IC50 value of 87.73 µM. Therefore, these results suggest that (±)-licarin A (1) and (-)-licarin A (2) are promising compounds that could be used for the development of schistosomicidal and trypanocidal agents.


Assuntos
Lignanas/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Esquistossomicidas/química , Tripanossomicidas/química , Trypanosoma cruzi/efeitos dos fármacos , Animais , Chlorocebus aethiops , Cromatografia Líquida de Alta Pressão/métodos , Feminino , Concentração Inibidora 50 , Lignanas/química , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Acoplamento Oxidativo , Esquistossomicidas/farmacologia , Relação Estrutura-Atividade , Tripanossomicidas/farmacologia , Células Vero
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