Reversal of metabolic disorders by pharmacological activation of bile acid receptors TGR5 and FXR.

ABSTRACT:

Objectives

Activation of the bile acid (BA) receptors farnesoid X receptor (FXR) or G protein-coupled bile acid receptor (GPBAR1; TGR5) improves metabolic homeostasis. In this study, we aim to determine the impact of pharmacological activation of bile acid receptors by INT-767 on reversal of diet-induced metabolic disorders, and the relative contribution of FXR vs. TGR5 to INT-767's effects on metabolic parameters.

Methods

Wild-type (WT), Tgr5^-/-, Fxr^-/-, Apoe^-/- and Shp^-/- mice were used to investigate whether and how BA receptor activation by INT-767, a semisynthetic agonist for both FXR and TGR5, could reverse diet-induced metabolic disorders.

Results

INT-767 reversed HFD-induced obesity dependent on activation of both TG

SUBMITTER: Jadhav K 

PROVIDER: S-EPMC5870099 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature