2. Academic Validation
  3. Lipstatin, an inhibitor of pancreatic lipase, produced by Streptomyces toxytricini. I. Producing organism, fermentation, isolation and biological activity

Lipstatin, an inhibitor of pancreatic lipase, produced by Streptomyces toxytricini. I. Producing organism, fermentation, isolation and biological activity

  • J Antibiot (Tokyo). 1987 Aug;40(8):1081-5. doi: 10.7164/antibiotics.40.1081.
E K Weibel 1,  P Hadvary,  E Hochuli,  E Kupfer,  H Lengsfeld
Affiliations

Affiliation

  • 1 Central Research Units, F. Hoffmann-La Roche & Co., Ltd., Basel, Switzerland.
PMID: 3680018 DOI: 10.7164/antibiotics.40.1081
Abstract

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 beta-lactone structure that probably accounts for the irreversible Lipase inhibition. The IC50 of lipstatin for pancreatic Lipase is 0.14 microM. 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 microM.

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