Abstract
A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2'',4''-O-diacetyl-alpha-l-rhamnopyranoside) (1), kaempferol 3-O-(3'',4''-O-diacetyl-alpha-l-rhamnopyranoside) (2), and kaempferol-3-O-(4''-O-acetyl-alpha-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC(50) value of 89 nM.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Acetylation
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Apocynaceae / chemistry*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Flavonols / chemistry
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Flavonols / pharmacology*
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Glycosides / chemistry
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Glycosides / pharmacology*
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Molecular Structure
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Ribosomal Protein S6 Kinases, 90-kDa / antagonists & inhibitors*
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Species Specificity
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Stereoisomerism
Substances
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Enzyme Inhibitors
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Flavonols
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Glycosides
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Plant Extracts
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Ribosomal Protein S6 Kinases, 90-kDa