Li Hui, Sun Jin, Xu Zhenghong
School of Pharmaceutical Science, Jiangnan University, 1800 Lihu Avenue, Wuxi, 214122, People's Republic of China.
Methods Mol Biol. 2017;1645:289-295. doi: 10.1007/978-1-4939-7183-1_20.
3β,7α,15α-Trihydroxy-5-androsten-17-one (7α,15α-diOH-DHEA) is a key intermediate of the novel oral contraceptive "Yasmin" (widely used in birth control pills and postmenopausal hormone replacement therapy pills; the active ingredient is drospirenone). It can be synthesized from dehydroepiandrosterone (DHEA) by microbial dihydroxylation at the C7 and C15 positions. Here we describe the method of bioconversion from DHEA into 7α,15α-diOH-DHEA by Colletotrichum lini. Using 6 g/L DHEA as a substrate, the DHEA conversion and the 7α,15α-diOH-DHEA molar yield were 72.6% and 51.2%, respectively.
3β,7α,15α-三羟基-5-雄甾烯-17-酮(7α,15α-二羟基脱氢表雄酮)是新型口服避孕药“优思明”(广泛用于避孕药和绝经后激素替代治疗药物;活性成分是屈螺酮)的关键中间体。它可以通过脱氢表雄酮(DHEA)在C7和C15位进行微生物双羟基化反应合成。在此,我们描述了亚麻炭疽菌将DHEA生物转化为7α,15α-二羟基脱氢表雄酮的方法。以6 g/L DHEA作为底物时,DHEA转化率和7α,15α-二羟基脱氢表雄酮的摩尔产率分别为72.6%和51.2%。