Diabetes Obesity and Metabolism · 2012 · 123 citations · 15 references
MedicineEndocrinologyPharmacologyMucosal Drug DeliveryPharmacodynamicsSignal TransductionBile Acid MetabolismBile SecretionDigestive PhysiologyGastrointestinal FunctionGastrointestinal PathophysiologyGastrointestinal PharmacologyAppetite Hormone RegulationBlood Glucose RegulationColonic PhysiologyEnteroendocrine CellsPeptide Yy PhysiologyPeptide Yy SignalingTgr5 SignalingTopical Application
Glucagon-like peptide-1 (GLP-1) and peptide YY (PYY), secreted by enteroendocrine L-cells located most densely in the colon and rectum, are of fundamental importance in blood glucose and appetite regulation. In animal models, colonic administration of bile acids can stimulate GLP-1 and PYY by TGR5 receptor activation. We evaluated the effects of taurocholic acid (TCA), administered as an enema, on plasma GLP-1 and PYY, as well as gastrointestinal sensations in 10 healthy male subjects, and observed that rectal administration of TCA promptly stimulated secretion of both GLP-1 and PYY, and increased fullness, in a dose-dependent manner. These observations confirm that topical application of bile acids to the distal gut may have potential for the management of type 2 diabetes and obesity.
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TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis
Charles Thomas, Antimo Gioiello, Lilia G. Noriega et al. · Cell Metabolism · 2009 · 1.8K citations · Full text
A G Protein-coupled Receptor Responsive to Bile Acids
Yuji Kawamata, Ryo Fujii, Masaki Hosoya et al. · Journal of Biological Chemistry · 2003 · 1.6K citations · Full text
Michael A. Nauck, Markus M. Heimesaat, Kai Behle et al. · The Journal of Clinical Endocrinology & Metabolism · 2002 · 579 citations · Full text