The Estrogenic and Antiestrogenic Activities of Droloxifene in Human Breast Cancers.
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概要
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The effects of a new antiestrogen, droloxifene (DROL, (<I>E</I>)-α-[<I>p</I>-[2-(dimethylamino)ethoxy]-phenyl]-α''-ethyl-3-stilbenol), on human breast cancer cells in vitro and in vivo were studied. Since phenol red has a binding affinity to the estrogen receptor (ER), we studied the activities of drugs in medium with or without this indicator. Estradiol-17β (E<SUB>2</SUB>) stimulated the growth of ER-positive breast cancer cells, MCF-7, ZR-75-1 and T-47D, in medium without phenol red, but not in medium containing this indicator. In medium without phenol red, DROL had no marked effects on the growth of MCF-7 and ZR-75-1, but slightly stimulated the growth of T-47D. Tamoxifen (TAM) stimulated the growth of these 3 cells. DROL dose-dependently inhibited the E<SUB>2</SUB>-induced stimulation of growth of these cells in medium without phenol red, but TAM inhibited the growth only at high concentrations. The growth of ER-negative breast cancer cells, MDA-MB-231, was not influenced by E<SUB>2</SUB>, DROL or TAM. DROL was more effective than TAM against ER-positive Br-10 breast carcinoma in nude mice, but neither drug had effects on ER-negative MX-1 breast carcinoma. These results suggest that DROL shows an antitumor effect on ER-positive breast cancers, being less estrogenic and more antiestrogenic than TAM.
- 公益社団法人 日本薬理学会の論文
著者
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Kawamura Ikuo
Department Of Bacteriology Niigata University School Of Medicine
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Shimomura Kyoichi
Department Of Pharmacology Pharmacological Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Tanaka Yoshio
Department Of Applied Chemistry Faculty Of Engineering Yokohama National University
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MANDA Toshitaka
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo
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Kohsaka Masanobu
Department of Pharmacology, Pharmacological Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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Kohsaka Masanobu
Department of Pharmacology, Product Development Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, Osaka 532, Japan
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Mizota Tamotsu
Department of Pharmacology, Product Development Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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Manda Toshitaka
Department of Pharmacology, Product Development Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, Osaka 532, Japan
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Lacey Elizabeth
Department of Pharmacology, Product Development Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, Osaka 532, Japan
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Kawamura Ikuo
Department of Pharmacology, Product Development Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, Osaka 532, Japan
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