Abstract
The marine endophytic fungus Coniothyrium cereale produces the structurally unusual polyketide-type alkaloids (-)-cereolactam (1) and (-)-cereoaldomine (3), incorporating a lactam and an imine functionality, respectively, as well as the related metabolite (-)-trypethelone (2). Compounds 1 and 3 showed selective inhibition of human leukocyte elastase with IC50 values of 9.28 and 3.01 μM, respectively. Compound 2 was found to be inhibitory toward Mycobacterium phlei, Staphylococcus aureus, and Escherichia coli and also cytotoxic against mouse fibroblast cells (IC50=7.5 μM).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / chemistry
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Alkaloids / isolation & purification*
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Alkaloids / pharmacology*
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Animals
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Ascomycota / chemistry*
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Escherichia coli / drug effects
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Fibroblasts
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Humans
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Inhibitory Concentration 50
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Leukocyte Elastase / antagonists & inhibitors*
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Marine Biology
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Mice
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Molecular Structure
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Mycobacterium phlei / drug effects
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Polyketides / chemistry
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Polyketides / isolation & purification*
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Polyketides / pharmacology*
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Staphylococcus aureus / drug effects
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Stereoisomerism
Substances
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Alkaloids
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Polyketides
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cereolactam
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Leukocyte Elastase