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Characterisation of the affinity of different anabolics and synthetic hormones to the human androgen receptor, human sex hormone binding globulin and to the bovine progestin receptor

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Abstract:

For the steroidal growth promoters trenbolone acetate (TBA) and melengestrol acetate (MGA) neither the complete spectrum of biological activities nor the potential endocrine disrupting activity of their excreted metabolites in the environment is fully understood. The potency of these substances in [3H]‐dihydrotestosterone ([3H]‐DHT) displacement from the recombinant human androgen receptor (rhAR) and from human sex‐hormone binding globulin (hSHBG) was evaluated. In addition, the potency for [3H]‐ORG2058 displacement from the bovine uterine progestin receptor (bPR) was tested. For comparison, different anabolics and synthetic hormones were also tested for their binding affinities. For 17β‐trenbolone (17β‐TbOH), the active compound after TBA administration, an affinity the rhAR similar to dihydrotestosterone (DHT) and a slightly higher affinity to the bPR than progesterone were demonstrated. The affinity of the two major metabolites, 17α‐trenbolone and trendione, was reduced to less than 5% of the 17β‐TbOH‐value. The affinity of these three compounds and of MGA to the hSHBG was much lower compared with DHT. MGA showed a 5.3‐fold higher affinity than progesterone to the bPR but only a weak affinity to the rhAR. The major MGA metabolites have an affinity to the bPR between 85% and 28% of the affinity of progesterone. In consequence, MGA and TBA metabolites may be hormonally active substances, which will be present in edible tissues and in manure. We conclude that detailed investigations on biodégradation, distribution and bio‐efficacy of these substances are necessary.

Document Type: Research Article

DOI: http://dx.doi.org/10.1111/j.1600-0463.2001.tb05797.x

Affiliations: 1: Institut für Physiologie, Research Center for Milk and Food Weihenstephan, Technical University Munich, D-85350 Freising 2: Schering AG, D-13342 Berlin 3: Institut für Anatomie, Physiologie und Hygiene der Haustiere, Rheinische Friedrich-Wilhelms-University Bonn, D-53115 Bonn, Germany

Publication date: July 1, 2001

mksg/apm/2001/00000109/A103s103/art00053
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