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.
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DOI：
10.1016/j.bmcl.2011.06.044
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发表时间：
2011-08-01
影响因子：
2.7
通讯作者：
Gustafson KR
中科院分区：
文献类型：
--
作者：
Diyabalanage T;Ratnayake R;Wilson JA;Henrich CJ;Beutler JA;Colburn NH;McMahon JB;Gustafson KR
致癌转录因子激活蛋白 1 (AP-1) 抑制剂的高通量筛选应用于 NCI 天然产物提取物存储库。植物 Nothospondias staudtii（Simaroubaceae）的亲脂性提取物表现出显着的 AP-1 抑制作用。通过生物测定指导对提取物进行分馏，得到一种名为 nothospondin (1) 的新型苦木素类化合物，以及已知的化合物 glaucarubinone (2)。通过光谱方法阐明了1的结构。化合物 1 和 2 在非细胞毒性浓度下显示出有效的剂量依赖性 AP-1 抑制作用。
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.