雄甾-4-烯-3,17-双酮转化菌株的筛选及转化产物的鉴定

目的甾体化合物雄甾-4-烯-3,17-双酮（andros-t 4-ene-3,17-dione,4AD）是制造甾体激素类药物的关键药物中间体之一,开展4AD的微生物转化,以探索具有新活性的4AD衍生物的合成。方法本研究通过摇瓶培养转化,TLC分析,筛选能够对4AD进行有效转化的菌株,利用硅胶柱层析对转化产物进行分离纯化,通过TOF-MS、IR、1 HNMR、13 C NMR光谱数据分析,同时与相关文献报道结合,确定转化产物的结构。结果本研究筛选到了一株能够对4AD进行有效转化的菌株,初步确定其为茄病镰孢菌（Fusarium solani）,得到2种转化产物：具有较大生物活性潜力的17-hydroxy-pregen-1,4-dien-3-one和重要的药物中间体雄二烯二酮（ADD）。结论本研究筛选得到的茄病镰孢菌能够对4AD进行有效转化,对于利用微生物转化的方法生产17位羟基化甾体物质和ADD具有较大的应用潜力。

Screening of AD-Transforming Strains and Identification of the Transformation Products

Objective Androst 4-ene-3,17-dione（AD）is an important drug intermediate for steroid hormone drugs and other drugs,it is necessary to search for new AD derivatives with activity through microbiotransformation.Methods The research purpose is to isolate the microorganisms which can biotransform AD through the flask culture and TLC analysis methods,meanwhile to purify the transformation products by using silica gel column and identify the product structures by spectroscopic methods such as IR,MS and MR.Results An fungi which can effective biotransform AD was isolated and identificated as Fusarium solani according to its ITS sequence analysis.The 2main transformation products were purified and characterized as 17-hydroxy-pregen-1,4-dien-3-one and androst-1,4-dien-3,17-dione.Conclusion The Fusarium Solani isolated can effective transform AD,It has important application potential in producing 17-hydroxy steroidal and ADD.