Celastrol downregulates E2F1 to induce growth inhibitory effects in hepatocellular carcinoma HepG2 cells

  • Authors:
    • Liang Ma
    • Lei Peng
    • Sheng Fang
    • Bangguo He
    • Zi Liu
  • View Affiliations

  • Published online on: September 19, 2017     https://doi.org/10.3892/or.2017.5971
  • Pages: 2951-2958
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Abstract

Celastrol, a natural compound extracted from Tripterygium wilfordii, is known to exhibit potential anticancer activities in various types of tumor cells. E2F1 is reported to be overexpressed in several types of human tumors and its inactivation may be a valuable novel potential therapeutic strategy for cancer treatment. However, the molecular mechanism underlying the pro-apoptotic effects of celastrol on hepatocellular carcinoma (HCC) cells remains unclear, and E2F1-targeted compounds have been rarely identified. In the present study, we demonstrated that celastrol inhibited the proliferation of human HCC cells and triggered apoptosis of HepG2 cells in a caspase-dependent manner. E2F1 was potently downregulated by celastrol in a dose- and time-dependent manner at both the mRNA and protein levels. Moreover, siRNA-mediated E2F1 silencing enhanced celastrol-induced apoptosis and inhibition of proliferation. Our data imply that downregulation of E2F1 may be a key factor in the celastrol-mediated inhibitory effects in HepG2 cells, and celastrol can serve as a leading compound for the development of compounds designed to inactivate E2F1 for HCC therapy.
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November-2017
Volume 38 Issue 5

Print ISSN: 1021-335X
Online ISSN:1791-2431

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Spandidos Publications style
Ma L, Peng L, Fang S, He B and Liu Z: Celastrol downregulates E2F1 to induce growth inhibitory effects in hepatocellular carcinoma HepG2 cells. Oncol Rep 38: 2951-2958, 2017
APA
Ma, L., Peng, L., Fang, S., He, B., & Liu, Z. (2017). Celastrol downregulates E2F1 to induce growth inhibitory effects in hepatocellular carcinoma HepG2 cells. Oncology Reports, 38, 2951-2958. https://doi.org/10.3892/or.2017.5971
MLA
Ma, L., Peng, L., Fang, S., He, B., Liu, Z."Celastrol downregulates E2F1 to induce growth inhibitory effects in hepatocellular carcinoma HepG2 cells". Oncology Reports 38.5 (2017): 2951-2958.
Chicago
Ma, L., Peng, L., Fang, S., He, B., Liu, Z."Celastrol downregulates E2F1 to induce growth inhibitory effects in hepatocellular carcinoma HepG2 cells". Oncology Reports 38, no. 5 (2017): 2951-2958. https://doi.org/10.3892/or.2017.5971