Inflammopharmacology

, Volume 16, Issue 5, pp 208–212 | Cite as

Green tea polyphenols as a natural tumour cell proteasome inhibitor

  • Q. P. Dou
  • K. R. Landis-Piwowar
  • D. Chen
  • C. Huo
  • S. B. Wan
  • T. H. Chan
Review

Abstract.

The cancer-preventive effects of green tea and its main constituent (-)-epigallocatechin gallate [(-)-EGCG] are widely supported by results from epidemiological, cell culture, animal and clinical studies although the molecular target has not been well defined. We previously reported that ester bond-containing tea polyphenols, e. g. (-)-EGCG, and their synthetic analogs potently and specifically inhibited the proteasomal activity. Subsequently, we further demonstrated that methylation on green tea polyphenols under physiological conditions decreased their proteasome-inhibitory activity, contributing to decreased cancer-preventive effects of tea consumption. Since (-)-EGCG is unstable under physiological conditions, we also developed the peracetate-protected or prodrug form of (-)-EGCG, Pro-EGCG (1), and shown that Pro-EGCG (1) increases the bioavailability, stability, and proteasome-inhibitory and anticancer activities of (-)-EGCG in human breast cancer cells and xenografts, suggesting its potential use for cancer prevention and treatment.

Keywords:

Tea polyphenols Proteasome inhibitors Molecular target Methylation Prodrug Cancer prevention Chemotherapy 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Copyright information

© Springer 2008

Authors and Affiliations

  • Q. P. Dou
    • 1
  • K. R. Landis-Piwowar
    • 1
  • D. Chen
    • 1
  • C. Huo
    • 2
    • 3
  • S. B. Wan
    • 2
    • 4
  • T. H. Chan
    • 2
    • 3
  1. 1.The Prevention Program, Barbara Ann Karmanos Cancer Institute and Department of Pathology, School of MedicineWayne State UniversityDetroitUSA
  2. 2.Department of Applied Biology and Chemical TechnologyThe Polytechnic University of Hong KongHung HomChina
  3. 3.Department of ChemistryMcGill UniversityMontrealCanada
  4. 4.Key Laboratory of Marine Drug, Ministry of Education, Medical CollegeOcean University of ChinaQingdaoChina

Personalised recommendations