Abstract
In the course of screening for antifungal agents, we have discovered eight novel compounds, haplofungin A, B, C, D, E, F, G and H, from a culture broth of the fungus strain Lauriomyces bellulus SANK 26899. Haplofungins are composed of an arabinonic acid moiety linked through an ester to a modified long alkyl chain and show potent inhibitory activities against fungal inositol phosphorylceramide (IPC) synthase. Haplofungin A inhibited the activity of IPC synthase from Saccharomyces cerevisiae with an IC(50) value of 0.0015 microg ml(-1). This inhibitor also suppressed the growth of Candida glabrata at the MIC value of 0.5 microg ml(-1).
MeSH terms
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Antifungal Agents / chemistry
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Antifungal Agents / isolation & purification
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Antifungal Agents / metabolism
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Antifungal Agents / pharmacology*
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Ascomycota / classification
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Ascomycota / growth & development
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Ascomycota / isolation & purification
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Ascomycota / metabolism*
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Candida glabrata / drug effects
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Candida glabrata / enzymology
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology*
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Fatty Acids, Unsaturated / chemistry
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Fatty Acids, Unsaturated / isolation & purification
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Fatty Acids, Unsaturated / metabolism
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Fatty Acids, Unsaturated / pharmacology*
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Fermentation
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Hexosyltransferases / antagonists & inhibitors*
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Humans
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Microbial Sensitivity Tests
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Saccharomyces cerevisiae / drug effects
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Saccharomyces cerevisiae / enzymology
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Soil Microbiology
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Structure-Activity Relationship
Substances
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Antifungal Agents
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Enzyme Inhibitors
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Fatty Acids, Unsaturated
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Hexosyltransferases
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phosphatidylinositol-ceramide phosphoinositol transferase