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Estrogenic and antiproliferative activities on MCF-7 human breast cancer cells by flavonoids
被引:159
作者:
Le Bail, JC
Varnat, F
Nicolas, JC
Habrioux, G
机构:
[1] Fac Pharm, Biochim Lab, UPRES EA 1085, F-87025 Limoges, France
[2] INSERM, U439, F-34090 Montpellier, France
关键词:
MCF-7;
cells;
estrogen receptor;
flavonoids;
luciferase activity;
D O I:
10.1016/S0304-3835(98)00141-4
中图分类号:
R73 [肿瘤学];
学科分类号:
100214 ;
摘要:
The interaction between the estrogen receptor and a variety of flavonoids was studied in the presence or absence of estradiol using a stably-transfected human boast cancer cell line (MVLN). On the other hand, flavonoids were evaluated for their effects on proliferation in estrogen-dependent (MCF-7) and independent (MDA-MB231) human breast cancer cells. We established a relationship structure-activity and determined regions and/or substituents essential for estrogenic or antiestrogenic activities. In contrast, we did not find the same relationship for cell proliferation. Among all flavonoids used, only 7-methoxyflavanone and 7,8-dihydroxyflavone at high concentrations (50 mu M) possess antiestrogenic and antiproliferative activities. These results suggest that two hydroxyls (in positions 7 and 8) or 7-methoxy substituents are essential for the antiestrogenic activity of flavonoids. However, it seems that flavonoids at high concentrations exert their antiproliferative activity through other estrogen receptor-independent mechanisms. (C) 1998 Elsevier Science Ireland Ltd. All rights reserved.
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页码:209 / 216
页数:8
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