Tauroursodeoxycholic acid is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans. Tauroursodeoxycholic acid, on the other hand, is produced abundantly in bears and has been used for centuries as a natural remedy in some Asian countries. It is approved in Italy and Turkey for the treatment of cholesterol gallstones and is an investigational drug in China, Unites States, and Italy. Tauroursodeoxycholic acid is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis. The only completed clinical trial thus far is a phase III clinical trial comparing tauroursodeoxycholic acid and ursofalk in PBC adult patients, but as of June 2013 no results of this trial have been published.
antagonizes FXR activation by synthetic agonist GW4064, and TUDCA
is rapidly hydrolyzed by gut bacterial BSH (C.X. and A.D.P., unpublished observations), suggesting that high doses of TUDCA
might inhibit FXR signalling, resulting in improved insulin resistance.
To test the neuroprotective effect of TUDCA
on retinal function, full-field ERG recording was performed in parallel on a group of rats that received a daily intraperitoneal dose of TUDCA
three days prior to NDMA administration, and until their sacrifice (Fig 1A).
To further verify whether the effect of ox-LDL on adipocytes is associated with ER stress activation, the adipocytes were pretreated for 12 hours with various doses of TUDCA
(580549, Calbiochem, Gibbstown, NJ)) ( 0- 400µM) ,a chemical chaperone known to ameliorate ER stress , and then stimulated with 50 μg/ml of ox-LDL plus ACAT inhibitor 58035 for 48 hours.