Bioanalysis Research Group, IMIM, Hospital del Mar, Doctor Aiguader 88, 08003 Barcelona, Spain.
Steroids. 2011 Nov;76(12):1367-76. doi: 10.1016/j.steroids.2011.07.005. Epub 2011 Jul 18.
The screening of testosterone misuse in the doping control field is normally performed by the measurement of the ratio between the concentrations of testosterone and epitestosterone excreted as glucuronides (T/E). Despite the satisfactory results obtained with this approach, the measurement of T/E presents some limitations like the long-term detection of oral testosterone administration. Recently, several testosterone metabolites released after basic treatment of the urine have been reported (androsta-1,4-dien-3,17-dione, androsta-4,6-dien-3,17-dione, 17β-hydroxy-androsta-4,6-dien-3-one and 15-androsten-3,17-dione). In the present work, the usefulness of these metabolites for the detection of oral testosterone misuse has been evaluated and compared with the conventional T/E measurement. For this purpose, 173 urine samples collected from healthy volunteers were analysed in order to obtain reference concentrations for the four metabolites released after alkaline treatment. On the other hand, urine samples collected from five volunteers before and after testosterone undecanoate administration were also analysed. Concentrations of androsta-4,6-dien-3,17-dione and 17β-hydroxy-androsta-4,6-dien-3-one showed a similar behaviour as the T/E, allowing the detection of the misuse for several hours after administration. More promising results were obtained by quantifying androsta-1,4-dien-3,17-dione and 15-androsten-3,17-dione. The time in which the concentrations of these analytes could be differentiated from the basal level was between 3 and 6 times longer than the obtained with T/E, as a result, an improvement in the detection of testosterone abuse can be achieved. Moreover, several ratios between these compounds were evaluated. Some of them improved the detection of testosterone misuse when comparing with T/E. The best results were obtained with those ratios involving androsta-1,4-dien-3,17-dione.
在兴奋剂检测领域，通常通过测量睾酮和表睾酮以葡萄糖醛酸酯形式排泄的浓度比值（T/E）来筛查睾酮滥用。尽管这种方法取得了令人满意的结果，但 T/E 的测量存在一些局限性，例如长期检测口服睾酮的使用。最近，已经报道了几种碱性处理尿液中释放的睾酮代谢物（雄甾-1,4-二烯-3,17-二酮、雄甾-4,6-二烯-3,17-二酮、17β-羟基雄甾-4,6-二烯-3-酮和 15-雄烯-3,17-二酮）。在本研究中，评估了这些代谢物在检测口服睾酮滥用中的有用性，并与传统的 T/E 测量进行了比较。为此，分析了 173 名健康志愿者采集的尿液样本，以获得碱性处理后释放的四种代谢物的参考浓度。另一方面，还分析了五名志愿者在接受十一酸睾酮给药前后采集的尿液样本。雄甾-4,6-二烯-3,17-二酮和 17β-羟基雄甾-4,6-二烯-3-酮的浓度与 T/E 相似，可在给药后数小时内检测到滥用。通过定量分析雄甾-1,4-二烯-3,17-二酮和 15-雄烯-3,17-二酮，得到了更有前途的结果。这些分析物的浓度可以与基础水平区分开来的时间比 T/E 长 3 到 6 倍，因此，可以提高睾酮滥用的检测能力。此外，还评估了这些化合物之间的几种比值。与 T/E 相比，其中一些比值提高了睾酮滥用的检测能力。使用涉及雄甾-1,4-二烯-3,17-二酮的比值可以获得最佳结果。
