[HTML][HTML] Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction

C Jiang, C Xie, Y Lv, J Li, KW Krausz, J Shi… - Nature …, 2015 - nature.com
C Jiang, C Xie, Y Lv, J Li, KW Krausz, J Shi, CN Brocker, D Desai, SG Amin, WH Bisson…
Nature communications, 2015nature.com
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we
show that treatment of mice with glycine-β-muricholic acid (Gly-MCA) inhibits FXR signalling
exclusively in intestine, and improves metabolic parameters in mouse models of obesity. Gly-
MCA is a selective high-affinity FXR inhibitor that can be administered orally and prevents,
or reverses, high-fat diet-induced and genetic obesity, insulin resistance and hepatic
steatosis in mice. The high-affinity FXR agonist GW4064 blocks Gly-MCA action in the gut …
Abstract
The farnesoid X receptor (FXR) regulates bile acid, lipid and glucose metabolism. Here we show that treatment of mice with glycine-β-muricholic acid (Gly-MCA) inhibits FXR signalling exclusively in intestine, and improves metabolic parameters in mouse models of obesity. Gly-MCA is a selective high-affinity FXR inhibitor that can be administered orally and prevents, or reverses, high-fat diet-induced and genetic obesity, insulin resistance and hepatic steatosis in mice. The high-affinity FXR agonist GW4064 blocks Gly-MCA action in the gut, and intestine-specific Fxr-null mice are unresponsive to the beneficial effects of Gly-MCA. Mechanistically, the metabolic improvements with Gly-MCA depend on reduced biosynthesis of intestinal-derived ceramides, which directly compromise beige fat thermogenic function. Consequently, ceramide treatment reverses the action of Gly-MCA in high-fat diet-induced obese mice. We further show that FXR signalling in ileum biopsies of humans positively correlates with body mass index. These data suggest that Gly-MCA may be a candidate for the treatment of metabolic disorders.
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