ArticleCancer prevention research (Philadelphia, Pa.)2013
Esculetin suppresses proliferation of human colon cancer cells by directly targeting β-catenin.
Article in Cancer prevention research (Philadelphia, Pa.), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 68 citations in OpenAlex.
- Exploring Natural Coumarins: Breakthroughs in Anticancer Therapeutics.Anti-cancer agents in medicinal chemistry · 2026Review
- Coumarins in Anticancer Therapy: Mechanisms of Action, Potential Applications and Research Perspectives.Pharmaceutics · 2025Review
- Combinatorial Effects of 5-Fluorouracil and Menadione on Wnt/β-Catenin Pathway in Human Colorectal Cancer Cells.Applied biochemistry and biotechnology · 2025Article
- Therapeutic potential of esculetin in various cancer types (Review).Oncology letters · 2024Review
- The possible anti-tumor actions and mechanisms of active metabolites from Cortex Fraxini.Frontiers in pharmacology · 2024Review
- Esculetin unveiled: Decoding its anti-tumor potential through molecular mechanisms-A comprehensive review.Cancer reports (Hoboken, N.J.) · 2024Review
- β-catenin inhibitors in cancer therapeutics: intricacies and way forward.Bioengineered · 2023Review
- Esculetin has therapeutic potential via the proapoptotic signaling pathway in A253 human submandibular salivary gland tumor cells.Experimental and therapeutic medicine · 2022Article
- Post-operative haemorrhage secondary to cinnamon use. A case report.International journal of surgery case reports · 2022Article
- Review
- Review
- Coumarins and Gastrointestinal Cancer: A New Therapeutic Option?Frontiers in oncology · 2021Review
- Emerging impact of the long noncoding RNA MIR22HG on proliferation and apoptosis in multiple human cancers.Journal of experimental & clinical cancer research : CR · 2020Review
- Esculetin Prevents the Induction of Matrix Metalloproteinase-1 by Hydrogen Peroxide in Skin Keratinocytes.Journal of cancer prevention · 2019Article
- Yifei Tongluo, a Chinese Herbal Formula, Suppresses Tumor Growth and Metastasis and Exerts Immunomodulatory Effect in Lewis Lung Carcinoma Mice.Molecules (Basel, Switzerland) · 2019Article
- Novel targeting approaches and signaling pathways of colorectal cancer: An insight.World journal of gastroenterology · 2018Article
- Esculetin Inhibits the Survival of Human Prostate Cancer Cells by Inducing Apoptosis and Arresting the Cell Cycle.Journal of cancer prevention · 2018Article
- WNT Signaling in Cardiac and Vascular Disease.Pharmacological reviews · 2018Review
- Topical administration of Esculetin as a potential therapy for experimental dry eye syndrome.Eye (London, England) · 2017Article
- Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a Natural Haspin Kinase Inhibitor.International journal of molecular sciences · 2017Article
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
Abstract
The Wnt pathway is a promising therapeutic and preventive target in various human cancers. The transcriptional complex of β-catenin-T-cell factor (Tcf), a key mediator of canonical Wnt signaling, has been implicated in human colon cancer development. Current treatment of colon cancer depends on traditional cytotoxic agents with limited effects. Therefore, the identification of natural compounds that can disrupt the β-catenin-TcF complex to suppress cancer cell growth with fewer adverse side effects is needed. To identify compounds that inhibit the association between β-catenin and Tcf, we used computer docking to screen a natural compound library. Esculetin, also known as 6,7-dihydroxycoumarin, is a derivative of coumarin and was identified as a potential small-molecule inhibitor of the Wnt-β-catenin pathway. We then evaluated the effect of esculetin on the growth of various human colon cancer cell lines and its effect on Wnt-β-catenin signaling in cells and in an embryonic model. Esculetin disrupted the formation of the β-catenin-Tcf complex through direct binding with the Lys312, Gly307, Lys345, and Asn387 residues of β-catenin in colon cancer cells. In addition, esculetin effectively decreased viability and inhibited anchorage-independent growth of colon cancer cells. Esculetin potently antagonized the cellular effects of β-catenin-dependent activity, and in vivo treatment with esculetin suppressed tumor growth in a colon cancer xenograft mouse model. Our data indicate that the interaction between esculetin and β-catenin inhibits the formation of the β-catenin-Tcf complex, which could contribute to esculetin's positive therapeutic and preventive effects against colon carcinogenesis.
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