Abstract
As part of a search for novel inhibitors of endothelin converting enzyme (ECE), the MeOH extract of a South African sponge, Pachastrella sp., was shown to be active. Bioassay-guided fractionation of the extract yielded a novel sterol sulfate, halistanol disulfate B (1). The structure and stereochemistry of 1 was established mainly by interpretation of spectral data. Disulfate (1) was found to be active at a micromolar concentration in the ECE assay.
MeSH terms
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Animals
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Chemical Phenomena
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Chemistry, Physical
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Endothelin-Converting Enzymes
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Humans
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Magnetic Resonance Spectroscopy
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Metalloendopeptidases
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Porifera / chemistry*
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Recombinant Proteins / chemistry
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Recombinant Proteins / pharmacology
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Spectrophotometry, Infrared
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Sterols / isolation & purification*
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Sterols / pharmacology
Substances
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Recombinant Proteins
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Sterols
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halistanol disulfate B
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Aspartic Acid Endopeptidases
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Metalloendopeptidases
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Endothelin-Converting Enzymes