Department of Biological Engineering, Utah State University, 4105 Old Main Hill, Logan, UT 84322, United States; College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, Zhejiang 310032, China.
Department of Biological Engineering, Utah State University, 4105 Old Main Hill, Logan, UT 84322, United States.
Bioorg Med Chem Lett. 2014 Jul 15;24(14):3023-5. doi: 10.1016/j.bmcl.2014.05.038. Epub 2014 May 22.
Spironolactone is a medicinally important molecule that is clinically used in the treatment and management of many diseases such as oedema and ascites in cirrhosis of the liver, malignant ascites, nephrotic syndrome, chronic lung disease, resistant hypertension, congestive heart failure, and primary hyperaldosteronism. Microbial transformations of spironolactone by Cunninghamella elegans ATCC 9245 was carried out. Two new hydroxylated derivatives, 12β-hydroxy-spironolactone and 2α-hydroxy-spironolactone, were synthesized. Their structures were characterized on the basis of the spectroscopic data. The substrate can be efficiently converted into the products within 72 h after its addition to the fermentation broth of C. elegans ATCC 9245.
螺内酯是一种具有医学重要性的分子，临床上用于治疗和管理许多疾病，如肝硬变的水肿和腹水、恶性腹水、肾病综合征、慢性肺病、耐药性高血压、充血性心力衰竭和原发性醛固酮增多症。用卷枝毛霉 ATCC 9245 对螺内酯进行微生物转化。合成了两种新的羟化衍生物 12β-羟基螺内酯和 2α-羟基螺内酯。根据光谱数据对其结构进行了表征。在向 C.elegans ATCC 9245 的发酵液中加入底物后，72 小时内可以有效地将其转化为产物。
