Universität zu Köln

Keiler, Annekathrin Martina, Zierau, Oliver, Wolf, Sylvi, Diel, Patrick, Schaenzer, Wilhelm, Vollmer, Gunter, Machalz, David ORCID: 0000-0001-8634-9411, Wolber, Gerhard ORCID: 0000-0002-5344-0048 and Parr, Maria Kristina ORCID: 0000-0001-7407-8300 (2018). Androgen-and estrogen-receptor mediated activities of 4-hydroxytestosterone, 4-hydroxyandrostenedione and their human metabolites in yeast based assays. Toxicol. Lett., 292. S. 39 - 46. CLARE: ELSEVIER IRELAND LTD. ISSN 1879-3169

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Abstract

4-Hydroxyandrost-4-ene-3,17-dione, also named formestane, is an irreversible aromatase inhibitor and therapeutically used as anti-breast cancer medication in post-menopausal women. Currently, no therapeutical indication led to approval of its 17-hydroxylated analog 4-hydroxytestosterone, an anabolic steroid. However, it is currently investigated in a clinical trial for breast cancer. In context with sports doping, aromatase inhibitors are administered to reduce estrogenic side effects of misused anabolic substances or their metabolites. Therefore, both substances are prohibited in sports by the World Anti-Doping Agency (WADA). Analysis of urinary phase I and phase II metabolites showed similar results for both compounds. In the current investigation, 4-hydroxyandrost-4-ene-3,17-dione, 4-hydroxytestosterone and seven of their described urinary metabolites as well as 2 alpha-hydroxyandrostenedione were tested in the yeast androgen screen and the yeast estrogen screen. Androgenic effects were observed for all tested substances, except for one, which showed anti-androgenic properties. With regard to the yeast estrogen screen, estrogenic effects were observed for only two metabolites at rather high concentrations, while six out of the ten substances tested showed anti-estrogenic properties. In terms of the strong androgenic effect observed for 4-hydroxytestosterone (10(-8) M), 4-hydroxyandrost-4-ene-3,17-dione (10(-8) M) and two more urinary metabolites, the yeast androgen assay may also be used to trace abuse in urine samples.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Keiler, Annekathrin Martina UNSPECIFIED UNSPECIFIED UNSPECIFIED Zierau, Oliver UNSPECIFIED UNSPECIFIED UNSPECIFIED Wolf, Sylvi UNSPECIFIED UNSPECIFIED UNSPECIFIED Diel, Patrick UNSPECIFIED UNSPECIFIED UNSPECIFIED Schaenzer, Wilhelm UNSPECIFIED UNSPECIFIED UNSPECIFIED Vollmer, Gunter UNSPECIFIED UNSPECIFIED UNSPECIFIED Machalz, David UNSPECIFIED orcid.org/0000-0001-8634-9411 UNSPECIFIED Wolber, Gerhard UNSPECIFIED orcid.org/0000-0002-5344-0048 UNSPECIFIED Parr, Maria Kristina UNSPECIFIED orcid.org/0000-0001-7407-8300 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-179281
DOI:	10.1016/j.toxlet.2018.04.026
Journal or Publication Title:	Toxicol. Lett.
Volume:	292
Page Range:	S. 39 - 46
Date:	2018
Publisher:	ELSEVIER IRELAND LTD
Place of Publication:	CLARE
ISSN:	1879-3169
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language BREAST-CANCER PATIENTS; CHROMATOGRAPHY MASS-SPECTROMETRY; TRANSACTIVATION SYSTEM; 4-HYDROXYANDROST-4-ENE-3,17-DIONE; IDENTIFICATION; FORMESTANE Multiple languages Toxicology Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/17928