The activation effect of nobiletin on cystic fibrosis transmembrane conductance regulator chloride channel / 药学学报
Acta Pharmaceutica Sinica
;
(12): 848-854, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-259541
ABSTRACT
Aim of the present study is to investigate activation effect of nobiletin on cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity. CFTR-mediated iodide influx assay and patch-clamp tests were done on FRT cells stably co-transfected with human CFTR and EYFP/H148Q. Nobiletin potently activated CFTR chloride channel activity in a dose- and time-dependent manner. The CFTR blocker CFTR(inh)-172 could completely reverse the effect. Preliminary mechanism study indicated that nobiletin activated CFTR chloride channel through a direct binding way. In addition, ex vivo tests done on mice trachea showed that nobiletin time-dependently stimulated submucosal gland fluid secretion. Nobiletin may be a therapeutic lead compound in treating CFTR-related diseases including disseminated bronchiectasis.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Ratos Endogâmicos F344
/
Glândula Tireoide
/
Fatores de Tempo
/
Traqueia
/
Benzoatos
/
Técnicas de Patch-Clamp
/
Regulador de Condutância Transmembrana em Fibrose Cística
/
Secreções Corporais
/
Biologia Celular
Limite:
Animais
/
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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