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1.
Eur J Pharmacol ; 755: 127-33, 2015 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-25773498

RESUMO

The aim of this study was to identify the active ingredients responsible for the anti-EV71 activity produced by Salvia miltiorrhiza extracts. A pGS-EV71 IRES-based bicistronic reporter assay platform was used for rapid analysis of compounds that could specifically inhibit EV71 viral IRES-mediated translation. The analysis identified 2 caffeic acid derivatives, magnesium lithospermate B (MLB) and rosmarinic acid (RA), which suppressed EV71 IRES-mediated translation at concentrations of 30µg/ml. We also found that MLB and RA inhibited EV71 infection when they were added to RD cells during the viral absorption stage. MLB had a low IC50 value of 0.09mM and a high TI value of 10.52. In contrast, RA had an IC50 value of 0.50mM with a TI value of 2.97. MLB and RA (100µg/ml) also reduced EV71 viral particle production and significantly decreased VP1 protein production. We propose that these two derivatives inhibit EV71 viral entry into cells and viral IRES activity, thereby reducing viral particle production and viral RNA expression and blocking viral VP1 protein translation. This study provides useful information for the development of anti-EV71 assays and reagents by demonstrating a convenient EV71 IRES-based bicistronic assay platform to screen for anti-EV71 IRES activity, and also reports 2 compounds, MLB and RA, which are responsible for the anti-EV71 activity of S. miltiorrhiza.


Assuntos
Antivirais/farmacologia , Cinamatos/farmacologia , Depsídeos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Enterovirus Humano A/efeitos dos fármacos , Animais , Células COS , Proteínas do Capsídeo/metabolismo , Linhagem Celular Tumoral , Chlorocebus aethiops , Enterovirus Humano A/metabolismo , Enterovirus Humano A/fisiologia , Infecções por Enterovirus/tratamento farmacológico , Humanos , Raízes de Plantas , Salvia miltiorrhiza , Replicação Viral/efeitos dos fármacos , Ácido Rosmarínico
2.
J Org Chem ; 76(2): 692-5, 2011 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-21162589

RESUMO

Starting from the sulfur-substituted indolizidines and quinolizidines, a few useful synthetic transformations have been developed and the synthesis of some natural products including indolizidine 209D, epimyrtine, lasubine II, 8a-epi-dendroprimine, and 5-epi-cermizine C has been accomplished.


Assuntos
Produtos Biológicos/síntese química , Compostos Heterocíclicos com 2 Anéis/síntese química , Indolizidinas/síntese química , Indolizinas/síntese química , Quinolizidinas/síntese química , Quinolizinas/síntese química , Enxofre/química , Produtos Biológicos/química , Compostos Heterocíclicos com 2 Anéis/química , Indolizidinas/química , Indolizinas/química , Estrutura Molecular , Quinolizidinas/química , Quinolizinas/química , Estereoisomerismo
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