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.

在DMH（二甲基肼）诱导的小鼠癌发生模型中,LCA几乎在癌前结肠中完全抑制细胞凋亡.将LCA及其缀合物施用于啮齿动物会引起肝内胆汁淤积,这是一种以胆汁流量减少和胆汁成分在肝脏和血液中积聚为特征的致病状态.Lithocholic acid激活维生素D 受体,诱导CYP3A在体内的表达,CYP3A是一种细胞色素P450酶,可将肝脏和肠中的LCA解毒.

Lithocholic acid具有肿瘤促进活性,抑制哺乳动物DNA聚合酶β,IC50为15 μM。Lithocholic acid引起肝内胆汁郁积(胆汁流终止或被阻碍)。Lithocholic acid激活PXR（孕烷X受体）,并且LCA诱导的严重肝脏损伤能够被PXR的激活保护。Lithocholic acid直接结合Ki为29 μM的维生素D受体,激活维生素D受体,Ki为30 μM,比其他核受体(例如 PXR,FXR)具有更高的敏感性,并且它的毒性效应因此被保护。

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.