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

CORC > 昆明植物研究所 > 中国科学院昆明植物研究所 > 植物化学与西部植物资源持续利用国家重点实验室

	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
刊名	PLOS ONE
	2013-07-02
卷号	8 期号:7 页码:e68525
关键词	Beta-catenin Colon-cancer Response Element Activation Expression Pathway Complex Growth Apc Antagonists
ISSN号	1932-6203
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
文献子类	Article
英文摘要	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.
学科主题	Multidisciplinary Sciences
WOS关键词	BETA-CATENIN ; COLON-CANCER ; RESPONSE ELEMENT ; ACTIVATION ; EXPRESSION ; PATHWAY ; COMPLEX ; GROWTH ; APC ; ANTAGONISTS
WOS研究方向	Science & Technology - Other Topics
语种	英语
WOS记录号	WOS:000321341000169
资助机构	100 Talents Program of the Chinese Academy of Sciences; West Light Foundation of the Chinese Academy of Sciences; Major State Basic Research Development Program of China [2009CB522300]; Natural Science Foundation of China [81173076, 81172939]; Recruited Top Talent of Sciences and Technology of Yunnan Province, China [2009C1120]
公开日期	2013-10-16
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn:8080/handle/151853/16741]
专题	昆明植物研究所_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.