2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether induces growth inhibition and apoptosis in MCF-7 human breast cancer cells

Arch Pharm Res. 2007 Sep;30(9):1132-7. doi: 10.1007/BF02980248.

Abstract

In this study, we investigated the effects of 2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether (TDB), isolated from Symphyocladia latiuscula (marine red algae), on the proliferation of MCF-7 human breast cancer cells. TDB treatment for 48 h inhibited cancer cell growth and induced DNA fragmentation. Furthermore, morphological characterizations such as apoptotic bodies and membrane blebs were shown by electronic microscopy. TDB-induced apoptosis in the MCF-7 cells was closely linked with the down-regulation of Bcl-2 protein expression and the cleavage of caspase-3 substrates, with poly(ADP-ribose) polymerase cleavage occurring by TDB treatment. TDB treatment also caused a marked increase in the level of p21WAF1/CIP1 protein in a p53-dependent manner. In addition, the upregulation of p21WAF1/CIP1 in the MCF-7 cells was related to a decrease in c-Myc protein in a dose-dependent manner. Based on our data, TDB is a good candidate for further evaluation as an effective chemotherapeutic agent, acting through the induction of apoptosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cyclin-Dependent Kinase Inhibitor p21 / analysis
  • Ethers / pharmacology*
  • Female
  • Humans
  • Proto-Oncogene Proteins c-bcl-2 / analysis
  • Proto-Oncogene Proteins c-jun / analysis
  • Tumor Suppressor Protein p53 / analysis
  • Tumor Suppressor Protein p53 / physiology

Substances

  • 2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether
  • Antineoplastic Agents
  • CDKN1A protein, human
  • Cyclin-Dependent Kinase Inhibitor p21
  • Ethers
  • Proto-Oncogene Proteins c-bcl-2
  • Proto-Oncogene Proteins c-jun
  • Tumor Suppressor Protein p53