Scyphostatin, a neutral sphingomyelinase inhibitor from a discomycete, Trichopeziza mollissima: taxonomy of the producing organism, fermentation, isolation, and physico-chemical properties

J Antibiot (Tokyo). 1999 Jun;52(6):525-30. doi: 10.7164/antibiotics.52.525.

Abstract

We performed experiments to screen for neutral sphingomyelinase inhibitors using rat brain microsomes as an enzyme source. Among more than 10,000 microbial extracts tested, a mycelial extract of Trichopeziza mollissima SANK 13892 exhibited potent inhibitory activity. The active compound, scyphostatin, was purified by a series of chromatographies. Scyphostatin inhibited the enzyme with an IC50 value of 1.0 microM.

MeSH terms

  • Amides / chemistry
  • Amides / isolation & purification*
  • Amides / pharmacology
  • Animals
  • Ascomycota / classification
  • Ascomycota / metabolism*
  • Brain / ultrastructure
  • Chemical Phenomena
  • Chemistry, Physical
  • Chromatography, High Pressure Liquid
  • Drug Stability
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification*
  • Enzyme Inhibitors / pharmacology
  • Fermentation*
  • Gram-Positive Bacteria / drug effects
  • Microsomes / enzymology
  • Pyrones / chemistry
  • Pyrones / isolation & purification*
  • Pyrones / pharmacology
  • Rats
  • Rats, Wistar
  • Sphingomyelin Phosphodiesterase / antagonists & inhibitors*

Substances

  • Amides
  • Enzyme Inhibitors
  • Pyrones
  • scyphostatin
  • Sphingomyelin Phosphodiesterase