Abstract
The present study investigated the effect of the phytochemical genistein on the proliferation and differentiation of MCF-7 and 3T3-L1 cells via the regulation of estrogen receptor-α (ERα) expression and the induction of apoptosis. When MCF-7 human breast cancer cells were treated with 50, 100, 150 and 200 μM genistein for 24, 48 or 72 h, cell growth was significantly decreased in a concentration-dependent manner. Notably, the patterns of ERα expression and proliferation in MCF-7 cells treated with genistein were similar. Furthermore, ERα expression in differentiating 3T3-L1 cells was significantly inhibited by 48 h treatment with 50 μM genistein, which was selected based on the results of cytotoxicity assays on 3T3-L1 preadipocytes [lactate dehydrogenase (LDH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) viability assays]. Under the same conditions, genistein-induced apoptotic features were observed in MCF-7 and differentiating 3T3-L1 cells. This observation is supported by the finding that B-cell lymphoma 2 (Bcl-2) expression was reduced while that of Bcl-2-associated X protein (Bax) was induced by genistein. The results of the present study suggest that an ERα-related pathway and the induction of apoptosis are involved in the proliferation of MCF-7 cells and the differentiation of 3T3-L1 cells.
Highlights
Genistein (4',5,7-trihydroxyisoflavone) is a major isoflavone present in plants, such as soybean, and in a variety of human foods [1,2,3]
To investigate the possible anticancer effects of the phytochemical genistein on MCF-7 human breast cancer cells, the present study initially examined the antiproliferative effects of genistein on MCF-7 cells using various concentrations (50, 100, 150 and 200 μM) of genistein for 24, 48 and 72 h (Fig. 1)
Genistein inhibited the growth of MCF-7 cells in a concentration‐dependent manner and revealed significant antiproliferative activity under all treatment conditions, with the exception of 50 μM for 24 h
Summary
Genistein (4',5,7-trihydroxyisoflavone) is a major isoflavone present in plants, such as soybean, and in a variety of human foods [1,2,3]. In 1987, it was discovered that genistein is a potent inhibitor of the tyrosine-specific protein kinase activity of the epidermal growth factor receptor [4]. Numerous researchers have studied the possible use of. Breast cancer belongs to a group of heterogeneous diseases with multiple clinical, molecular and histopathological forms, which makes achieving effective chemotherapy problematic [12]. To develop breast cancer therapies, the targeting of estrogen receptor-α (ERα), which is expressed in ~70% of breast cancers and which makes it difficult to obtain a response to cancer drug treatment [13,14], requires consideration
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