1. Academic Validation
  2. Quassinoid inhibition of AP-1 function does not correlate with cytotoxicity or protein synthesis inhibition

Quassinoid inhibition of AP-1 function does not correlate with cytotoxicity or protein synthesis inhibition

  • J Nat Prod. 2009 Mar 27;72(3):503-6. doi: 10.1021/np800732n.
John A Beutler 1 Moon-Il Kang Francis Robert Jason A Clement Jerry Pelletier Nancy H Colburn Tawnya C McKee Ekaterina Goncharova James B McMahon Curtis J Henrich
Affiliations

Affiliation

  • 1 Molecular Targets Development Program and Laboratory of Cancer Prevention, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, USA. beutlerj@mail.nih.gov
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.

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