Xylogranin B: A Potent Wnt Signal Inhibitory Limonoid from Xylocarpus granatum

被引：31
|
作者：
Toume, Kazufumi [1 ]
Kamiya, Kentaro [1 ]
Arai, Midori A. [1 ]
Mori, Naomi [1 ]
Sadhu, Samir K. [2 ]
Ahmed, Firoj [3 ]
Ishibashi, Masami [1 ]
机构：
[1] Chiba Univ, Grad Sch Pharmaceut Sci, Chuo Ku, Chiba 2608675, Japan
[2] Khulna Univ, Sch Life Sci, Pharm Discipline, Khulna 9208, Bangladesh
[3] Univ Dhaka, Dept Pharmaceut Chem, Dhaka 1000, Bangladesh
来源：
ORGANIC LETTERS | 2013年 / 15卷 / 23期
基金：
日本学术振兴会;
关键词：
CATENIN; STEREOCHEMISTRY; MUTATIONS; DISEASE;
D O I：
10.1021/ol4029995
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
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.
引用
收藏
页码：6106 / 6109
页数：4
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