Abstract
A cojugate(Lys-UDCA)of ursodeoxycholic acid (UDCA) with L-lysine was newly synthesized, and basic studies on this compound were carried out. In the incubation experiments with plasma, homogenates of the liver and small intestine, various pancreatic enzymes and cholylglycine hydrolase (CGH), carboxypeptidase B and CGH deconjugated Lys-UDCA. In the experiment using rodent everted gut sac, Lys-UDCA was actively absorbed from the terminal ileum. Conjugated (tauro-or glyco-UDCA) and free UDCA as well as Lys-UDCA were recovered well in the bile after intravenous or intraileal administration of Lys-UDCA in biliary fistula rat. Lys-UDCA showed less hemolytic action compared to tauro-UDCA and free UDCA. These data suggest that Lys-UDCA is a good prodrug of UDCA for intravenous administration.
