1999 Volume 52 Issue 6 Pages 531-535
Scyphostatin is a specific inhibitor for mammalian neutral magnesium-dependent Sphingomyelinase with a fifty percent inhibition concentration (IC50) value of 1.0 μM. When used to inhibit lysosomal acid Sphingomyelinase, an approximately 50-fold greater concentration is required. In human peripheral monocytes, the compound inhibits bacterial lipopolysaccharide (LPS)-induced prostaglandin E2 production and LPS-induced interleukin-1β production with IC50 values of 0.8 μM and 0.1 μM, respectively. In rat, p.o. administration of the compound has also been shown to inhibit carrageenin-induced paw edema. Thus, it is hoped that utility of scyphostatin as a pharmacological tool will contribute to our understanding of the role of ceramide in the cellular inflammation process.
