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Braz. j. med. biol. res ; 43(11): 1054-1061, Nov. 2010. ilus, tab
Artigo em Inglês | LILACS | ID: lil-564126

RESUMO

Hypnophilin and panepoxydone, terpenoids isolated from Lentinus strigosus, have significant inhibitory activity onTrypanosoma cruzi trypanothione reductase (TR). Although they have similar TR inhibitory activity at 10 μg/mL (40.3 μM and 47.6 μM for hypnophilin and panepoxydone, respectively; ~100 percent), hypnophilin has a slightly greater inhibitory activity (~71 percent) on T. cruzi amastigote (AMA) growth in vitro as well as on in vitro phytohemagglutinin (PHA)-induced peripheral blood mononuclear (PBMC) proliferation (~70 percent) compared to panepoxydone (69 percent AMA inhibition and 91 percent PBMC inhibition). Hypnophilin and panepoxydone at 1.25 μg/mL had 67 percent inhibitory activity onLeishmania (Leishmania) amazonensis amastigote-like (AMA-like) growth in vitro. The panepoxydone activity was accompanied by a significant inhibitory effect on PHA-induced PBMC proliferation, suggesting a cytotoxic action. Moreover, incubation of human PBMC with panepoxydone reduced the percentage of CD16+ and CD14+ cells and down-regulated CD19+, CD4+ and CD8+ cells, while hypnophilin did not alter any of the phenotypes analyzed. These data indicate that hypnophilin may be considered to be a prototype for the design of drugs for the chemotherapy of diseases caused by Trypanosomatidae.


Assuntos
Humanos , Antiprotozoários/farmacologia , Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Leishmania/efeitos dos fármacos , Lentinula/química , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Antígenos CD/efeitos dos fármacos , Compostos Bicíclicos Heterocíclicos com Pontes/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Desenho de Fármacos , Leucócitos Mononucleares/efeitos dos fármacos , Sesquiterpenos/isolamento & purificação
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