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Biological Activities of Scyphostatin, a Neutral Sphingomyelinase Inhibitor from a Discomycete, Trichopeziza mollisima.

1999; Springer Nature; Volume: 52; Issue: 6 Linguagem: Inglês

10.7164/antibiotics.52.531

1881-1469

Futoshi Nara, Masahiro Tanaka, SEIKO MASUDA-INOUE, YOKO YAMASATO, HIROMI DOI-YOSHIOKA, Keiko Suzuki‐Konagai, Seiichiro Kumakura, Takeshi Ogita,

Polysaccharides and Plant Cell Walls

Scyphostatin is a specific inhibitor for mammalian neutral magnesium-dependent sphingomyelinase with a fifty percent inhibition concentration (IC50) value of 1.0 microM. 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-1beta production with IC50 values of 0.8 microM and 0.1 microM, 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.