TUDCA (25 micromol/L) reversed the effects of TLCA on bile flow, secretion of HRP and GS-DNP, and distribution of alpha-PKC. TUDCA reduced membrane binding of epsilon-PKC and increased Mrp2 density 4-fold in canalicular membranes of cholestatic hepatocytes.

2020年7月9日 · 熊去氧胆酸 (UDCA)是一种用于胆汁淤积性肝病治疗的重要药物。 UDCA 作为内源性药物的代表，在人体内具有胆汁酸特有的宿主-肠道菌群共代谢和肝-胆-肠循环处置特征，这为其仿制药研发带来了高度的技术挑战。 这些技术挑战不仅有来源于分子两亲性质的生物药剂学问题和来源于大规格的药剂学问题，更有来源于内源性、长半衰期、高变异、准确测定多个代谢物的药代动力学问题。 基于此，本文系统整理了人体UDCA药代动力学和内源性UDCA 代谢相关的文 …

UDCA activates transporter proteins such as bile acid export pump (BSEP), multiresistance protein 2 (MRP2) – conjugates transporter, type 2 anion exchanger (AE2), and promotes their movement to the canalicular membrane of cells.

2018年3月1日 · Mrp2 is the primary transporter to eliminate GSH-ANIT conjugate via the biliary route, and the induction of Mrp2 by UDCA would indicate that there might be more excretion of GSH-ANIT into bile duct in the acute model (Dietrich et al., 2001), which could cause greater injury to the cholangiocytes.

2005年12月12日 · Its taurine conjugate, TUDCA, was recently shown to stimulate insertion of the apical conjugate export pump, Mrp2 (ABCC2), into canalicular membranes of rat hepatocytes made cholestatic by...

Effect of ursodeoxycholic acid (UDCA) treatment on the expression and function of intestinal multidrug resistance-associated protein (Mrp) 2 was examined in rats. When rats were orally administered 0.5% UDCA solution for 6 days, mRNA and protein levels of Mrp2 in the intestine were increased about t …

Ursodeoxycholic acid exerts anticholestatic effects in chronic cholestatic liver disease in humans as well as in experimental animal models of cholestasis. Its taurine conjugate, TUDCA, was recently shown to stimulate insertion of the apical conjugate export pump, Mrp2 (ABCC2), into canalicular memb …

Ursodeoxycholic acid (UDCA) exerts anticholestatic, antifibrotic and antiproliferative effects in primary biliary cirrhosis (PBC) via mechanisms not yet fully understood. Its adequate biliary enrichment is considered mandatory for therapeutic efficacy.

In in vitro everted sac study, Mrp2-mediated efflux of 2,4-dinitrophenyl-S-glutathione (DNP-SG) to the mucosal surface was shown to be increased by UDCA treatment. In vivo intestinal exsorption clearance of DNP-SG was also increased by UDCA treatment.

2020年1月9日 · One bile acid has shown best potential improvement of PB oral delivery (ursodeoxycholic acid, UDCA). This study aimed to examine PB and UDCA microcapsules (with UDCA microcapsules serving...