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. 2022 Oct 6;13:1016836. doi: 10.3389/fphar.2022.1016836

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 ↓