Lipstatin, an inhibitor of pancreatic lipase, produced by streptomyces toxytricini i. producing organism, fermentation, isolation and biological activity

Abstract

Lipstatin, a new and very potent inhibitor of pancreatic lipase (the key enzyme of in-testinal fat digestion) was isolated from Streptomyces toxytricini. Lipstatin contains a structure that probably accounts for the irreversible lipase inhibition. The IC50 of lipstatin for pancreatic lipase is 0.14. In mice triolein absorption was dose-dependently inhibited by lipstatin, whereas oleic acid was absorbed normally. Other pancreatic enzymes, such as phospholipase A2 and trypsin, were not inhibited even at an inhibitor concentration of 200 μm. © 1987, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.