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

作者：Diyabalanage Thushara; Ratnayake Ranjala; Wilson Jennifer A; Henrich Curtis J; Beutler John A; Colburn Nancy H; McMahon James B; Gustafson Kirk R^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(15): 4397-4399.

DOI：10.1016/j.bmcl.2011.06.044

• Quassinoid
• Nothospondias staudtii
• Simaroubaceae
• Transcription factor
• AP-1

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.

• 出版日期2011-8-1