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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Diyabalanage, Thushara¹  Ratnayake, Ranjala¹  Wilson, Jennifer A.¹  Henrich, Curtis J.^1,2  Beutler, John A.¹  Colburn, Nancy H.³  McMahon, James B.¹  Gustafson, Kirk R.¹ 

[1] NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA

[2] NCI, SAIC Frederick, Frederick, MD 21702 USA

[3] NCI, Lab Canc Prevent, Ctr Canc Res, Frederick, MD 21702 USA

关键词: Quassinoid;    Nothospondias staudtii;    Simaroubaceae;    Transcription factor;    AP-1;   

DOI  :  10.1016/j.bmcl.2011.06.044

来源: Elsevier

【 摘 要 】

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. Published by Elsevier Ltd.

【 授权许可】

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