Abstract
2-Methoxyestradiol (2-ME) has been found to possess antitumor activity in vivo and in vitro. It has been suggested that 2-ME induces apoptosis resulting in G2/M arrest of tumor cells. In this study, the effect of 2-ME was evaluated in rat osteosarcoma and malignant fibrous histiocytoma (MFH) cell lines. 2-ME was used at final concentrations of 100 nM to 2 microM. The effect of 2-ME on cell growth was measured by the MTS assay. Induction of apoptosis and activation of caspase-3 were investigated along with apoptosis-related gene expression. The data showed that 2-ME significantly inhibited cell growth, inducing apoptosis. The activity of caspase-3 was increased at 20 h and 40 h in both cell lines. 2-ME induced p16 expression, which was possibly involved in the apoptotic process. These results suggested that the 2-ME-induced apoptosis of rat osteosarcoma and rat MFH cells was accompanied by caspase-3 activation through p16 induction.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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2-Methoxyestradiol
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Animals
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects*
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Caspase 3 / genetics
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Caspase 3 / metabolism
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Cell Line, Tumor
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Cell Survival / drug effects
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Cyclin-Dependent Kinase Inhibitor p16 / genetics
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Cyclin-Dependent Kinase Inhibitor p16 / metabolism
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Estradiol / analogs & derivatives*
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Estradiol / pharmacology
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Gene Expression Regulation, Neoplastic / drug effects
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Histiocytoma, Malignant Fibrous / pathology*
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Indicators and Reagents / metabolism
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Osteosarcoma / pathology*
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RNA, Messenger / metabolism
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RNA, Neoplasm / analysis
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Rats
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Tetrazolium Salts / metabolism
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Tubulin Modulators / pharmacology*
Substances
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Antineoplastic Agents
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Cyclin-Dependent Kinase Inhibitor p16
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Indicators and Reagents
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RNA, Messenger
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RNA, Neoplasm
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Tetrazolium Salts
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Tubulin Modulators
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Estradiol
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2-Methoxyestradiol
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Caspase 3