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
in Chinese
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Rats, Inbred F344
/
Thyroid Gland
/
Time Factors
/
Trachea
/
Benzoates
/
Patch-Clamp Techniques
/
Cystic Fibrosis Transmembrane Conductance Regulator
/
Bodily Secretions
/
Cell Biology
Limits:
Animals
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Type:
Article
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