The activation effect of nobiletin on cystic fibrosis transmembrane conductance regulator chloride channel.
- Author:
Shuang YANG
;
Bo YU
;
Yaofang ZHANG
;
Xue WANG
;
Hong YANG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2013;48(6):848-54
- CountryChina
- Language:Chinese
-
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.
