An internal standard for the quantification of ursodeoxycholic acid
Ursodeoxycholic acid-d4 (UDCA-d4) is intended for use as an internal standard for the quantification of UDCA by GC- or LC-MS. UDCA is a secondary bile acid formed via epimerization of chenodeoxycholic acid .1,2 UDCA is also a metabolite of lithocholic acid in human liver microsomes.3 It inhibits taurocholic acid uptake in HeLa cells expressing recombinant sodium/taurocholate cotransporting polypeptide (NTCP) with an IC50 value of 3.6 μM.4 UDCA (50 μM) inhibits apoptosis induced by deoxycholic acid or ethanol in primary rat hepatocytes.5 Dietary administration of UDCA blocks DCA-induced increases in the number of TUNEL-positive hepatocytes in rats. Formulations containing UDCA have been used in the treatment of primary biliary cirrhosis.
1.Dawson, P.A., and Karpen, S.J.Intestinal transport and metabolism of bile acidsJ. Lipid Res.56(6)1085-1099(2015) 2.Chiang, J.Y.L.Bile acid metabolism and signaling in liver disease and therapyLiver Res.1(1)3-9(2017) 3.Deo, A.K., and Bandiera, S.M.3-Ketocholanoic acid is the major in vitro human hepatic microsomal metabolite of lithocholic acidDrug Metab. Dispos.37(9)1938-1947(2009) 4.Kim, R.B., Leake, B., Cvetkovic, M., et al.Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activityJ. Pharmacol. Exp. Ther.291(3)1204-1209(1999) 5.Rodrigues, C.M.P., Fan, G., Ma, X., et al.A novel role for ursodeoxycholic acid in inhibiting apoptosis by modulating mitochondrial membrane perturbationJ. Clin. Invest.101(12)2790-2799(1998)
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