Potent inhibition of human telomerase by helenalin

Pei Rong Huang, Yuan Ming Yeh, Tzu Chien V. Wang*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

64 Scopus citations

Abstract

Telomerase activity is repressed in normal human somatic cells, but is activated in most cancers, suggesting that telomerase may be an important target for cancer therapy. Inhibition of telomerase in cancer cells has been shown to limit the growth of human cancer cells in culture. In this study, we report that helenalin, a natural sesquiterpene lactone, is a potent and selective inhibitor for human telomerase. In vitro studies indicate that this drug can inactivate telomerase directly in a manner that is dependent on concentration and time. The inhibitory action of this drug on telomerase is selective since the presence of excessive externally added proteins did not protect the inhibition and all of the other enzymes tested in this study were not inhibited by this drug. Furthermore, we demonstrated that helenalin can inhibit the expression of hTERT and telomerase in hematopoietic cancer cells. Therefore, the anti-tumor activity of helenalin is attributed, at least in part, to the inhibition of telomerase.

Original languageEnglish
Pages (from-to)169-174
Number of pages6
JournalCancer Letters
Volume227
Issue number2
DOIs
StatePublished - 28 09 2005

Keywords

  • Cancer therapy
  • Helenalin
  • NF-κB
  • Telomerase inhibitor
  • hTERT

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