Betulin

Betulin (lup-20 (29) -ene-3β,28-diol) is an abundant, naturally occurring triterpene. It is commonly isolated from the bark of birch trees where it forms up to 30% of the dry weight of the extractive and is found in birch sap as well. (In Vitro) :Obeticholic acid (INT-747) increases the expression of FXR-regulated genes in rat hepatocytes. Obeticholic acid (INT-747) reduces expression of liver JNK-1 and JNK-2. Obeticholic acid (INT-747) (256 μg/mL) shows complete inhibition of bacterial growth in all strains tested. Intestinal permeability remains unaffected after INT-747-addition to an IFN-γ-exposed intestinal epithelium of Caco-2 cells. (In Vivo) :Obeticholic acid (INT-747) (10 mg/kg/day) completely reverted cholestasis induced by E217α. Administration of Obeticholic acid (INT-747) partially prevents the impairment in total bile acid output caused by E217α by increasing the relative abundance of β-MCA and TCDCA and TDCA. Obeticholic acid (INT-747) 7 (10 mg/kg) and HS increases the pulmonary congestion in the animals. INT-747 does not improve renal pathology in the HS-fed animals. Obeticholic acid (INT-747) (5 mg/kg) significantly increases survival in BDL rats. Obeticholic acid (INT-747) -treated BDL rats exhibits a significant selective ileal increase in expression of pore-closing claudin-1. Ileal expression of ZO-1 is significantly up-regulated in INT-747-treated BDL rats.