Institute of Doping Analysis and Sports Biochemistry Dresden, Kreischa, Germany.
Environmental Monitoring and Endocrinology, Faculty of Biology, Dresden, Germany.
Arch Toxicol. 2022 Jul;96(7):2139-2142. doi: 10.1007/s00204-022-03283-5. Epub 2022 Mar 28.
Dietary supplements sold for anabolic benefits or performance enhancement often contain substances, which are non-approved and might lack quality controls. With regard to athletes, the inclusion of substances or methods in the prohibited list of the World Anti-Doping Agency is based on medical or scientific evidence. 5α-hydroxy-laxogenin is a synthetic spirostane-type steroid, which is contained in dietary supplements and advertised as anabolic agent. To date, evidence is missing on anabolic or androgenic activity of 5α-hydroxy-laxogenin. We investigated its androgenic potential in two in vitro bioassays. While no activity was observed in the yeast androgen screen, 5α-hydroxy-laxogenin was able to trans-activate the androgen receptor in human prostate cells in a dose-dependent manner. Interestingly, a biphasic response was observed with antagonistic properties at lower concentrations and agonistic effects at higher concentrations tested. The demonstrated androgenic properties of the higher concentrations demonstrate that further investigations should focus on the safety as well as on potential anabolic effects of 5α-hydroxy-laxogenin. This is of interest with regard to abuse for doping purposes.
用于促进合成代谢或增强运动表现的膳食补充剂通常含有未经批准的物质，并且可能缺乏质量控制。对于运动员来说，世界反兴奋剂机构禁用清单中包含的物质或方法是基于医学或科学证据。5α-羟基拉索精是一种合成螺甾烷型类固醇，存在于膳食补充剂中，并被宣传为合成代谢剂。迄今为止，5α-羟基拉索精缺乏关于其合成代谢或雄激素活性的证据。我们在两项体外生物测定中研究了其雄激素潜力。虽然在酵母雄激素筛选中未观察到活性，但 5α-羟基拉索精能够以剂量依赖性方式在人前列腺细胞中转激活雄激素受体。有趣的是，在较低浓度下观察到了双相反应，具有拮抗特性，而在较高浓度下则具有激动作用。较高浓度的雄激素特性表明，进一步的研究应集中在 5α-羟基拉索精的安全性以及潜在的合成代谢作用上。这对于出于兴奋剂目的滥用的情况是有意义的。
