Micromolar concentrations of 2-methoxyestradiol kill glioma cells by an apoptotic mechanism, without destroying their microtubule cytoskeleton

K. Chamaon, J. Stojek, D. Kanakis, S. Braeuninger, Elmar Kirches, G. Krause, C. Mawrin, K. Dietzmann

Research output: Contribution to journalArticlepeer-review

Abstract

The purpose of this study was to investigate the potential effects of 2-methoxyestradiol, a natural mammalian steroid, in glioma cells, since antiproliferative effects of this compound had been shown earlier in several leukemia and carcinoma cell lines. The effects of 0.2, 2 and 20μM concentrations of 2-methoxyestradiol were measured in three malignant human glioma cell lines (U87MG, U138MG, LN405) and one malignant rat glioma cell line (RG-2) using a microtiter-tetrazolium (MTT) assay. In all cell lines, a significant reduction of the viable cell number by more then 75% occurred (P < 0.05) for concentrations of 2 and 20μM 2-methoxyestradiol after 6 days. A concentration of 0.2 μM had smaller effects (10-40% cell reduction), which were significant in two of the cell lines tested. The apoptotic nature of cell death was further analyzed in U87MG and RG-2 cells. Caspase-3 activity was significantly induced to levels between 3.4- and 23-fold after 4 days for the two higher 2-methoxyestradiol concentrations (P < 0.05). In the cell line RG-2 nuclear fragmentation was visible in many nuclei, following stains with Hoechst H33258. A round cell morphology occurred in most treated cells, which was not accompanied by a complete destruction of the microtubule network, as it can be observed with other microtubule targeting drugs.

Original languageEnglish
Pages (from-to)11-16
Number of pages6
JournalJournal of Neuro-Oncology
Volume72
Issue number1
DOIs
Publication statusPublished - Mar 2005

Keywords

  • 2-methoxyestradiol
  • Glioblastoma
  • Glioma
  • Microtiter-tetrazolium assay
  • Microtubules
  • Proliferation

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