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

Full text not available from this repository.

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:
CreatorsEmailORCIDORCID Put Code
Keiler, Annekathrin MartinaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Zierau, OliverUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Wolf, SylviUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Diel, PatrickUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Schaenzer, WilhelmUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Vollmer, GunterUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Machalz, DavidUNSPECIFIEDorcid.org/0000-0001-8634-9411UNSPECIFIED
Wolber, GerhardUNSPECIFIEDorcid.org/0000-0002-5344-0048UNSPECIFIED
Parr, Maria KristinaUNSPECIFIEDorcid.org/0000-0001-7407-8300UNSPECIFIED
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:
KeywordsLanguage
BREAST-CANCER PATIENTS; CHROMATOGRAPHY MASS-SPECTROMETRY; TRANSACTIVATION SYSTEM; 4-HYDROXYANDROST-4-ENE-3,17-DIONE; IDENTIFICATION; FORMESTANEMultiple languages
ToxicologyMultiple languages
Refereed: Yes
URI: http://kups.ub.uni-koeln.de/id/eprint/17928

Downloads

Downloads per month over past year

Altmetric

Export

Actions (login required)

View Item View Item