Conjugated bile salts

Conjugated bile salts are steroid-derived amphipathic molecules synthesized in the liver from cholesterol and conjugated with glycine or taurine to increase their solubility at physiological pH (PubChem: Bile Acids and Salts, 2024). Secreted into the intestinal lumen via the biliary tract, they play a critical role in the emulsification and absorption of dietary lipids and fat-soluble vitamins. Beyond digestion, they serve as important signaling molecules that activate the farnesoid X receptor (FXR) and the G protein-coupled bile acid receptor (TGR5), thereby regulating lipid, glucose, and energy homeostasis (Journal of Lipid Research: Bile acids as signaling molecules, 2009). In clinical practice, these molecules are targeted by bile acid sequestrants, which are non-absorbable resins that bind bile salts in the gut to prevent their reabsorption in the terminal ileum. This interruption of the enterohepatic circulation prompts the liver to upregulate the conversion of endogenous cholesterol into new bile acids, effectively lowering serum low-density lipoprotein (LDL) cholesterol levels (NIH: LiverTox - Bile Acid Sequestrants, 2020). Consequently, they are key targets in the management of hypercholesterolemia and certain cholestatic liver diseases (StatPearls: Bile Acid Sequestrants, 2023).

Other names

Conjugated bile acidsBile saltsGlyco-conjugated bile acidsTauro-conjugated bile acidsBile acid conjugates

Bile acid sequestration and interruption of enterohepatic circulation