Abstract
Chemically synthesized naringenin derivatives, identical to natural occurring compounds, were tested for their estrogenic activity using two independent estrogen screening assays. Using a yeast based estrogen receptor assay, strong estrogenic activities were demonstrated for 6-(1,1-dimethylallyl)naringenin and 8-prenylnaringenin, while the parent compound naringenin did not show recognizable estrogenic activity. In MVLN cells, a bioluminescent MCF-7-derived cell line, the estrogenic activity of 8-prenylnaringenin and 6-(1,1-dimethylallyl)naringenin was detected at concentrations of 10-6 M and 5 × 10-6 M respectively. Naringenin demonstrated estrogenic activity but only at a concentration of 10-5 M. These estrogenic effects are mediated by the ER, as the antiestrogen 4-hydroxytamoxifen inhibited these activities. In summary, this study provides the further confirmation that 8-prenylnaringenin demonstrates high estrogenic activity, and demonstrated for the first time for 6-(1,1-dimethylallyl)naringenin a reasonable high estrogenic activity, while naringenin exhibit low or no estrogenic activity.
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Dr. Oliver Zierau
Technische Universität Dresden
Institut für Zoologie
Zellescher Weg 20, EG., Raum: 28a
01217 Dresden
Germany
Phone: +49-351-46 33 78 41
Fax: +49-351-46 3319 23
Email: Oliver.Zierau@mailbox.tu-dresden.de