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Bile acids are amphipathic steroid molecules synthesized from cholesterol in the liver and secreted into the gastrointestinal lumen to facilitate the digestion and absorption of dietary fats and fat-soluble vitamins. In the gut, they act as detergents to emulsify lipids and also serve as important signaling molecules that regulate metabolic processes through the activation of receptors like the farnesoid X receptor (FXR) and TGR5 (Nature Reviews Gastroenterology & Hepatology, 10.1038/nrgastro.2017.132). As a therapeutic target, bile acids in the gastrointestinal lumen are bound by non-absorbable resins known as bile acid sequestrants. This binding prevents their enterohepatic recirculation, leading to increased hepatic synthesis of bile acids from cholesterol and a subsequent reduction in serum LDL cholesterol levels (StatPearls, NBK526095). Additionally, targeting the bile acid pool is essential in managing bile acid malabsorption, which causes chronic diarrhea, and in alleviating pruritus associated with cholestatic liver diseases. The modulation of bile acid concentrations in the lumen also influences the gut microbiome and systemic metabolic health (PubMed, 28848233).
Bile acid sequestrants are non-absorbable anion-exchange resins that bind to negatively charged bile acids in the gastrointestinal lumen, forming insoluble complexes that are excreted in the feces and preventing their enterohepatic recirculation (StatPearls, NBK526095).
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