Entero-hepatic Circulation
Role of the Intestinal Bile Acid Transporters in Bile Acid and Drug Disposition, 2011
NTCP
The functional role of sodium taurocholate cotransporting polypeptide NTCP in the life cycle of hepatitis B, C and D viruses, 2018
Bile Acid Sequestrants for Lipid and Glucose Control, 2010
TGR5/GPBAR1
GPBAR1+and+cell+proliferation
GPBAR1
Metabolic effects of intestinal absorption and enterohepatic cycling of bile acids, 2015
hepatic+sodium bile+acid+uptake+tgr5
FXR/NR1H4
NR1H4
Bile acid treatment and FXR agonism lower postprandial lipemia in mice, 2020
free or conjugates bile acids interact with their receptors??
bile+acids+and+glycine
bile+acids+and+cysteine
interessante
Synthetic analogs
Obeticholic acid
Protein Aminoacids Percentage (Width 700 px)
- Postprandial dyslipidemia is a common feature of insulin-resistant states and contributes to increased cardiovascular disease risk. Recently, bile acids have been recognized beyond their emulsification properties as important signaling molecules that promote energy expenditure, improve insulin sensitivity, and lower fasting lipemia. Although bile acid receptors have become novel pharmaceutical targets, their effects on postprandial lipid metabolism remain unclear. Here, we investigated the potential role of bile acids in regulation of postprandial chylomicron production and triglyceride excursion. Healthy C57BL/6 mice were given an intraduodenal infusion of taurocholic acid (TA) under fat-loaded conditions, and circulating lipids were measured. Targeting of bile acid receptors was achieved with GW4064, a synthetic agonist to the farnesoid X receptor (FXR), and deoxycholic acid (DCA), an activator of the Takeda G-protein-coupled receptor 5. TA, GW4064, and DCA treatments all lowered postprandial lipemia. FXR agonism also reduced intestinal triglyceride content and activity of microsomal triglyceride transfer protein, involved in chylomicron assembly. Importantly, TA (but not DCA) effects were largely lost in FXR knockout mice. These bile acid effects are reminiscent of the antidiabetic hormone glucagon-like peptide-1 (GLP-1). Although the GLP-1 receptor agonist exendin-4 retained its ability to acutely lower postprandial lipemia during bile acid sequestration and FXR deficiency, it did raise hepatic expression of the rate-limiting enzyme for bile acid synthesis. Bile acid signaling may be an important mechanism of controlling dietary lipid absorption, and bile acid receptors may constitute novel targets for the treatment of postprandial dyslipidemia.
Bile acid treatment and FXR agonism lower postprandial lipemia in mice, 2020 PDF
