Abstract
Several quassinoids were identified in a high-throughput screening assay as inhibitors of the transcription factor AP-1. Further biological characterization revealed that while their effect was not specific to AP-1, protein synthesis inhibition and cell growth assays were inconsistent with a mechanism of simple protein synthesis inhibition. Numerous plant extracts from the plant family Simaroubaceae were also identified in the same screen; bioassay-guided fractionation of one extract (Ailanthus triphylla) yielded two known quassinoids, ailanthinone (3) and glaucarubinone (4), which were also identified in the pure compound screening procedure.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
MeSH terms
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Ailanthus / chemistry*
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Cytotoxins / chemistry
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Cytotoxins / isolation & purification*
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Cytotoxins / pharmacology*
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Glaucarubin / analogs & derivatives
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Humans
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Molecular Structure
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Protein Synthesis Inhibitors / chemistry
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Protein Synthesis Inhibitors / isolation & purification*
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Protein Synthesis Inhibitors / pharmacology*
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Quassins / chemistry
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Quassins / isolation & purification*
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Quassins / pharmacology*
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Transcription Factor AP-1 / antagonists & inhibitors*
Substances
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Cytotoxins
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Protein Synthesis Inhibitors
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Quassins
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Transcription Factor AP-1
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ailanthinone
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glaucarubinone
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Glaucarubin