Fatty acid bile acid conjugates - novel agents for prevention and treatment of gallstones

摘要

Phospholipids play an important role in biliary cholesterol solubilization as well as crystallization; they increase the cholesterol-carrying capacity of bile salt micelles by forming mixed micelles. Moreover, phospholipids by themselves can carry biliary cholesterol within vesicles with a 3-fold capacity compared to micelles. The addition of small amounts of phospholipids to bile inhibits cholesterol crystallization significantly, while similar amounts of bile salts have no notable effect. Phospholipids with long saturated acyl chain are more effective than less saturated ones. We have shown that the saturation of the sn-2 fatty acid chain of phospholipids, which is more prone to variation in human bile, plays a particularly important role in cholesterol solubilization and crystallization. Moreover, long chain saturated free fatty acids by themselves can prolong the cholesterol crystallization time of biles.