Bile Acids Transport and Receptors
Bile Acids Synthesis

Author: Gianpiero Pescarmona
Date: 27/06/2021

Description

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

Attachments
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BA_TR_R_ch1.pnggp01/08/2021
BA_TR_R_ch2.pnggp01/08/2021
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