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] | – | |||
GW4064 | N/A | – | ↑ Glycogen [150] ↑ Insulin sensitivity [151] ↓ Glucose | ↓ TAG/FFA | ↑ 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] | – |