Skip to main content

Advertisement

Table 1 Bile acid receptors, ligands and cardiometabolic physiological effects

From: Bile acids at the cross-roads of gut microbiome–host cardiometabolic interactions

Receptor Natural and synthetic ligands Serum concentration (nM) [107] Relative potency Reported physiological effects
Adiposity glucose metabolism Lipid metabolism Vascular disease HF and HTN
FXR CDCA 380 ↑ BAT [39] ↓ Glucose ↓ Insulin [147] ↓ TAG [147] ↑ RCT [86] ↓ BP [98]
CA 440
DCA 320
LCA < LOD
UDCA 43
WAY-362450 N/A   ↓ TAG [148] ↓ Cholesterol [89, 149] ↓ Atherosclerosis [88, 89]
GW4064 N/A ↑ Glycogen [150] ↑ Insulin sensitivity [151] ↓ Glucose ↓ TAG/FFA ↓ Cholesterol [152,153,154] ↑ RCT [87]
OCA N/A ↑ BAT ↓ WAT [113] ↓ Glucose [113] ↑ LDL [113] ↓ HDL [117] ↑ RCT [155] ↓ BP [78]
Fexaramine N/A ↑ BAT [52] ↓ Glucose ↓ Gluconeogenesis ↓ Insulin [52] ↓ Cholesterol [52]
TGR5 LCA < LOD ↑ BAT ↑ T4 T3 [40] ↓ Glucose ↓ Insulin [40] ↑ NO ↓ Monocyte infiltration [94]
TLCA 0.33
CA 440
DCA 320
CDCA 380
6-EMCA/INT-777 N/A   ↑ BAT ↓ WAT [156] ↑ GLP-1 [156] ↓ TAG/NEFA [156] ↓ Atherosclerosis ↓ Foam cell [93]
  1. BAT brown adipose tissue, WAT white adipose tissue, T4 thyroxine, T3 triiodothyronine, GLP-1 glucagon-like peptide-1, TAG triacylglycerides, FFA free fatty acids, NEFA non-esterified fatty acids, RCT reverse cholesterol transport, NO nitric oxide, BP blood pressure, LOD limit of detection, N/A not applicable