Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Adicionar filtros








Intervalo de ano
1.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 361-367, 2015.
Artigo em Inglês | WPRIM | ID: wpr-812134

RESUMO

The present study was designed to determine the effects of Guanfu base A (GFA) on the late sodium current (INa.L), transient sodium current (INa.T), HERG current (IHERG), and Kv1.5 current (IKv1.5). The values of INa.L, INa.T, IHERG and IKv1.5 were recorded using the whole-cell patch clamp technique. Compared with other channels, GFA showed selective blocking activity in late sodium channel. It inhibited INa.L in a concentration-dependent manner with an IC50 of (1.57 ± 0.14) μmol · L(-1), which was significantly lower than its IC50 values of (21.17 ± 4.51) μmol · L(-1) for the INa.T. The inhibitory effect of GFA on INa,L was not affected by 200 μmol · L(-1) H2O2. It inhibited IHERG with an IC50 of (273 ± 34) μmol · L(-1) and has slight blocking effect on IKv1.5, decreasing IKv1.5 by only 20.6% at 200 μmol · L(-1). In summary, GFA inhibited INa.L selectively and remained similar inhibition in presence of reactive oxygen species. These findings may suggest a novel molecular mechanism for the potential clinical application of GFA in the treatment of cardiovascular disorders.


Assuntos
Animais , Feminino , Humanos , Masculino , Análise de Variância , Antiarrítmicos , Farmacologia , Relação Dose-Resposta a Droga , Cobaias , Células HEK293 , Ventrículos do Coração , Compostos Heterocíclicos de 4 ou mais Anéis , Farmacologia , Concentração Inibidora 50 , Potenciais da Membrana , Miócitos Cardíacos , Metabolismo , Técnicas de Patch-Clamp , Bloqueadores dos Canais de Sódio , Farmacologia , Canais de Sódio
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA