Graduate School of Pharmaceutical Sciences, Chiba University , 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan , Pharmacy Discipline, Life Science School, Khulna University , Khulna 9208, Bangladesh , and Department of Pharmaceutical Chemistry, University of Dhaka , Dhaka 1000, Bangladesh.
Org Lett. 2013 Dec 6;15(23):6106-9. doi: 10.1021/ol4029995. Epub 2013 Nov 20.
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/β-catenin transcriptional activity (IC50 48.9 nM) and exhibited strong cytotoxicity against colon cancer cell lines. Compound 2 significantly decreased β-catenin protein levels in nuclei but not in the cytosol. These results indicated that a decrease in β-catenin levels in nuclei by 2 resulted in the Wnt signal inhibitory effects of 2.
木菠萝素 B（2）是通过针对 Wnt 信号通路的基于细胞的荧光素酶筛选系统从木菠萝（楝科）叶中分离得到的。化合物 2 抑制 TCF/β-catenin 转录活性（IC50 为 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 显著降低细胞核中 β-catenin 蛋白水平，但不降低细胞质中的 β-catenin 蛋白水平。这些结果表明，2 导致细胞核中 β-catenin 水平降低，从而产生 2 的 Wnt 信号抑制作用。
