2. Academic Validation
  3. Nothospondin, a new AP-1 inhibitory quassinoid from the Cameroonian plant Nothospondias staudtii

Nothospondin, a new AP-1 inhibitory quassinoid from the Cameroonian plant Nothospondias staudtii

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4397-9. doi: 10.1016/j.bmcl.2011.06.044.
Thushara Diyabalanage 1,  Ranjala Ratnayake,  Jennifer A Wilson,  Curtis J Henrich,  John A Beutler,  Nancy H Colburn,  James B McMahon,  Kirk R Gustafson
Affiliations

Affiliation

  • 1 Molecular Targets Laboratory, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, USA.
PMID: 21733691 DOI: 10.1016/j.bmcl.2011.06.044
Abstract

A high throughput screen for inhibitors of the oncogenic transcription factor activator protein-1 (AP-1) was applied to the NCI repository of natural product extracts. The liphophilic extract of the plant Nothospondias staudtii (Simaroubaceae) displayed significant AP-1 inhibition. Bioassay-guided fractionation of the extract lead to a new quassinoid named nothospondin (1), and the known compound glaucarubinone (2). The structure of 1 was elucidated by spectroscopic methods. Compounds 1 and 2 showed potent, dose-dependent AP-1 inhibition at noncytotoxic concentrations.

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