LIPSTATIN, AN INHIBITOR OF PANCREATIC LIPASE, PRODUCED BY STREPTOMYCES TOXYTRICINI

I. PRODUCING ORGANISM, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITY

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Lipstatin, a new and very potent inhibitor of pancreatic lipase (the key enzyme of intestinal fat digestion) was isolated from Streptomyces toxytricini. Lipstatin contains a β-lactone structure that probably accounts for the irreversible lipase inhibition. The IC₅₀ of lipstatin for pancreatic lipase is 0.14 μM. 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.