普瑞巴林手性中间体水解酶产生菌的筛选及诱变选育 |
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引用本文: | 黄百祺,刘梦.普瑞巴林手性中间体水解酶产生菌的筛选及诱变选育[J].安徽农学通报,2012,18(11):42-44,48. |
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作者姓名: | 黄百祺 刘梦 |
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作者单位: | 广东科贸职业学院,广东广州,510430;广东科贸职业学院,广东广州,510430 |
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摘 要: | 以合成普瑞巴林关键性中间体2-羧乙基-3-氰基-5-甲基己酸乙酯为碳源,采用手性液相法检测,从土壤中筛选出1株产对映体选择性水解酶的菌株KM8,该菌产的水解酶能优先水解S型底物生成(3S)-2-羧乙基-3-氰基-5-甲基乙酸。菌株KM8经过紫外和硫酸二甲酯(DES)诱变,转化率提高到76.1%,产物对映体过量值(ee.)达到90.0%以上,较好地实现了手性拆分制备普瑞巴林中间体的目标。
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关 键 词: | 普瑞巴林 水解酶 菌种筛选 诱变 |
Strain Screening and Mutation for the Enantioselectively Hydrolysis of Chiral Intermediate of Pre- gabalin |
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Institution: | Huang Baiqi et al. (Guangdong Vocational College of Science and Trade, Guangzhou 510430, China) |
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Abstract: | Using ( S, R) - 2 - carboxyethyl - 3 - cyano - 5 - methyl - hexanoic acid ethylester ( rac - CCMAE ), a key in- termediate of pregabalin, as carbon source, KM8 was isolated which can enantioselectively hydrolyze (S) -CCMAE to (3S) -2 - carboxyethyl -3 - cyano -5 - methyl - hexanoic acid ( S - CCMA). Conversion rate and enantiomeric excess ( ee. ) were improved to 75.53% and more than 90.0% through UV and diethyl sulfate (DES) mutation, respectively, which would pave a way for the biotransformation of pregabalin. |
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Keywords: | Pregabalin Hydrolase Screening Mutation |
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