EFFECTS OF SUCRALFATE AND ITS COMPONENTS ON ACID-INDUCED AND PEPSIN-INDUCED DAMAGE TO RAT GASTRIC EPITHELIAL-CELLS

We have established models of cell damage induced by acid and pepsin u sing rat gastric epithelial cells (RGM1). In the present study, the ef fects of aluminum hydroxide [AI(OH)(3)] and potassium sucrose octasulf ate (KSOS), which are components of sucralfate, and sucralfate on cell damage and peptic activity of pepsin were examined. Pretreatment of c ells with sucralfate (0.1-3 mg/ml) or Al(OH)3 (0.1-1 mg/ml) for 2 hr p revented both acid-(pH 4.0) and pepsin-(pH 4.5) induced cell damage. H owever, KSOS (0.1-1 mg/ml) did not show any effects on two different t ypes of cell damage. The peptic activity of pepsin at pH 4.5 was about 10% of that at pH 2.0. Sucralfate and KSOS slightly inhibited peptic activity at pH 4.5. AI(OH)3 inhibited peptic activity by approximately 50%; however, no concentration-dependent pattern was observed. Pepsta tin (0.003-0.1 mg/ml), a specific inhibitor of pepsin, inhibited the p eptic activity in a concentration-dependent manner. Here, we confirmed that sucralfate and Al(OH)3 have cytoprotective effects against acid- and pepsin-induced cell damage. The mechanism behind the cytoprotectiv e effects of sucralfate seems to relate to adhesion of the cell surfac e and neutralization of hydrogen ion by aluminum that prevents the pen etration of hydrogen ions into the cells.