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Binding Characteristics of Zearalenone Analogs to Estrogen Receptors¹

Section of Medical Oncology, Department of Medicine [D. T. K., B. J. K.], and Department of Plant Pathology [S. V. P., C. J. M.], University of Minnesota, Minneapolis, Minnesota 55455

The estrogenic effect of zearalenone derivatives was investigated for their binding characteristics to cytosol and nuclear receptors in the uterus. Competition with 17ß-estradiol at the cytosol receptor sites was observed in four of the six derivatives tested, namely trans- and cis-zearalenone, zearalenol, and zearalanol. The other two, 8'-hydroxyzearalenone and 6'-aminozearalene, lacked the binding ability to receptors and were biologically inactive.

trans-Zearalenone, like 17ß-estradiol, could elicit an immediate translocation of cytosol-receptor complexes into the uterine nuclel. However, it differs from either 17ß-estradiol or antiestrogens (tamoxifen) in three aspects: (a) a second wave of translocation occurred 6 to 12 hr following zearalenone injection; (b) there was a much longer nuclear retention (over 24 hr) than in the case of 17ß-estradiol; and (c) following a depletion of cytosol receptors, trans-zearalenone induced an overreplenishment by 24 hr, whereas tamoxifen is reported to suppress the replenishment.

¹ Supported by Research Grants CA-19527, 16450, 08832, and CB-64000 from the National Cancer Institute of USPHS; by the Minnesota Medical Foundation; and by the Masonic Memorial Hospital Fund, Inc.

² To whom requests for reprints should be addressed.

Received 5/ 8/78. Accepted 7/21/78.