Hypocholesterolemic effect of bile acid sulfonate analogs in hamsters

We studied the effects of bile acid sulfonate analogs, namely, 3 alpha ,7 a lpha ,12 alpha -trihydroxy-5 beta -cholane-24-sulfonate (C-sul), 3 alpha ,7 alpha -dihydroxy-5 beta -cholane-24-sulfonate (CDC-sul), and 3 alpha ,7 be ta -dihydroxy-5 beta -cholane-24-sulfonate (UDC-sul), on serum and Liver ch olesterol levels, cholesterol 7 alpha -hydroxylase activity, and biliary bi le acid composition in hamsters fed cholesterol, Of the three analogs studi ed, UDC-sul slightly but significantly decreased free, esterified, and tota l cholesterol concentrations in the serum. UDC-sul and CDC-sul reduced live r total cholesterol levels by 25% and 18%, respectively, particularly in th e esterified cholesterol fraction. Analysis of biliary bile acids showed th e presence of the administered analogs, indicating that sulfonate analogs e fficiently participate in enterohepatic cycling. The proportion of cholic a cid was increased in all groups fed sulfonate analogs, but the ratio of gly cine to taurine conjugated bile acids (GIT) was elevated only in UDC-sul fe eding hamsters, There was no significant change in cholesterol 7 alpha -hyd roxylase activity in hamsters fed C-sul or CDC-sul, while UDC-sul slightly stimulated the enzyme activity compared to the control. The UDC-sul induced decrease in serum and liver cholesterol concentrations may be secondary to enhanced bile acid synthesis. This is supported by the increased cholester ol 7a-hydroxylase activity and elevated G/T ratio in biliary bile acids obs erved following UDC-sul administration.