Abstract
EI-1507-1 and -2, novel interleukin-1 beta converting enzyme (ICE) inhibitors, were isolated from the culture broths of Streptomyces sp. E-1507. EI-1507-1 and EI-1507-2 selectively inhibited the recombinant human ICE activity with IC50 values of 0.23 and 0.42 microM, respectively. EI-1507-1 and EI-1507-2 also inhibited mature interleukin-1 beta secretion from THP-1 cells with IC50 values of 1.1 and 1.4 microM, respectively.
MeSH terms
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Amino Acid Sequence
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Anthraquinones / chemistry*
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Anthraquinones / classification
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Anthraquinones / pharmacology
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Benz(a)Anthracenes / chemistry*
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Benz(a)Anthracenes / classification
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Benz(a)Anthracenes / pharmacology
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Caspase 1
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Cell Survival / drug effects
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Cysteine Endopeptidases / biosynthesis*
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Cysteine Proteinase Inhibitors / chemistry*
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Cysteine Proteinase Inhibitors / classification
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Cysteine Proteinase Inhibitors / pharmacology
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Dose-Response Relationship, Drug
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Humans
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Magnetic Resonance Spectroscopy
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Sequence Data
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Molecular Structure
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Monocytes / drug effects
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Monocytes / metabolism
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Streptomyces / growth & development
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Streptomyces / metabolism*
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Streptomyces / physiology
Substances
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Anthraquinones
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Benz(a)Anthracenes
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Cysteine Proteinase Inhibitors
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EI 1507-1
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EI 1507-2
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Cysteine Endopeptidases
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Caspase 1