Bariatric surgery reveals a gut-restricted TGR5 agonist with anti-diabetic effects

Nat Chem Biol. 2021 Jan;17(1):20-29. doi: 10.1038/s41589-020-0604-z. Epub 2020 Aug 3.

Abstract

Bariatric surgery, the most effective treatment for obesity and type 2 diabetes, is associated with increased levels of the incretin hormone glucagon-like peptide-1 (GLP-1) and changes in levels of circulating bile acids. The levels of individual bile acids in the gastrointestinal (GI) tract after surgery have, however, remained largely unstudied. Using ultra-high performance liquid chromatography-mass spectrometry-based quantification, we observed an increase in an endogenous bile acid, cholic acid-7-sulfate (CA7S), in the GI tract of both mice and humans after sleeve gastrectomy. We show that CA7S is a Takeda G-protein receptor 5 (TGR5) agonist that increases Tgr5 expression and induces GLP-1 secretion. Furthermore, CA7S administration increases glucose tolerance in insulin-resistant mice in a TGR5-dependent manner. CA7S remains gut restricted, minimizing off-target effects previously observed for TGR5 agonists absorbed into the circulation. By studying changes in individual metabolites after surgery, the present study has revealed a naturally occurring TGR5 agonist that exerts systemic glucoregulatory effects while remaining confined to the gut.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Obesity Agents / metabolism
  • Anti-Obesity Agents / pharmacology*
  • Bariatric Surgery / methods*
  • Bile / chemistry
  • Bile / metabolism
  • Caco-2 Cells
  • Cholic Acid / biosynthesis
  • Cholic Acid / pharmacology*
  • Colon / metabolism
  • Gene Expression Regulation
  • Glucagon-Like Peptide 1 / genetics
  • Glucagon-Like Peptide 1 / metabolism
  • Glucose Tolerance Test
  • HEK293 Cells
  • Humans
  • Insulin Resistance
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Obese
  • Obesity / genetics
  • Obesity / metabolism
  • Obesity / pathology
  • Obesity / surgery*
  • RNA, Small Interfering / genetics
  • RNA, Small Interfering / metabolism
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / genetics*
  • Receptors, G-Protein-Coupled / metabolism
  • Signal Transduction
  • Sulfates

Substances

  • Anti-Obesity Agents
  • GPBAR1 protein, human
  • Gpbar1 protein, mouse
  • RNA, Small Interfering
  • Receptors, G-Protein-Coupled
  • Sulfates
  • Glucagon-Like Peptide 1
  • Cholic Acid