| Name | Lithocholic acid |
| Description | Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic. |
| Kinase Assay | Competitive ligand binding assay.: Ligand binding is performed using lysates from COS-7 cells transfected with expression plasmids for VDR or RXRα. Binding is performed overnight at 4°C in lysate buffer with 0.71 nM (18 Ci/mmol) [3H]1,25(OH)2D3 and bile acid competitor. Unbound [3H]1,25(OH)2D3 is removed by adsorption to dextran-coated charcoal and the supernatant removed for scintillation counting. Ki values are calculated from a computer fit of competition curves from triplicate assays. |
| In vitro | In a mouse cancer model induced by DMH (dimethylhydrazine), LCA effectively inhibits apoptosis almost completely in the precancerous colon. When administered to rodents, LCA and its conjugates cause intrahepatic cholestasis, a pathological state characterized by reduced bile flow and the accumulation of bile components in the liver and blood. Lithocholic acid activates the vitamin D receptor, inducing the expression of CYP3A, a cytochrome P450 enzyme that detoxifies LCA in the liver and intestines. |
| In vivo | Lithocholic acid exhibits tumor-promoting activity and inhibits mammalian DNA polymerase β with an IC50 of 15 μM. It causes cholestasis (cessation or obstruction of bile flow) within the liver. Furthermore, lithocholic acid activates the Pregnane X Receptor (PXR), and the severe liver damage induced by LCA can be mitigated by the activation of PXR. Additionally, lithocholic acid directly binds to the vitamin D receptor with a Ki of 29 μM, activating it with a sensitivity higher than that for other nuclear receptors (e.g., PXR, FXR), with a Ki of 30 μM. This activation offers protection from its toxic effects. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 44 mg/mL (116.8 mM)
DMSO : 55 mg/mL (146.05 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Autophagy | Apoptosis | Lithocholic acid | inhibit | Endogenous Metabolite | Inhibitor | 3a-Hydroxy-5b-cholanic acid | 3alpha-Hydroxy-5beta-cholanic acid |
| Inhibitors Related | Sucrose | Hydroxychloroquine | Daidzein | Guanidine hydrochloride | Tributyrin | Ferulic Acid | Paeonol | Glycerol | Thymidine |
| Related Compound Libraries | Anti-Tumor Natural Product Library | Microbial Natural Product Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Natural Product Library for HTS | Human Endogenous Metabolite Library | Anti-infective Natural Product Library | Anti-Aging Compound Library | Gut Microbial Metabolite Library | Anti-Cancer Drug Library |
United States
