Vitamin D receptor as an intestinal bile acid sensor.

Regulation of Bile Acid Synthesis by Fat-soluble Vitamins A and D*

Bile acids are required for proper absorption of dietary lipids, including fat-soluble vitamins. Here, we show that the dietary vitamins A and D inhibit bile acid synthesis by repressing hepatic expression of the rate-limiting enzyme CYP7A1. Receptors for vitamin A and D induced expression of Fgf15, an intestine-derived hormone that acts on liver to inhibit Cyp7a1. These effects were mediated t...

Regulation of Vitamin D Receptor (VDR) Expression in Rat and Human intestine and Liver – Consequences for bile acid detoxification

Nuclear receptors as targets for drug development: regulation of cholesterol and bile acid metabolism by nuclear receptors.

Nuclear receptors are ligand-dependent transcription factors that recently have been shown to play important roles in the metabolism of cholesterol and bile acids. Cholesterol homeostasis is maintained by de novo synthesis, absorption from diet, catabolism to bile acids and other steroids, and excretion into bile. Dysregulation of this mechanism leads to atherosclerosis and its life-threatening...

Bile acid signaling in metabolic disease and drug therapy.

Bile acids are the end products of cholesterol catabolism. Hepatic bile acid synthesis accounts for a major fraction of daily cholesterol turnover in humans. Biliary secretion of bile acids generates bile flow and facilitates hepatobiliary secretion of lipids, lipophilic metabolites, and xenobiotics. In the intestine, bile acids are essential for the absorption, transport, and metabolism of die...

Bile Acid sulfation: a pathway of bile acid elimination and detoxification.

Sulfotransferase-2A1 catalyzes the formation of bile acid-sulfates (BA-sulfates). Sulfation of BAs increases their solubility, decreases their intestinal absorption, and enhances their fecal and urinary excretion. BA-sulfates are also less toxic than their unsulfated counterparts. Therefore, sulfation is an important detoxification pathway of BAs. Major species differences in BA sulfation exist...