Spandidos Publications Logo
  • About
    • About Spandidos
    • Aims and Scopes
    • Abstracting and Indexing
    • Editorial Policies
    • Reprints and Permissions
    • Job Opportunities
    • Terms and Conditions
    • Contact
  • Journals
    • All Journals
    • Oncology Letters
      • Oncology Letters
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Oncology
      • International Journal of Oncology
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Molecular and Clinical Oncology
      • Molecular and Clinical Oncology
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Experimental and Therapeutic Medicine
      • Experimental and Therapeutic Medicine
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Molecular Medicine
      • International Journal of Molecular Medicine
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Biomedical Reports
      • Biomedical Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Oncology Reports
      • Oncology Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Molecular Medicine Reports
      • Molecular Medicine Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • World Academy of Sciences Journal
      • World Academy of Sciences Journal
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Functional Nutrition
      • International Journal of Functional Nutrition
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Epigenetics
      • International Journal of Epigenetics
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Medicine International
      • Medicine International
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
  • Articles
  • Information
    • Information for Authors
    • Information for Reviewers
    • Information for Librarians
    • Information for Advertisers
    • Conferences
  • Language Editing
Spandidos Publications Logo
  • About
    • About Spandidos
    • Aims and Scopes
    • Abstracting and Indexing
    • Editorial Policies
    • Reprints and Permissions
    • Job Opportunities
    • Terms and Conditions
    • Contact
  • Journals
    • All Journals
    • Biomedical Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Experimental and Therapeutic Medicine
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Epigenetics
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Functional Nutrition
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Molecular Medicine
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • International Journal of Oncology
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Medicine International
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Molecular and Clinical Oncology
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Molecular Medicine Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Oncology Letters
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • Oncology Reports
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
    • World Academy of Sciences Journal
      • Information for Authors
      • Editorial Policies
      • Editorial Board
      • Aims and Scope
      • Abstracting and Indexing
      • Bibliographic Information
      • Archive
  • Articles
  • Information
    • For Authors
    • For Reviewers
    • For Librarians
    • For Advertisers
    • Conferences
  • Language Editing
Login Register Submit
  • This site uses cookies
  • You can change your cookie settings at any time by following the instructions in our Cookie Policy. To find out more, you may read our Privacy Policy.

    I agree
Search articles by DOI, keyword, author or affiliation
Search
Advanced Search
presentation
Molecular and Clinical Oncology
Join Editorial Board Propose a Special Issue
Print ISSN: 2049-9450 Online ISSN: 2049-9469
Journal Cover
March-April 2013 Volume 1 Issue 2

Full Size Image

Sign up for eToc alerts
Recommend to Library

Journals

International Journal of Molecular Medicine

International Journal of Molecular Medicine

International Journal of Molecular Medicine is an international journal devoted to molecular mechanisms of human disease.

International Journal of Oncology

International Journal of Oncology

International Journal of Oncology is an international journal devoted to oncology research and cancer treatment.

Molecular Medicine Reports

Molecular Medicine Reports

Covers molecular medicine topics such as pharmacology, pathology, genetics, neuroscience, infectious diseases, molecular cardiology, and molecular surgery.

Oncology Reports

Oncology Reports

Oncology Reports is an international journal devoted to fundamental and applied research in Oncology.

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine is an international journal devoted to laboratory and clinical medicine.

Oncology Letters

Oncology Letters

Oncology Letters is an international journal devoted to Experimental and Clinical Oncology.

Biomedical Reports

Biomedical Reports

Explores a wide range of biological and medical fields, including pharmacology, genetics, microbiology, neuroscience, and molecular cardiology.

Molecular and Clinical Oncology

Molecular and Clinical Oncology

International journal addressing all aspects of oncology research, from tumorigenesis and oncogenes to chemotherapy and metastasis.

World Academy of Sciences Journal

World Academy of Sciences Journal

Multidisciplinary open-access journal spanning biochemistry, genetics, neuroscience, environmental health, and synthetic biology.

International Journal of Functional Nutrition

International Journal of Functional Nutrition

Open-access journal combining biochemistry, pharmacology, immunology, and genetics to advance health through functional nutrition.

International Journal of Epigenetics

International Journal of Epigenetics

Publishes open-access research on using epigenetics to advance understanding and treatment of human disease.

Medicine International

Medicine International

An International Open Access Journal Devoted to General Medicine.

Journal Cover
March-April 2013 Volume 1 Issue 2

Full Size Image

Sign up for eToc alerts
Recommend to Library

  • Article
  • Citations
    • Cite This Article
    • Download Citation
    • Create Citation Alert
    • Remove Citation Alert
    • Cited By
  • Similar Articles
    • Related Articles (in Spandidos Publications)
    • Similar Articles (Google Scholar)
    • Similar Articles (PubMed)
  • Download PDF
  • Download XML
  • View XML
Review

Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review)

  • Authors:
    • Ying Wang
    • Wenli Ma
    • Wenling Zheng
  • View Affiliations

    Affiliations: Institute of Genetic Engineering, Southern Medical University, Tonghe, Guangzhou 510515, P.R. China
  • Published online on: October 18, 2012     https://doi.org/10.3892/mco.2012.36
  • Pages: 215-219
Metrics: Total Views: 0 (Spandidos Publications: | PMC Statistics: )
Metrics: Total PDF Downloads: 0 (Spandidos Publications: | PMC Statistics: )
Cited By (CrossRef): 0 citations Loading Articles...

This article is mentioned in:



Abstract

Deguelin is a natural compound of the flavonoid family products isolated from Derris trifoliata Lour. or Mundulea sericea (Leguminosae). It exhibited significant anti-tumorigenesis and anti-proliferative activity in various types of cancer both in vitro and in vivo. Deguelin induced cell apoptosis by blocking anti-apoptotic pathways, such as PI3K-Akt, IKK-IκBα-NF-κB and AMPK-mTOR-survivin, while inhibiting tumor cell propagation and malignant transformation through p27-cyclinE-pRb-E2F1 cell cycle control and HIF-1α-VEGF anti-angiogenic pathways. In pre-clinical trials, deguelin markedly decreased the tumor incidence. These biological findings identified deguelin as a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention and chemotherapy.
View Figures

Figure 1

Figure 2

View References

1 

Yoshitani SI, Tanaka T, Kohno H and Takashima S: Chemoprevention of azoxymethane-induced rat colon carcinogenesis by dietary capsaicin and rotenone. Int J Oncol. 19:929–939. 2001.PubMed/NCBI

2 

Thamilselvan V, Menon M and Thamilselvan S: Anticancer efficacy of deguelin in human prostate cancer cells targeting glycogen synthase kinase-3 beta/beta-catenin pathway. Int J Cancer. 129:2916–2927. 2011. View Article : Google Scholar : PubMed/NCBI

3 

Matsuda H, Yoshida K, Miyagawa K, et al: Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa. Bioorg Med Chem. 15:1539–1546. 2007. View Article : Google Scholar : PubMed/NCBI

4 

Mulcahy P, O’Doherty A, Paucard A, O’Brien T, Kirik D and Dowd E: Development and characterisation of a novel rat model of Parkinson’s disease induced by sequential intranigral administration of AAV-α-synuclein and the pesticide, rotenone. Neuroscience. 203:170–179. 2012.PubMed/NCBI

5 

Udeani GO, Gerhauser C, Thomas CF, et al: Cancer chemo-preventive activity mediated by deguelin, a naturally occurring rotenoid. Cancer Res. 57:3424–3428. 1997.PubMed/NCBI

6 

Gills JJ, Kosmeder J II, Moon RC, Lantvit DD and Pezzuto JM: Effect of deguelin on UVB-induced skin carcinogenesis. J Chemother. 17:297–301. 2005. View Article : Google Scholar : PubMed/NCBI

7 

Yan Y, Wang Y, Tan Q, Lubet RA and You M: Efficacy of deguelin and silibinin on benzo(a)pyrene-induced lung tumorigenesis in A/J mice. Neoplasia. 7:1053–1057. 2005. View Article : Google Scholar : PubMed/NCBI

8 

Lee HY, Oh SH, Woo JK, et al: Chemopreventive effects of deguelin, a novel Akt inhibitor, on tobacco-induced lung tumorigenesis. J Natl Cancer Inst. 97:1695–1699. 2005. View Article : Google Scholar : PubMed/NCBI

9 

Long JS and Ryan KM: New frontiers in promoting tumour cell death: targeting apoptosis, necroptosis and autophagy. Oncogene. Feb 6–2012.(Epub ahead of print).

10 

Chun KH, Kosmeder JW II, Sun S, et al: Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells. J Natl Cancer Inst. 95:291–302. 2003. View Article : Google Scholar : PubMed/NCBI

11 

Chen Y, Wu Q, Cui GH, Chen YQ and Li R: Deguelin blocks cells survival signal pathways and induces apoptosis of HL-60 cells in vitro. Int J Hematol. 89:618–623. 2009. View Article : Google Scholar : PubMed/NCBI

12 

Bortul R, Tazzari PL, Billi AM, et al: Deguelin, A PI3K/AKT inhibitor, enhances chemosensitivity of leukaemia cells with an active PI3K/AKT pathway. Br J Haematol. 129:677–686. 2005. View Article : Google Scholar : PubMed/NCBI

13 

Chu ZH, Liang XH, Zhou XL, Huang RF, Zhan Q and Jiang JW: Effects of deguelin on proliferation and apoptosis of MCF-7 breast cancer cells by phosphatidylinositol 3-kinase/Akt signaling pathway. Zhong Xi Yi Jie He Xue Bao. 9:533–538. 2011.(In Chinese).

14 

Lee HY: Molecular mechanisms of deguelin-induced apoptosis in transformed human bronchial epithelial cells. Biochem Pharmacol. 68:1119–1124. 2004. View Article : Google Scholar : PubMed/NCBI

15 

Li R, Chen Y, Shu WX, Chen Z and Ke WJ: Involvement of SRC-3 in deguelin-induced apoptosis in Jurkat cells. Int J Hematol. 89:628–635. 2009. View Article : Google Scholar : PubMed/NCBI

16 

Nair AS, Shishodia S, Ahn KS, Kunnumakkara AB, Sethi G and Aggarwal BB: Deguelin, an Akt inhibitor, suppresses IkappaBalpha kinase activation leading to suppression of NF-kappaB-regulated gene expression, potentiation of apoptosis, and inhibition of cellular invasion. J Immunol. 177:5612–5622. 2006. View Article : Google Scholar

17 

Dat NT, Lee JH, Lee K, Hong YS, Kim YH and Lee JJ: Phenolic constituents of Amorpha fruticosa that inhibit NF-kappaB activation and related gene expression. J Nat Prod. 71:1696–1700. 2008.PubMed/NCBI

18 

Geeraerts B, Vanhoecke B, Vanden Berghe W, Philippe J, Offner F and Deforce D: Deguelin inhibits expression of IkappaBalpha protein and induces apoptosis of B-CLL cells in vitro. Leukemia. 21:1610–1618. 2007. View Article : Google Scholar : PubMed/NCBI

19 

Chen WH, Chen Y and Cui GH: Deguelin inhibits expression of IkappaBalpha protein in Raji and U937 cells. Acta Pharmacol Sin. 27:485–490. 2006. View Article : Google Scholar : PubMed/NCBI

20 

Dell’Eva R, Ambrosini C, Minghelli S, Noonan DM, Albini A and Ferrari N: The Akt inhibitor deguelin, is an angiopreventive agent also acting on the NF-kappaB pathway. Carcinogenesis. 28:404–413. 2007.PubMed/NCBI

21 

Jin Q, Feng L, Behrens C, et al: Implication of AMP-activated protein kinase and Akt-regulated survivin in lung cancer chemopreventive activities of deguelin. Cancer Res. 67:11630–11639. 2007. View Article : Google Scholar : PubMed/NCBI

22 

Xiang X, Saha AK, Wen R, Ruderman NB and Luo Z: AMP-activated protein kinase activators can inhibit the growth of prostate cancer cells by multiple mechanisms. Biochem Biophys Res Commun. 321:161–167. 2004. View Article : Google Scholar : PubMed/NCBI

23 

Cao C, Lu S, Kivlin R, et al: AMP-activated protein kinase contributes to UV- and H2O2-induced apoptosis in human skin keratinocytes. J Biol Chem. 283:28897–28908. 2008. View Article : Google Scholar : PubMed/NCBI

24 

Okoshi R, Ozaki T, Yamamoto H, et al: Activation of AMP-activated protein kinase induces p53-dependent apoptotic cell death in response to energetic stress. J Biol Chem. 283:3979–3987. 2008. View Article : Google Scholar : PubMed/NCBI

25 

Zheng QY, Jin FS, Yao C, Zhang T, Zhang GH and Ai X: Ursolic acid-induced AMP-activated protein kinase (AMPK) activation contributes to growth inhibition and apoptosis in human bladder cancer T24 cells. Biochem Biophys Res Commun. 419:741–747. 2012. View Article : Google Scholar : PubMed/NCBI

26 

Chen MB, Shen WX, Yang Y, Wu XY, Gu JH and Lu PH: Activation of AMP-activated protein kinase is involved in vincristine-induced cell apoptosis in B16 melanoma cell. J Cell Physiol. 226:1915–1925. 2011. View Article : Google Scholar : PubMed/NCBI

27 

Murillo G, Salti GI, Kosmeder JW II, Pezzuto JM and Mehta RG: Deguelin inhibits the growth of colon cancer cells through the induction of apoptosis and cell cycle arrest. Eur J Cancer. 38:2446–2454. 2002. View Article : Google Scholar : PubMed/NCBI

28 

Lee HY, Suh YA, Kosmeder JW, Pezzuto JM, Hong WK and Kurie JM: Deguelin-induced inhibition of cyclooxygenase-2 expression in human bronchial epithelial cells. Clin Cancer Res. 10:1074–1079. 2004. View Article : Google Scholar : PubMed/NCBI

29 

Murillo G, Peng X, Torres KE and Mehta RG: Deguelin inhibits growth of breast cancer cells by modulating the expression of key members of the Wnt signaling pathway. Cancer Prev Res (Phila). 2:942–950. 2009. View Article : Google Scholar : PubMed/NCBI

30 

Liu HL, Chen Y, Cui GH, Wu QL, Chen WH and He J: Effect of deguelin on proliferation and apoptosis of lymphoma Daudi cells and its mechanism. Zhonghua Zhong Liu Za Zhi. 29:176–180. 2007.(In Chinese).

31 

Oh SH, Woo JK, Jin Q, et al: Identification of novel antiangiogenic anticancer activities of deguelin targeting hypoxia-inducible factor-1 alpha. Int J Cancer. 122:5–14. 2008. View Article : Google Scholar : PubMed/NCBI

32 

Oh SH, Woo JK, Yazici YD, et al: Structural basis for depletion of heat shock protein 90 client proteins by deguelin. J Natl Cancer Inst. 99:949–961. 2007. View Article : Google Scholar : PubMed/NCBI

33 

Kim WY, Oh SH, Woo JK, Hong WK and Lee HY: Targeting heat shock protein 90 overrides the resistance of lung cancer cells by blocking radiation-induced stabilization of hypoxia-inducible factor-1alpha. Cancer Res. 69:1624–1632. 2009. View Article : Google Scholar : PubMed/NCBI

34 

Caboni P, Sherer TB, Zhang N, et al: Rotenone, deguelin, their metabolites, and the rat model of Parkinson’s disease. Chem Res Toxicol. 17:1540–1548. 2004.PubMed/NCBI

35 

Kim WY, Chang DJ, Hennessy B, et al: A novel derivative of the natural agent deguelin for cancer chemoprevention and therapy. Cancer Prev Res (Phila). 1:577–587. 2008. View Article : Google Scholar : PubMed/NCBI

36 

Greenamyre JT, Cannon JR, Drolet R and Mastroberardino PG: Lessons from the rotenone model of Parkinson’s disease. Trends Pharmacol Sci. 31:141–143. 2010.PubMed/NCBI

37 

Banerji U, O’Donnell A, Scurr M, et al: Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies. J Clin Oncol. 23:4152–4161. 2005. View Article : Google Scholar : PubMed/NCBI

38 

Grem JL, Morrison G, Guo XD, et al: Phase I and pharmacologic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with solid tumors. J Clin Oncol. 23:1885–1893. 2005. View Article : Google Scholar : PubMed/NCBI

Related Articles

  • Abstract
  • View
  • Download
  • Twitter
Copy and paste a formatted citation
Spandidos Publications style
Wang Y, Ma W and Zheng W: Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review). Mol Clin Oncol 1: 215-219, 2013.
APA
Wang, Y., Ma, W., & Zheng, W. (2013). Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review). Molecular and Clinical Oncology, 1, 215-219. https://doi.org/10.3892/mco.2012.36
MLA
Wang, Y., Ma, W., Zheng, W."Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review)". Molecular and Clinical Oncology 1.2 (2013): 215-219.
Chicago
Wang, Y., Ma, W., Zheng, W."Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review)". Molecular and Clinical Oncology 1, no. 2 (2013): 215-219. https://doi.org/10.3892/mco.2012.36
Copy and paste a formatted citation
x
Spandidos Publications style
Wang Y, Ma W and Zheng W: Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review). Mol Clin Oncol 1: 215-219, 2013.
APA
Wang, Y., Ma, W., & Zheng, W. (2013). Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review). Molecular and Clinical Oncology, 1, 215-219. https://doi.org/10.3892/mco.2012.36
MLA
Wang, Y., Ma, W., Zheng, W."Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review)". Molecular and Clinical Oncology 1.2 (2013): 215-219.
Chicago
Wang, Y., Ma, W., Zheng, W."Deguelin, a novel anti-tumorigenic agent targeting apoptosis, cell cycle arrest and anti-angiogenesis for cancer chemoprevention (Review)". Molecular and Clinical Oncology 1, no. 2 (2013): 215-219. https://doi.org/10.3892/mco.2012.36
Follow us
  • Twitter
  • LinkedIn
  • Facebook
About
  • Spandidos Publications
  • Careers
  • Cookie Policy
  • Privacy Policy
How can we help?
  • Help
  • Live Chat
  • Contact
  • Email to our Support Team