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Thread: Grape Seed Extract Is an Aromatase Inhibitor and a Suppressor of Aromatase Expression

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    Grape Seed Extract Is an Aromatase Inhibitor and a Suppressor of Aromatase Expression

    Grape Seed Extract Is an Aromatase Inhibitor and a Suppressor of Aromatase Expression

    Ikuko Kijima, Sheryl Phung, Gene Hur, Sum-Ling Kwok and Shiuan Chen
    Department of Surgical Research, Beckman Research Institute of the City of Hope, Duarte, California

    Aromatase is the enzyme that converts androgen to estrogen. It is expressed at higher levels in breast cancer tissues than normal breast tissues. Grape seed extract (GSE) contains high levels of procyanidin dimers that have been shown in our laboratory to be potent inhibitors of aromatase. In this study, GSE was found to inhibit aromatase activity in a dose-dependent manner and reduce androgen-dependent tumor growth in an aromatase-transfected MCF-7 (MCF-7aro) breast cancer xenograft model, agreeing with our previous findings.

    We have also examined the effect of GSE on aromatase expression. Reverse transcription-PCR experiments showed that treatment with 60 µg/mL of GSE suppressed the levels of exon I.3–, exon PII–, and exon I.6–containing aromatase mRNAs in MCF-7 and SK-BR-3 cells. The levels of exon I.1–containing mRNA, however, did not change with GSE treatment. Transient transfection experiments with luciferase-aromatase promoter I.3/II or I.4 reporter vectors showed the suppression of the promoter activity in a dose-dependent manner. The GSE treatment also led to the down-regulation of two transcription factors, cyclic AMP-responsive element binding protein-1 (CREB-1) and glucocorticoid receptor (GR). CREB-1 and GR are known to up-regulate aromatase gene expression through promoters I.3/II and I.4, respectively. We believe that these results are exciting in that they show GSE to be potentially useful in the prevention/treatment of hormone-dependent breast cancer through the inhibition of aromatase activity as well as its expression. (Cancer Res 2006; 66(11): 5960-7)
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    We believe that these results are exciting in that they show GSE to be potentially useful in the prevention/treatment of hormone-dependent breast cancer through the inhibition of aromatase activity as well as its expression.

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    What's the active ingredient that's causing the inhibition? Is it present in grape seed oil since many of us are injecting with that?

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    I wondered the same thing. Would the grape seed oil help work as an AI?

    Generally on studies like this; they obtain just seeds and crush them.

    Grape seed oil from what i understand is made ina multi step process and is not exactly considered a pure extract.

    The study does not mention and I do no think they have isolated the exact factor responsible.

    But, having said and read all that if you do buy and eat grapes get the ones with seeds.

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    Has to be extract.It is also a strong antioxidant.

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    Good info dancer.

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    Quote Originally Posted by Dancer View Post
    I wondered the same thing. Would the grape seed oil help work as an AI?

    Generally on studies like this; they obtain just seeds and crush them.

    Grape seed oil from what i understand is made ina multi step process and is not exactly considered a pure extract.

    The study does not mention and I do no think they have isolated the exact factor responsible.

    But, having said and read all that if you do buy and eat grapes get the ones with seeds.
    http://www.uzzireissmd.com/bin/53-Gr...%20Supreme.pdf

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    name is
    LEUCOTENESELECT PHITOSOME

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    Quote Originally Posted by romo6 View Post
    Has to be extract.It is also a strong antioxidant.
    I would agree with that. I take it to help regulate my blood pressure.

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    Quote Originally Posted by Kratos View Post
    What's the active ingredient that's causing the inhibition? Is it present in grape seed oil since many of us are injecting with that?
    I read that the procyanidin B dimers are the active ones. These are also found in red wine.

    It also seems to inhibit cortisol by glucocorticoid receptor binding. As other phenols, such as Quercetin.

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    Quote Originally Posted by Swifto;4***665
    I read that the procyanidin B dimers are the active ones. These are also found in red wine.

    It also seems to inhibit cortisol by glucocorticoid receptor binding. As other phenols, such as Quercetin.
    good to know!

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