ReferenceID 340

Inhibition of CFTR-mediated intestinal chloride secretion as potential therapy for bile acid diarrhea

FASEB J

Bile acid diarrhea (BAD) is common with ileal resection, Crohn's disease, and diarrhea-predominant irritable bowel syndrome. Here, we demonstrate the efficacy of cystic fibrosis transmembrane conductance regulator (CFTR

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Reference Id
340
Evidence Id
16930
Core Evidence Id
16930
Source Reference Id
648
Herb2 Reference Id
HBREF001088
Subject Paper Key
HBIN020281_31268738
Pubmed Id
31268738
Doi
10.1096/fj.201901166R
Paper Title
Inhibition of CFTR-mediated intestinal chloride secretion as potential therapy for bile acid diarrhea
Paper Abstract
Bile acid diarrhea (BAD) is common with ileal resection, Crohn's disease, and diarrhea-predominant irritable bowel syndrome. Here, we demonstrate the efficacy of cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor (R)-benzopyrimido-pyrrolo-oxazine-dione-27 (BPO-27) in reducing bile acid-induced fluid and electrolyte secretion in colon. Short-circuit current measurements in human T84 colonic epithelial cells and planar colonic enteroid cultures showed a robust secretory response following mucosal but not serosal addition of chenodeoxycholic acid (CDCA) or its taurine conjugate, which was fully blocked by CFTR inhibitors, including (R)-BPO-27. (R)-BPO-27 also fully blocked CDCA-induced secretory current in murine colon. CFTR activation by CDCA primarily involved Ca2+ signaling. In closed colonic loops in vivo, luminal CDCA produced a robust secretory response, which was reduced by 70% by (R)-BPO-27 or in CFTR-deficient mice. In a rat model of BAD produced by intracolonic infusion of CDCA, (R)-BPO-27 reduced the elevation in stool water content by >55%. These results implicate CFTR activation in the colon as a major prosecretory mechanism of CDCA, a bile acid implicated in BAD, and support the potential therapeutic efficacy of CFTR inhibition in bile acid-associated diarrheas.-Duan, T., Cil, O., Tse, C. M., Sarker, R., Lin, R., Donowitz, M., Verkman, A. S. Inhibition of CFTR-mediated intestinal chloride secretion as potential therapy for bile acid diarrhea.
Journal
FASEB J
Publish Year
2019
Experiment Subject
mouse; cells
Experiment Type
Animal & Cell Experiment
Phenotype Related
Paper Title Cn
Paper Title En
Inhibition of CFTR-mediated intestinal chloride secretion as potential therapy for bile acid diarrhea
Bilingual Status
semi_complete