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Secondary (iso)BAs cooperate with endogenous ligands to activate FXR under physiological and pathological conditions
Secondary bile acids work with natural molecules to activate the FXR receptor in healthy and diseased states
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Abstract
Almost 50% of isoBAs were metabolized to 3-oxo-BAs within 4 hours in cell-based assays.
- IsoBAs, stereoisomers of bile acids, are present in the feces and plasma of humans.
- Compared to CDCA and isoCDCA, DCA and isoDCA, as well as UDCA and isoUDCA, resulted in only slight increases in mRNA expression of FXR target genes.
- IsoCDCA was more effective than CDCA in stimulating FXR activity.
- IsoDCA and isoUDCA allowed FXR to be re-stimulated by a second dose of GW4064.
- In animals with biliary obstruction, UDCA did not increase intestinal Fgf15 levels, indicating a potential limitation of its efficacy in such conditions.
- UDCA was effective in inducing ileal Fgf15 and repressing hepatic bile acid synthesis in mice with impaired bile acid circulation.
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