Abstract
As part of a search for novel inhibitors of endothelin converting enzyme (ECE), the MeOH-CH2Cl2 extract of the roots of Dalea filiciformis was shown to be active. Bioassay-guided fractionation of the extract yielded a novel phytoalexin, daleformis (1), whose structure was determined by interpretation of spectral data and X-ray analysis. Daleformis (1) inhibited ECE with an IC50 of 9 microM.
MeSH terms
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Acetylation
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Benzofurans / isolation & purification*
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Benzofurans / pharmacology
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Benzopyrans / isolation & purification*
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Benzopyrans / pharmacology
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Chromatography, Thin Layer
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Crystallography, X-Ray
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Endothelin-Converting Enzymes
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Enzyme Inhibitors / isolation & purification*
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Enzyme Inhibitors / pharmacology
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Metalloendopeptidases / antagonists & inhibitors*
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Molecular Conformation
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Plant Roots / chemistry*
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Plants, Medicinal / chemistry*
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Spectrophotometry, Infrared
Substances
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Benzofurans
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Benzopyrans
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Enzyme Inhibitors
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daleformis
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Aspartic Acid Endopeptidases
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Metalloendopeptidases
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Endothelin-Converting Enzymes