Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1

Biochem Biophys Res Commun. 2005 Apr 1;329(1):386-90. doi: 10.1016/j.bbrc.2005.01.139.


Bile acids play essential roles in the absorption of dietary lipids and in the regulation of bile acid biosynthesis. Recently, a G protein-coupled receptor, TGR5, was identified as a cell-surface bile acid receptor. In this study, we show that bile acids promote glucagon-like peptide-1 (GLP-1) secretion through TGR5 in a murine enteroendocrine cell line STC-1. In STC-1 cells, bile acids promoted GLP-1 secretion in a dose-dependent manner. As STC-1 cells express TGR5 mRNA, we examined whether bile acids induce GLP-1 secretion through TGR5. RNA interference experiments showed that reduced expression of TGR5 resulted in reduced secretion of GLP-1. Furthermore, transient transfection of STC-1 cells with an expression plasmid containing TGR5 significantly enhanced GLP-1 secretion, indicating that bile acids promote GLP-1 secretion through TGR5 in STC-1 cells. Bile acids induced rapid and dose-dependent elevation of intracellular cAMP levels in STC-1 cells. An adenylate cyclase inhibitor, MDL12330A, significantly suppressed bile acid-promoted GLP-1 secretion, suggesting that bile acids induce GLP-1 secretion via intracellular cAMP production in STC-1 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclase Inhibitors
  • Animals
  • Bile Acids and Salts / chemistry*
  • Bile Acids and Salts / metabolism
  • Cell Line
  • Cyclic AMP / metabolism
  • Dose-Response Relationship, Drug
  • Enteroendocrine Cells / cytology*
  • Genetic Vectors
  • Glucagon / metabolism*
  • Glucagon-Like Peptide 1
  • Imines / pharmacology
  • Mice
  • Peptide Fragments / metabolism*
  • Plasmids / metabolism
  • Protein Precursors / metabolism*
  • RNA / chemistry
  • RNA Interference
  • RNA, Messenger / metabolism
  • Receptors, G-Protein-Coupled / metabolism*
  • Transfection
  • alpha-Linolenic Acid / chemistry


  • Adenylyl Cyclase Inhibitors
  • Bile Acids and Salts
  • GPBAR1 protein, human
  • Imines
  • Peptide Fragments
  • Protein Precursors
  • RNA, Messenger
  • Receptors, G-Protein-Coupled
  • alpha-Linolenic Acid
  • RNA
  • RMI 12330A
  • Glucagon-Like Peptide 1
  • Glucagon
  • Cyclic AMP