摘要
脱酰基酶可以将echinocandin B(ECB)脱去酰基侧链得到ECB母核,用于化学合成抗真菌药阿尼芬净。本研究考察了以二甲基亚砜(DMSO)助溶剂的转化体系脱酰基酶对ECB转化的各因素,建立了转化工艺(磷酸缓冲浓度:0.02mol/L,pH7.0,KCl浓度:0.68mol/L,DMSO浓度:15%,ECB浓度:450mg/L,加酶量:10%,转化温度:40℃)。为了提高转化效率,探索了新的转化体系即以β-环糊精助溶剂的转化体系,其优势为:当ECB与β-环糊精的浓度比为1:6时,ECB可在体系中完全溶解,底物浓度可以达到2g/L。
The deacylase can take the acyl side chain off echinocandin B（ECB） and get the ECB＇s mother scaffold, which was used for the chemical synthesis of antifungal drug anidulafungin. This study investigated the factors of converting ECB in the DMSO system and established the conversion process （phosphate buffer concentration： 0.02mol/L, pH： 7.0, KCl concentration： 0.68mol/L, DMSO concentration： 15%, the ECB concentration： 450mg/L, enzyme amount： 10%, transformation temperature： 40℃）. In order to improve the conversion efficiency, a new conversion system was explored, in which the cosolvent was β-cyclodextrin. The advantage is： when the ECB with β-cyclodextrin concentration ratio was 1：6, the ECB could be completely dissolved in the system and the substrate concentration can reach 2g/L.
作者
朱进伟
滕云
张敏
高祥
郑玲辉
Zhu Jin-wei;Teng Yun;Zhang Min;Gao Xiang;Zheng Ling-hui(Hisun Pharmaceutical（Hang Zhou）Co.Ltd,Hangzhou 311404;Zhejiang Hisun Pharmaceutical Co.,Ltd.,Taizhou 318000;Zhejiang Anti-fungal Drug Key Laboratory,Taizhou 318000)
出处
《中国抗生素杂志》
CAS
CSCD
2018年第11期1376-1383,共8页
Chinese Journal of Antibiotics
