کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8553183 | 1562580 | 2018 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Androgen- and estrogen-receptor mediated activities of 4-hydroxytestosterone, 4-hydroxyandrostenedione and their human metabolites in yeast based assays
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
DHTWADA17β-estradiol - 17β استرادیولDMSO - DMSOFormestane - formestaneWorld Anti-Doping Agency - آژانس جهانی ضد دوپینگYES - بلهDoping - دوپینگDihydrotestosterone - دی هیدروتستوسترونDimethyl sulfoxide - دیمتیل سولفواکسیدSaccharomyces cerevisiae - ساکارومایسس سرویزیهyeast androgen screen - صفحه نمایش آندروژن مخمرYeast Estrogen Screen - صفحه نمایش استروئید مخمرMolecular modeling - مدل سازی مولکولیoptical density - چگالی نوریYAS - یاس
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم محیط زیست
بهداشت، سم شناسی و جهش زایی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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 2α-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 (10â8â¯M), 4-hydroxyandrost-4-ene-3,17-dione (10â8â¯M) and two more urinary metabolites, the yeast androgen assay may also be used to trace abuse in urine samples.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Toxicology Letters - Volume 292, August 2018, Pages 39-45
Journal: Toxicology Letters - Volume 292, August 2018, Pages 39-45
نویسندگان
Annekathrin Martina Keiler, Oliver Zierau, Sylvi Wolf, Patrick Diel, Wilhelm Schänzer, Günter Vollmer, David Machalz, Gerhard Wolber, Maria Kristina Parr,