Xylogranin B: A Potent Wnt Signal Inhibitory Limonoid from Xylocarpus granatum
Xylogranin B: A Potent Wnt Signal Inhibitory Limonoid from Xylocarpus granatum
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DOI：
10.1021/ol4029995
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发表时间：
2013-12-06
期刊：
影响因子：
5.2
通讯作者：
Ishibashi, Masami
中科院分区：
文献类型：
--
作者：
Toume, Kazufumi;Kamiya, Kentaro;Ishibashi, Masami
通过使用针对 Wnt 信号通路的基于细胞的荧光素酶筛选系统，从 Xylocarpus granatum（楝科）叶子中分离出 Xylogranin B (2)。化合物 2 抑制 TCF/β-catenin 转录活性 (IC50 48.9 nM)，并对结肠癌细胞系表现出强烈的细胞毒性。化合物 2 显着降低细胞核中的 β-连环蛋白水平，但不降低细胞质中的 β-连环蛋白水平。这些结果表明，细胞核中 β-连环蛋白水平降低 2 会导致 Wnt 信号抑制效果降低 2。
Xylogranin B (2) was isolated from Xylocarpus granatum (Meliaceae) leaves, by use of a cell-based luciferase screening system targeting a Wnt signaling pathway. Compound 2 inhibited TCF/beta-catenin transcriptional activity (IC50 48.9 nM) and exhibited strong cytotoxicity against colon cancer cell lines. Compound 2 significantly decreased beta-catenin protein levels in nuclei but not in the cytosol. These results indicated that a decrease in beta-catenin levels in nuclei by 2 resulted in the Wnt signal inhibitory effects of 2.