Suppression of aromatase (estrogen synthetase) by red wine phytochemicals

Estrogen promotes the proliferation of breast cancer cells. Aromatase is th e enzyme that converts androgen to estrogen. In tumors, the expression of a romatase is upregulated compared to surrounding non-cancerous tissue. In th is study, we found that wine contains phytochemicals that are capable of su ppressing aromatase. Red wine was shown to be much more effective than whit e wine in the suppression of aromatase activity. Whole wine, lyophilized wi ne, and heat-treated extracts were examined for aromatase inhibition in a h uman placenta microsomal assay. C18 Sep-Pak cartridge (Waters Co.) separati on of red wine extracts under an increasing acetonitrile (ACN) gradient fou nd that the most active components were in the 20 % ACN fraction, in that t hey inhibited the wild-type human placenta aromatase, wild-type porcine pla centa and blastocyst aromatase in a dose-dependent fashion. The 20 % ACN ac tive fraction was heat stable and inhibited aromatase in a non-competitive manner. The aromatase-inhibitory action of red wine extracts was also exami ned with a transgenic mouse model in which aromatase is over-expressed in t he mammary tissues. It was found that the intake of the 20 % ACN fraction b y gavage completely abrogated aromatase-induced hyperplasia and other chang es in the mammary tissue. This is the first report demonstrating that wine, especially red wine, contains phytochemicals that can inhibit aromatase.