Department of Chemistry, Wrocław University of Environmental and Life Sciences,Wrocław, Poland.
Steroids. 2010 Dec 12;75(13-14):1146-52. doi: 10.1016/j.steroids.2010.08.001. Epub 2010 Aug 18.
Dehydroepiandrosterone (DHEA) and its metabolite 7α-OH DHEA have many diverse physiological, biological and biochemical effects encompassing various cell types, tissues and organs. In in vitro studies, DHEA analogues have myriad biological actions, but in vivo, especially in oral administration, DHEA produces far more limited clinical effects. One of the possible solutions of this problem is conversion of DHEA to active analogues and/or its transformation into prodrug form. In this article, the studies on the conversion of DHEA and 7α-OH DHEA into their phosphatides by the phosphodiester approach are described. In this esterification, N,N-dicyclohexylcarbodiimide (DCC) was the most efficient coupling agent as well as p-toluenesulphonyl chloride (TsCl).
脱氢表雄酮（DHEA）及其代谢产物 7α-OH DHEA 具有许多不同的生理、生物学和生物化学作用，涵盖了各种细胞类型、组织和器官。在体外研究中，DHEA 类似物具有多种生物学作用，但在体内，特别是口服给药时，DHEA 产生的临床效果要有限得多。解决这个问题的一种可能方法是将 DHEA 转化为活性类似物和/或将其转化为前药形式。本文描述了通过磷酸二酯途径将 DHEA 和 7α-OH DHEA 转化为其磷脂的研究。在这种酯化反应中，N,N-二环己基碳二亚胺（DCC）是最有效的偶联剂，对甲苯磺酰氯（TsCl）也是如此。
