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