Inhibition of estrogenic stimulation of gene expression by genistein

Ratna, Warren N

doi:10.1016/s0024-3205(02)01770-8

Cited by 36 publications

(23 citation statements)

References 31 publications

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“…In vivo, phytoestrogens may also compete with estrogen for binding to ER or interfere with key enzymes of the hormonal metabolism [5]. Thus, the hormonal environment is likely to be important; indeed, genistein has been reported to behave as a partial agonist by itself, and as an antagonist in the presence of estrogen [70].…”

Section: Discussionmentioning

confidence: 99%

Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha

Seo

DeNardo

Jacquot

et al. 2006

Breast Cancer Res Treat

115

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Genistein and apigenin are phytoestrogens present in commercial preparations used for the treatment of postmenopausal symptoms. In this study, we assessed the influence of these compounds on mammary tumor growth. Both compounds stimulate the proliferation of MCF-7 and T47D cells [estrogen receptor alpha (ERalpha-positive)], but do not stimulate the proliferation of an ERalpha-negative cell line (MDA-MB-435 cells). Genistein appeared more efficient in this regard due to its higher binding affinity for ERalpha, a property explained by a structural analysis of the binding of these compounds to the ERalpha's ligand binding domain. As previously described for estradiol (E(2)), genistein and apigenin down regulated ERalpha and enhanced estrogen response element (ERE)-dependent gene expression. The additional finding that genistein antagonizes the anti-proliferative effect of hydroxytamoxifen suggests phytoestrogens may be detrimental in women with breast cancer who are being treated with tamoxifen. In addition, because of their ability to stimulate breast cell growth, the widespread use of phytoestrogens in postmenopausal women could be detrimental.

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Section: Discussionmentioning

confidence: 99%

Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha

Seo

DeNardo

Jacquot

et al. 2006

Breast Cancer Res Treat

115

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“…Genistein is the most biologically active isoflavone; it shows antimicrobial activity and is classified as preformed and inducible phytoalexin (15)(16)(17)(18). It is interesting to note that genistein is the only isoflavone found in leaves, independent of the cultivar and the sampling period, according to Ho et al (14).…”

Section: Discussionmentioning

confidence: 99%

Polyphenolic Content in Different Plant Parts of Soy Cultivars Grown under Natural Conditions

Romani

Vignolini

Galardi

et al. 2003

J. Agric. Food Chem.

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Roots, cotyledons, leaves, stems, pods, and seeds of three soy cultivars were analyzed for their content of isoflavones, flavonols, coumarins, and phenolic acid derivatives with three samplings during a three-month period. The extracts were analyzed by HPLC/DAD and HPLC/MS, allowing us to confirm the presence of daidzein and genistein derivatives as the major isoflavones and to characterize coumarins, most flavonols and phenolic acid derivatives. Seeds exhibited the highest content of isoflavones: 12.61 g/kg of dry weight (DW) in cv. Emiliana; 8.97 g/kg of DW in cv. Elvir; 4.49 g/kg of DW in cv. Kure, and roots are the only part with coumarins, ranging from 4.08 g/kg of DW (cv. Emiliana) to 1.29 g/kg of DW (cv. Elvir) for the longest sampling period. Leaves, pods, and stems have flavonols, and in particular leaves showed: 7.28 g/kg of DW in cv. Emiliana; 6.57 g/kg of DW in cv. Elvir; 7.08 g/kg of DW in cv. Kure. The high content of isoflavones found in the seeds could be ascribed to the natural conditions under which the soy plants were grown.

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“…Since, as noted above, isoflavone levels have not been demonstrated to be different between males and females on identical diets, the absolute influence of these compounds should be substantially greater in the male animals that have virtually no basal estrogenic stimulation. Moreover, there is in vivo evidence that genistein acts as an agonist at ERs when administered alone and as an antagonist when coadministered with 17β-estradiol (63). It is plausible that a similar mechanism is behind the sex difference in cardiac phenotype.…”

Section: Figurementioning

confidence: 99%

Soy diet worsens heart disease in mice

Stauffer

Konhilas

Luczak

et al. 2005

Journal of Clinical Investigation

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We report that dietary modification from a soy-based diet to a casein-based diet radically improves disease indicators and cardiac function in a transgenic mouse model of hypertrophic cardiomyopathy. On a soy diet, males with a mutation in the α-myosin heavy chain gene progress to dilation and heart failure. However, males fed a casein diet no longer deteriorate to severe, dilated cardiomyopathy. Remarkably, their LV size and contractile function are preserved. Further, this diet prevents a number of pathologic indicators in males, including fibrosis, induction of β-myosin heavy chain, inactivation of glycogen synthase kinase 3β (GSK3β), and caspase-3 activation.

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Inhibition of estrogenic stimulation of gene expression by genistein

Cited by 36 publications

References 31 publications

Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha

Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha

Polyphenolic Content in Different Plant Parts of Soy Cultivars Grown under Natural Conditions

Soy diet worsens heart disease in mice

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