摘要
在现有手性药物的制备过程中,通常使用化学催化、气相或液相色谱分离纯化的方法,而耗能大、花费高、副产物多等是其主要缺点.近年来,生物酶法拆分手性药物的研究逐渐增多,多类生物酶已被报道具有催化手性拆分的能力,其对不同类底物的应用是目前研究的重点之一.在生物酶法拆分手性药物的过程中,反应溶剂与酰基供体是影响对映选择拆分效率的主要因素;另外,合理应用酶的固定化技术能有效的提高拆分效率,使其具有工业应用的可能.生物酶法拆分手性药物因具有副产物少、操作简便、环境友好等优点而备受关注,有望补充或替换化学法在手性药物制备中的作用.随着结构生物学、现代分子生物学的发展与酶法拆分手性药物研究的不断深入,通过对酶分子空间结构与催化机理的分析研究,人工合成具有特定催化功能的酶成为可能,生物酶法拆分手性药物技术的应用有望得到较大的突破.
Chemical catalysis, gas or liquid chromatography separation and purification are the main technologies in chiral drug preparation, which result in high energy consumption, high cost, and multi-byproducts and so on. Enzymatic resolution in chiral drugs preparation was attracted increasing attention in recent years. Many kinds of enzyme were investigated on their resolution ability towards different substrates, and their application has become a topic subject. It was found that the reaction solvent and acyl donor are the most important factors to enantio selective efficiency. A proper immobilization technology can significantly enhance the enzyme activity and pave the way to industrialization. The enzymatic resolution of chiral drugs could play a key role in chiral pharmacy production with less byproducts, simple operation and environmental frendliness. Based on the rapid progress in structure biology, especially deep understand of enzyme structure and catalytic mechanism, the enzymatic chiral resolution is expected to be made great advances with the development of modern techniques of molecular biology and chiral drug.
出处
《武汉工程大学学报》
CAS
2016年第6期517-520,526,共5页
Journal of Wuhan Institute of Technology
基金
国家自然科学基金项目(31170078)
国家863课题(2014AA093510)
关键词
酶法拆分
手性药物
对映选择性
异构体
enzymatic chiral resolution
chiral drug
enantioselective
isomer
