TABLE 3.
Effects of FXR agonists on IBD and CRC.
| Disease | FXR agonist | Effect | Model | Reference |
|---|---|---|---|---|
| IBD | OCA (INT-747; 6-ECDCA) | Immune dysfunction ↓ | 2,4,6-trinitrobenzene sulfonic acid (TNBS) or DSS -induced colitis mice | Vavassori et al., 2009 (Vavassori et al., 2009) |
| Inflammation ↓ | ||||
| Splenic DCs ↑ | DSS-treated mice | Massafra et al., 2016 (Massafra et al., 2016) | ||
| Migration of DCs and effector T cells to the colon ↓ | ||||
| Migration of Tregs to the colon↑ | ||||
| IL-10 ↑ | ||||
| Colonic inflammation ↓ | ||||
| GW4064 | LPS-induced TLR4/MyD88 signaling pathway ↓ | WT and FXR KO mice | Liu et al., 2017 (Liu et al., 2017) | |
| Barrier damage in the ileum ↓ | ||||
| Mitochondrial dysfunction ↓ | ||||
| FexD | TGF-β Signaling ↑ | DSS-induced UC mice | Zhao et al., 2020 (Zhao et al., 2020) | |
| The phosphorylated level of Smad2 ↑ | ||||
| Tissue Damage ↓ | ||||
| Fexaramine | The bacterial abundance of short-chain fatty acids (SCFA) ↑ | DCA-treated mice | Xu et al., 2021 (Xu et al., 2021) | |
| DCA-induced intestinal inflammation ↓ | ||||
| Intestinal FgF15 ↑ | ||||
| Bile acid synthesis ↓ | ||||
| Nelumal A | Incidence of colonic mucosal ulcers ↓ | DSS-induced colitis mice | Miyazaki et al., 2021 (Miyazaki et al., 2021) | |
| Oxidative damage ↓ | ||||
| TNF-α ↓ | ||||
| CRC | OCA (INT-747; 6-ECDCA) | SOCS3 ↑ | HT-29 and Caco-2 cells; nude mice | Li et al., 2020 (Li et al., 2020) |
| The activity of the JAK2/STAT3 pathway ↓ | ||||
| EMT ↓ | ||||
| Nelumal A | Incidence of adenocarcinoma ↓ | AOM/DSS-induced CRC mice | Miyazaki et al., 2021 (Miyazaki et al., 2021) | |
| Oxidative damage ↓ | ||||
| Apoptotic cancer cells ↑ | ||||
| TNF-α ↓ |