Lithocholic acid

Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR. Lithocholic acid directly binds VDR (vitamin D receptor) with Ki of 29μM, activates VDR (vitamin D receptor) 30 μM, with much more sensitivity than the other nuclear receptors (eg. PXR, FXR), and its toxic effect is thus protected. Lithocholic acid has tumor-promoting activity, inhibits mammalian DNA Polymerase β with IC50 of 15 μM.