Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells

	Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells
	Li, Xingyao 1,3; Pu, Jianxin1 ; Jiang, Shiyou 2,3; Su, Jia 1,3; Kong, Lingmei 1,3; Mao, Bingyu 2; Sun, Handong1 ; Li, Yan1
通讯作者	Sun, HD (reprint author), Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming, Peoples R China. ; hdsun@mail.kib.ac.cn ; liyanb@mail.kib.ac.cn
	2013-07-02
发表期刊	PLOS ONE
ISSN	1932-6203
卷号	8 期号:7 页码:e68525
摘要	Aberrant Wnt/beta-catenin signaling has been strongly associated with the tumorigenesis of human colorectal cancer. Inhibitors of this pathway may then offer therapeutic strategies as well as chemoprevention for this malignant disease. Henryin is an ent-kaurane diterpenoid isolated from Isodon rubescens var. lushanensis, a plant long been used in folk medicine to prevent inflammation and gastrointestinal disease. In the present study, we report that henryin selectively inhibits the proliferation of human colorectal cancer cells with a GI(50) value in the nano-molar range. Microarray analysis and reporter assays showed that henryin worked as a novel antagonist of Wnt signaling pathway. Henryin reduced the expression of Cyclin D1 and C-myc, and induced G1/S phase arrest in HCT116 cells. Concurrently, henryin did not affect the cytosol-nuclear distribution of soluble beta-catenin, but impaired the association of beta-catenin/TCF4 transcriptional complex likely through directly blocking the binding of beta-catenin to TCF4. We also then analyzed the structure-activity relationship among the ent-kaurane type diterpenoids. Our data suggests that henryin, as a novel inhibitor of Wnt signaling, could be a potential candidate for further preclinical evaluation for colon cancer treatment, and as such warrants further exploration.
关键词	Beta-catenin Colon-cancer Response Element Activation Expression Pathway Complex Growth Apc Antagonists
学科领域	Multidisciplinary Sciences
收录类别	SCI
语种	英语
WOS记录号	WOS:000321341000169
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/16741
专题	植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming, Peoples R China 2.Chinese Acad Sci, Kunming Inst Zool, State Key Lab Genet Resources & Evolut, Kunming, Peoples R China 3.Univ Chinese Acad Sci, Beijing, Peoples R China
推荐引用方式 GB/T 7714	Li, Xingyao,Pu, Jianxin,Jiang, Shiyou,et al. Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells[J]. PLOS ONE,2013,8(7):e68525.
APA	Li, Xingyao.,Pu, Jianxin.,Jiang, Shiyou.,Su, Jia.,Kong, Lingmei.,...&Li, Yan.(2013).Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells.PLOS ONE,8(7),e68525.
MLA	Li, Xingyao,et al."Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells".PLOS ONE 8.7(2013):e68525.

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