Henryin, an ent-kaurane Diterpenoid, Inhibits Wnt Signaling through Interference with beta-Catenin/TCF4 Interaction in Colorectal Cancer Cells
Li, Xingyao1,3; Pu, Jianxin1; Jiang, Shiyou2,3; Su, Jia1,3; Kong, Lingmei1,3; Mao, Bingyu2; Sun, Handong1; Li, Yan1
Corresponding AuthorSun, 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
Source PublicationPLOS ONE
ISSN1932-6203
Volume8Issue:7Pages:e68525
AbstractAberrant 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.
KeywordBeta-catenin Colon-cancer Response Element Activation Expression Pathway Complex Growth Apc Antagonists
Subject AreaMultidisciplinary Sciences
Indexed BySCI
Language英语
WOS Research AreaScience & Technology - Other Topics
WOS SubjectMultidisciplinary Sciences
WOS IDWOS:000321341000169
Citation statistics
Cited Times:20[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/16741
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.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
Recommended Citation
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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