Abstract
The root and stem bark extracts of a Nigerian sample of Leptonychia pubescens Keay (Sterculiaceae) were found to inhibit the serine protease tryptase, a potential therapeutic target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Bioassay-guided isolation led to the identification of 1-beta-ribofuranosylbrunfelsamidine as the active component with a tryptase IC (50) of 3 microM. Brunfelsamidine was also isolated, but was only weakly active.
MeSH terms
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Humans
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Lung / enzymology
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Malvaceae / chemistry*
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Molecular Structure
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Monosaccharides / chemistry
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Monosaccharides / isolation & purification
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Monosaccharides / pharmacology*
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Plant Bark / chemistry
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Plant Extracts / chemistry
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Plant Roots / chemistry
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Serine Endopeptidases / metabolism*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / isolation & purification
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Serine Proteinase Inhibitors / pharmacology*
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Tryptases
Substances
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1-beta-ribofuranosylbrunfelsamidine
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Monosaccharides
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Plant Extracts
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Serine Proteinase Inhibitors
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Serine Endopeptidases
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Tryptases