Repression of telomerase reverse transcriptase mRNA and hTERT promoter by gambogic acid in human gastric carcinoma cells

Cancer Chemother Pharmacol. 2006 Oct;58(4):434-43. doi: 10.1007/s00280-005-0177-2. Epub 2006 Feb 10.

Abstract

Objectives: To investigate the effects and potential mechanisms of gambogic acid (GA), a naturally occurring anticancer agent, on the expression and regulation of telomerase in human gastric carcinoma cells.

Methods: GA-induced inhibition of cell proliferation was evaluated by the commonly employed MTT assay on two human gastric carcinoma cell lines, MGC-803 and SGC-7901. Telomerase activity and hTERT mRNA expression were determined by telomeric repeat amplication protocol-polymerase chain reaction and reverse transcription-polymerase chain reaction, respectively. The hTERT promoter activity was measured by luciferase assay. The expression of c-MYC, an apoptotic gene that modulates the expression of hTERT promoter, was quantified by Western blotting.

Results: The proliferation of human gastric carcinoma cell lines, MGC-803 and SGC-7901, was significantly inhibited with GA treatment. Both telomerase activity and hTERT mRNA expression were notably decreased in cells treated with GA. The activity of hTERT promoter and the expression of c-MYC were also remarkably decreased in GA-treated cells.

Conclusion: This study demonstrated that GA treatment of human gastric carcinoma cell lines, MGC-803 and SGC-7901, significantly reduced the expression of c-MYC in a time- and concentration-dependent manner accompanied with the down-regulation of the hTERT transcription and the ultimate reduction in telomerase activity. Our results indicate that the hTERT is a target of c-MYC activity and identify a feasible mechanism of GA's potent anticancer activity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • DNA-Binding Proteins / drug effects*
  • DNA-Binding Proteins / metabolism
  • Down-Regulation
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Peptide Fragments / drug effects*
  • Peptide Fragments / metabolism
  • RNA, Messenger
  • Stomach Neoplasms / enzymology
  • Telomerase / drug effects*
  • Telomerase / metabolism
  • Transcription Factors / drug effects
  • Transcription Factors / metabolism
  • Xanthones / pharmacology*

Substances

  • DNA-Binding Proteins
  • MYCBP protein, human
  • Peptide Fragments
  • RNA, Messenger
  • Transcription Factors
  • Xanthones
  • gambogic acid
  • telomerase reverse transcriptase (540-548)
  • Telomerase