The activation effect of nobiletin on cystic fibrosis transmembrane conductance regulator chloride channel / 药学学报
Acta Pharmaceutica Sinica
;
(12): 848-854, 2013.
Article
Dans Chinois
| 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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Rats de lignée F344
/
Glande thyroide
/
Facteurs temps
/
Trachée
/
Benzoates
/
Techniques de patch-clamp
/
Protéine CFTR
/
Sécrétions corporelles
/
Biologie cellulaire
Limites du sujet:
Animaux
/
Humains
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2013
Type:
Article
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