Anal Bioanal Chem.
2008 Feb;390(4):1111-9. Epub 2008 Jan 11. Screening of synthetic and plant-derived compounds for (anti)estrogenic and (anti)androgenic activities.Bovee TF
, Schoonen WG
, Hamers AR
, Bento MJ
, Peijnenburg AA
Department of Safety & Health, RIKILT-Institute of Food Safety, P.O. Box 230, 6700 AE, Wageningen, The Netherlands. email@example.com Abstract
Recently we constructed yeast cells that either express the human estrogen
receptor alpha or the human androgen receptor in combination with a consensus ERE or ARE repeat in the promoter region of a green fluorescent protein (yEGFP) read-out system. These bioassays were proven to be highly specific for their cognate agonistic compounds. In this study the value of these yeast bioassays was assessed for analysis of compounds with antagonistic properties. Several pure antagonists, selective estrogen
receptor modulators (SERMs) and plant-derived compounds were tested. The pure antiestrogens ICI 182,780 and RU 58668 were also classified as pure ER antagonists in the yeast estrogen
bioassay and the pure antiandrogen flutamide was also a pure AR antagonist in the yeast androgen bioassay. The plant-derived compounds flavone and guggulsterone displayed both antiestrogenic and antiandrogenic activities, while 3,3'-diindolylmethane (DIM) and equol combined an estrogenic mode of action with an antiandrogenic activity.
Indol-3-carbinol (I3C) only showed an antiandrogenic activity. Coumestrol, genistein, naringenin and 8-prenylnaringenin were estrogenic and acted additively, while the plant sterols failed to show any effect. Although hormonally inactive, in vitro and in vivo metabolism of the aforementioned plant sterols may still lead to the formation of active metabolites in other test systems.