去唾液酸糖蛋白受体配体胆固醇-半乳糖苷的酶促合成优化研究  

Optimization of enzymatic synthesis of asialoglycoprotein receptor ligand cholesterol-vinyl sebacate-lactitol

作　　者：陈静[1] 程怡[1] 郑品劲[1] 聂华[1] 陈宇潮 仝一丹 罗利华[1] 李朝[1] 

机构地区：[1]广州中医药大学中药学院,广东广州510006

出　　处：《中草药》2015年第4期502-506,共5页Chinese Traditional and Herbal Drugs

基　　金：教育部高等学校博士学科点专项科研基金(20134425110010)

摘　　要：目的在有机相中利用酶促反应合成能被去唾液酸糖蛋白受体(ASGPR)特异性识别的配体胆固醇-半乳糖苷分子,对其合成工艺进行优化。方法采用质谱和核磁碳谱鉴别产物结构;单因素和正交设计法优化酶促合成条件。结果酶促最佳条件为底物胆固醇癸二酸乙烯酯(CH-VS)与乳糖醇(LA)物质的量之比4∶1,脂肪酶Novozym 435 25 mg,反应32 h,产率高达92%。结论该方法高效、反应条件可行、产物专一。Objective To synthesize asialoglycoprotein receptor（ASGPR） ligand cholesterol-vinyl sebacate-lactitol（CH-VS-LA） by using enzymatic reaction in organic phase and to optimize its synthesis process. Methods MS and 13C-NMR were used to identify the structure of product, enzymatic synthesis conditions were optimized via single-factor test and orthogonal experimental design. Results The enzymatic optimum conditions were as following： the molar ratio of cholesterol-vinyl sebacate（CH-VS） and lactitol（LA） was 4∶1, the amount of lipase Novozym 435 was 25 mg, reactional time was 32 h, and productive rate was 92%. Conclusion The method is highly effecient, the reaction conditions are reasonable, and the process produces no by-product.

关 键 词：去唾液酸糖蛋白受体(ASGPR)配体 胆固醇-半乳糖苷 酶促合成 单因素试验 正交试验设计 

分 类 号：R283.6[医药卫生—中药学]