Effects of rectal administration of taurocholic acid on glucagon-like peptide-1 and peptide YY secretion in healthy humans

Diabetes Obes Metab. 2013 May;15(5):474-7. doi: 10.1111/dom.12043. Epub 2012 Dec 17.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Rectal
  • Adult
  • Appetite Regulation / drug effects
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Body Mass Index
  • Cholagogues and Choleretics / administration & dosage
  • Cholagogues and Choleretics / pharmacology
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / physiopathology
  • Enema
  • Glucagon-Like Peptide 1 / drug effects*
  • Glucagon-Like Peptide 1 / metabolism*
  • Humans
  • Male
  • Obesity / drug therapy
  • Obesity / physiopathology
  • Peptide YY / drug effects*
  • Peptide YY / metabolism*
  • Taurocholic Acid / administration & dosage*
  • Taurocholic Acid / pharmacology*
  • Treatment Outcome


  • Blood Glucose
  • Cholagogues and Choleretics
  • Peptide YY
  • Taurocholic Acid
  • Glucagon-Like Peptide 1