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In vitro and in vivo antitumor effect of 2-methoxyestradiol on human melanoma

✍ Scribed by Judit Dobos; József Tímár; József Bocsi; Zsuzsanna Burián; Katalin Nagy; Gábor Barna; István Peták; Andrea Ladányi

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
462 KB
Volume
112
Category
Article
ISSN
0020-7136

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✦ Synopsis

Abstract

2‐methoxyestradiol (2ME~2~) is an endogenous metabolite of estradiol with estrogen‐receptor‐independent antitumor and antiangiogenic activity. We examined the effects of 2ME~2~ on the cellular proliferation of 8 human melanoma cell lines. We show that 2ME~2~ inhibited cell proliferation by inducing apoptosis and an arrest in the G~2~/M phase, and the mechanism of action involved microtubules, mitochondrial damage and caspase activation. In male SCID mice, 2ME~2~ was effective in reducing primary tumor weight and the number of liver metastases after intrasplenic injection of human melanoma cells. In the metastases, we found a significantly higher rate of apoptotic cells after 2ME~2~ treatment. These findings on the antitumor effect of 2ME~2~ in cell culture as well as in an animal model may have implications for designing alternative treatment options for patients with advanced malignant melanoma. © 2004 Wiley‐Liss, Inc.

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