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
Oncology Reports
Join Editorial Board Propose a Special Issue
Print ISSN: 1021-335X Online ISSN: 1791-2431
Journal Cover
November 2012 Volume 28 Issue 5

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
November 2012 Volume 28 Issue 5

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
Article

Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells

  • Authors:
    • Jie Ren
    • Hong Cheng
    • Wen Qun Xin
    • Xin Chen
    • Kun Hu
  • View Affiliations / Copyright

    Affiliations: School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou, Jiangsu 213164, P.R. China
  • Pages: 1719-1726
    |
    Published online on: September 4, 2012
       https://doi.org/10.3892/or.2012.2016
  • Expand metrics +
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

The antitumor activity of 7-piperazinethylchrysin (7-PEC) was investigated in HCT-116 human colon cancer cells. MTT assay revealed that the IC50 of 7-PEC in HCT-116 cells was 1.5 µM after 72 h of treatment, much lower than that of chrysin (>100 µM). The data showed that 7-PEC was able to inhibit the growth of HCT-116 cells in a concentration- and time-dependent manner. Topical morphological changes of apoptotic body formation after 7-PEC treatment were observed by Hoechst 33258 staining. 7-PEC reduced mitochondrial membrane potential (∆Ψm) of cells in a concentration-dependent manner and increased the production of intracellular reactive oxygen species (ROS). After treatment with 7-PEC, a significant increase of Bax protein expression and decrease of Bcl-2 protein expression were observed at the same time. These events paralleled with activation of p53, caspase-3 and -9 and the release of cytochrome c (cyt‑c), as well as poly(ADP-ribose) polymerase-1 (PARP1) cleavage and downregulation of p-Akt. However, the apoptosis induced by 7-PEC was blocked by Ac-DEVD-CHO, a caspase-3 inhibitor. These results demonstrate that 7-PEC-induced mitochondrial dysfunction in HCT-116 human colon cancer cells triggers events responsible for caspase-dependent apoptosis pathways, and the elevated ratio of Bax/Bcl-2 is likely involved in this effect.
View Figures

Figure 1

Figure 2

Figure 3

Figure 4

Figure 5

Figure 6

View References

1 

Kaufmann SH and Hengartner MO: Programmed cell death: alive and well in the new millennium. Trends Cell Biol. 11:526–534. 2001. View Article : Google Scholar : PubMed/NCBI

2 

Reed JC: Apoptosis-regulating proteins as targets for drug discovery. Trends Mol Med. 7:314–319. 2001. View Article : Google Scholar : PubMed/NCBI

3 

Earnshaw WC, Martins LM and Kaufmann SH: Mammalian caspases: structure, activation, substrates, and functions during apoptosis. Annu Rev Biochem. 68:383–424. 1999. View Article : Google Scholar : PubMed/NCBI

4 

Sun XM, MacFarlane M, Zhuang J, Wolf BB, Green DR and Cohen GM: Distinct caspase cascades are initiated in receptor-mediated and chemical-induced apoptosis. J Biol Chem. 274:5053–5060. 1999. View Article : Google Scholar : PubMed/NCBI

5 

Thompson CB: Apoptosis in the pathogenesis and treatment of disease. Science. 267:1456–1462. 1995. View Article : Google Scholar : PubMed/NCBI

6 

Lee KH: Anticancer drug design based on plant-derived natural products. J Biomed Sci. 6:236–250. 1999.PubMed/NCBI

7 

Arts IC: A review of the epidemiological evidence on tea, flavonoids, and lung cancer. J Nutr. 138:S1561–S1566. 2008.PubMed/NCBI

8 

Kupeli E, Sahin FP, Yesilada E, Calis I and Ezer N: In vivo anti-inflammatory and antinociceptive activity evaluation of phenolic compounds from Sideritis stricta. J Biosci. 62:519–525. 2007.PubMed/NCBI

9 

Terao J: Dietary flavonoids as antioxidants. Forum Nutr. 61:87–94. 2009. View Article : Google Scholar

10 

Sobocanec S, Sverko V, Balog T, et al: Oxidant/antioxidant properties of Croatian native propolis. J Agric Food Chem. 54:8018–8026. 2006. View Article : Google Scholar : PubMed/NCBI

11 

Dhawan K, Kumar S and Sharma A: Beneficial effects of chrysin and benzoflavone on virility in 2-year-old male rats. J Med Food. 5:43–48. 2002.PubMed/NCBI

12 

Lapidot T, Walker MD and Kanner J: Antioxidant and prooxidant effects of phenolics on pancreatic beta-cells in vitro. J Agric Food Chem. 50:7220–7225. 2002. View Article : Google Scholar : PubMed/NCBI

13 

Schnitzler P, Neuner A, Nolkem per S, Zundel C, Nowack H, Sensch KH and Reichling J: Antiviral activity and mode of action of propolis extracts and selected compounds. Phytother Res. 24:S20–S28. 2010. View Article : Google Scholar : PubMed/NCBI

14 

Khoo BY, Chua SL and Balaram P: Apoptotic effects of chrysin in human cancer cell lines. Int J Mol Sci. 11:2188–2199. 2010. View Article : Google Scholar : PubMed/NCBI

15 

Weng MS, Ho YS and Lin JK: Chrysin induces G1 phase cell cycle arrest in C6 glioma cells through inducing p21Waf1/Cip1 expression: involvement of p38 mitogen-activated protein kinase. Biochem Pharmacol. 69:1815–1827. 2005. View Article : Google Scholar : PubMed/NCBI

16 

Li X, Huang Q, Ong CN, Yang XF and Shen HM: Chrysin sensitizes tumor necrosis factor-alpha-induced apoptosis in human tumor cells via suppression of nuclear factor-kappaB. Cancer Lett. 293:109–116. 2010. View Article : Google Scholar : PubMed/NCBI

17 

Hu K, Wang W, Cheng H, Pan SS and Ren J: Synthesis and cytotoxicity of novel chrysin derivatives. Med Chem Res. 20:838–846. 2011. View Article : Google Scholar

18 

Thornberry NA and Lazebnik Y: Caspase: enemies within. Science. 281:1308–1312. 1998. View Article : Google Scholar

19 

Choi BH, Kim W, Wang QC, et al: Kinetin riboside preferentially induces apoptosis by modulating Bcl-2 family proteins and caspase-3 in cancer cells. Cancer Lett. 261:37–45. 2008. View Article : Google Scholar : PubMed/NCBI

20 

Ly JD, Grubb DR and Lawen A: The mitochondrial membrane potential (deltapsi(m)) in apoptosis; an update. Apoptosis. 8:115–128. 2003. View Article : Google Scholar : PubMed/NCBI

21 

Zhou PH, Liu SQ and Peng H: The effect of hyaluronic acid on IL-1beta-induced chondrocyte apoptosis in a rat model of osteoarthritis. J Orthop Res. 26:1643–1648. 2008. View Article : Google Scholar : PubMed/NCBI

22 

Ling YH, Liebes L, Zou Y and Perez-Soler R: Reactive oxygen species generation and mitochondrial dysfunction in the apoptotic response to Bortezomib, a novel proteasome inhibitor, in human H460 non-small cell lung cancer cells. Biol Chem. 278:33714–33723. 2003. View Article : Google Scholar : PubMed/NCBI

23 

Ryan L, O’Callaghan YC and O’Brien NM: The role of the mitochondria in apoptosis induced by 7β-hydroxycholesterol and cholesterol-5β, 6β-epoxide. Br J Nutr. 94:519–525. 2005.

24 

Tang L and Zhang Y: Mitochondria are the primary target in isothiocyanate-induced apoptosis in human bladder cancer cells. Mol Cancer Ther. 4:1250–1259. 2005. View Article : Google Scholar : PubMed/NCBI

25 

Doi S, Soda H, Oka M, et al: The histone deacetylase inhibitor FR901228 induces caspase-dependent apoptosis via the mitochondrial pathway in small cell lung cancer cells. Mol Cancer Ther. 3:1397–1402. 2003.PubMed/NCBI

26 

Ogbourne SM, Suhrbier A, Jones B, et al: Antitumor activity of 3-ingenylangelate: plasma membrane and mitochondrial disruption and necrotic cell death. Cancer Res. 64:2833–2839. 2004. View Article : Google Scholar : PubMed/NCBI

27 

Rotem R, Heyfets A, Fingrut O, Blickstein D, Shaklai M and Flescher E: Jasmonates: novel anticancer agents acting directly and selectively on human cancer cell mitochondria. Cancer Res. 65:1984–1993. 2005. View Article : Google Scholar : PubMed/NCBI

28 

Wu CC, Chan ML, Chen WY, Tsai CY, Chang FR and Wu YC: Pristimerin induces caspase-dependent apoptosis in MDA-MB-231 cells via direct effects on mitochondria. Mol Cancer Ther. 4:1277–1285. 2005. View Article : Google Scholar : PubMed/NCBI

29 

Franke TF, Hornik CP, Segev L, Shostak GA and Sugimoto C: PI3K/Akt and apoptosis: size matters. Oncogene. 22:8983–8998. 2003. View Article : Google Scholar : PubMed/NCBI

30 

Panka DJ, Mano T, Suhara T, Walsh K and Mier JW: Phosphatidylinositol 3-kinase/Akt activity regulates c-FLIP expression in tumor cells. J Biol Chem. 276:6893–6896. 2001. View Article : Google Scholar : PubMed/NCBI

31 

Hayward RL, Macpherson JS, Cummings J, Monia BP, Smyth JF and Jodrell DI: Enhanced oxaliplatin-induced apoptosis following antisense Bcl-xl down-regulation is p53 and Bax dependent: genetic evidence for specificity of the antisense effect. Mol Cancer Ther. 3:169–178. 2004.

32 

Sinicrope FA and Penington RC: Sulindac sulfide-induced apoptosis is enhanced by a small-molecule Bcl-2 inhibitor and by TRAIL in human colon cancer cells over-expressing Bcl-2. Mol Cancer Ther. 4:1475–1483. 2005. View Article : Google Scholar : PubMed/NCBI

33 

Yamanaka K, Rocchi P, Miyake H, Fazli L, Vessella B, Zangemeister-Wittke U and Gleave ME: A novel antisense oligonucleotide inhibiting several antiapoptotic Bcl-2 family members induces apoptosis and enhances chemosensitivity in androgen-independent human prostate cancer PC3 cells. Mol Cancer Ther. 4:1689–1698. 2005. View Article : Google Scholar

34 

Childs AC, Phaneuf SL, Dirks AJ, Phillips T and Leeuwenburgh C: Doxorubicin treatment in vivo causes cytochrome C release and cardiomyocyte apoptosis, as well as increased mitochondrial efficiency, superoxide dismutase activity, and Bcl-2/Bax ratio. Cancer Res. 62:4592–4598. 2002.

35 

Katiyar SK, Roy AM and Baliga MS: Silymarin induces apoptosis primarily through a p53-dependent pathway involving Bcl-2/Bax, cytochrome c release, and caspase activation. Mol Cancer Ther. 4:207–216. 2005.PubMed/NCBI

36 

Batra S, Reynolds CP and Maurer BJ: Fenretinide cytotoxicity for Ewing’s sarcoma and primitive neuroectodermal tumor cell lines is decreased by hypoxia and synergistically enhanced by ceramide modulators. Cancer Res. 64:5415–5424. 2004.

37 

Wang CC, Liu TY, Cheng CH and Jan TR: Involvement of the mitochondrion-dependent pathway and oxidative stress in the apoptosis of murine splenocytes induced by areca nut extract. Toxicol In Vitro. 23:840–847. 2009. View Article : Google Scholar : PubMed/NCBI

38 

Xiao D, Powolny AA, Antosiewicz J, et al: Cellular responses to cancer chemopreventive agent D,L-sulforaphane in human prostate cancer cells are initiated by mitochondrial reactive oxygen species. Pharm Res. 26:1729–1738. 2009. View Article : Google Scholar : PubMed/NCBI

39 

Zhang H, Kong X, Kang J, Su J, Li Y, Zhong J and Sun L: Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 110:376–388. 2009. View Article : Google Scholar : PubMed/NCBI

Related Articles

  • Abstract
  • View
  • Download
  • Twitter
Copy and paste a formatted citation
Spandidos Publications style
Ren J, Cheng H, Xin WQ, Chen X and Hu K: Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells. Oncol Rep 28: 1719-1726, 2012.
APA
Ren, J., Cheng, H., Xin, W.Q., Chen, X., & Hu, K. (2012). Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells. Oncology Reports, 28, 1719-1726. https://doi.org/10.3892/or.2012.2016
MLA
Ren, J., Cheng, H., Xin, W. Q., Chen, X., Hu, K."Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells". Oncology Reports 28.5 (2012): 1719-1726.
Chicago
Ren, J., Cheng, H., Xin, W. Q., Chen, X., Hu, K."Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells". Oncology Reports 28, no. 5 (2012): 1719-1726. https://doi.org/10.3892/or.2012.2016
Copy and paste a formatted citation
x
Spandidos Publications style
Ren J, Cheng H, Xin WQ, Chen X and Hu K: Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells. Oncol Rep 28: 1719-1726, 2012.
APA
Ren, J., Cheng, H., Xin, W.Q., Chen, X., & Hu, K. (2012). Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells. Oncology Reports, 28, 1719-1726. https://doi.org/10.3892/or.2012.2016
MLA
Ren, J., Cheng, H., Xin, W. Q., Chen, X., Hu, K."Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells". Oncology Reports 28.5 (2012): 1719-1726.
Chicago
Ren, J., Cheng, H., Xin, W. Q., Chen, X., Hu, K."Induction of apoptosis by 7-piperazinethylchrysin in HCT-116 human colon cancer cells". Oncology Reports 28, no. 5 (2012): 1719-1726. https://doi.org/10.3892/or.2012.2016
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