Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK.

Xu YM, Smith JA, Lannigan DA, Hecht SM
Bioorg Med Chem. 2006 14 (11): 3974-7

PMID: 16524738 · DOI:10.1016/j.bmc.2006.01.066

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.

MeSH Terms (10)

Acetylation Apocynaceae Enzyme Inhibitors Flavonols Glycosides Molecular Structure Plant Extracts Ribosomal Protein S6 Kinases, 90-kDa Species Specificity Stereoisomerism

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