METHOD OF INHIBITING THE PRODUCTION AND/OR EFFECTS OF INTESTINAL PRO-INFLAMMATORY CYTOKINES, PROSTAGLANDINS AND OTHERS

摘要

The present invention shows that UR-12746-S, a novel locally acting compound which combines 5-ASA (an anti-inflammatory) and UR-12715 (a PAF antagonist) through an azo link, and analogous azo derivatives of 5-aminosalicylic acid compounds are able to inhibit cytokine production (IL-8, IL-1β and TNF-α in vitro, and are shown to have intestinal anti-inflammatory activity in vivo. Moreover, daily oral administration of azo derivatives of 5-aminosalicylic acid sodium salts are able to alleviate and/or prevent relapse of inflammatory disease induced in colitic rats. This beneficial effect is evidenced by a significant reduction in colonic myeloperoxidase activity and by a significant decrease in colonic IL-Iβ and TNF-α.