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Analytical and Bioanalytical Chemistry

, Volume 390, Issue 4, pp 1111–1119 | Cite as

Screening of synthetic and plant-derived compounds for (anti)estrogenic and (anti)androgenic activities

  • Toine F. H. BoveeEmail author
  • Willem G. E. J. Schoonen
  • Astrid R. M. Hamers
  • Marta Jorge Bento
  • Ad A. C. M. Peijnenburg
Original Paper

Abstract

Recently we constructed yeast cells that either express the human estrogen receptor α 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.

Keywords

Agonist Antagonist Plant hormones Synthetic antiestrogens Yeast estrogen bioassay Yeast androgen bioassay 

Notes

Acknowledgements

This project was financially supported by the Dutch Ministry of Agriculture, Nature and Food Quality (project number 772027.01). The authors thank Ron Hoogenboom for reading the manuscript and his advice.

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Copyright information

© Springer-Verlag 2007

Authors and Affiliations

  • Toine F. H. Bovee
    • 1
    Email author
  • Willem G. E. J. Schoonen
    • 2
  • Astrid R. M. Hamers
    • 1
  • Marta Jorge Bento
    • 1
  • Ad A. C. M. Peijnenburg
    • 1
  1. 1.Department of Safety & HealthRIKILT-Institute of Food SafetyWageningenThe Netherlands
  2. 2.Department of PharmacologyNV OrganonOssThe Netherlands

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