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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 the ligand cholesterol-galactoside molecule that can be specifically recognized by asialoglycoprotein receptor (ASGPR) in the organic phase by enzymatic reaction and optimize its synthesis process. Methods The structure of the product was identified by mass spectrometry and nuclear magnetic resonance spectroscopy. The enzymatic synthesis conditions were optimized by single factor and orthogonal design. Results The optimal enzymatic conditions were as follows: the ratio of cholesterol to sebacate (CH-VS) to lactitol (LA) was 4:1, Novozym 435 25 mg, reaction time was 32 h and the yield was 92 %. Conclusion The method is efficient, the reaction conditions are feasible, product specificity.