有机相脂肪酶催化合成脂质体修饰物胆固醇癸二酸单烯酯  

Lipase-catalyzed synthesis of cholesteryl vinyl hemi-sebacate for selective targeting of liposomes in organic media

作　　者：聂华[1] 郑品劲[1] 罗利华[1] 程怡[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》2013年第23期3289-3295,共7页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(30772790)

摘　　要：目的在非水相中利用酶法合成胆固醇癸二酸单烯酯,并对其最优合成工艺条件进行研究。方法利用TLC、MS和NMR法对合成产物进行结构鉴定;通过正交试验对合成处方工艺进行优化。结果最佳反应条件为胆固醇与癸二酸二乙烯酯物质的量之比为1∶6,Candida rugosa Lipase 10 mg/mL,异辛烷5 mL,温度35℃,反应时间24 h。结论该条件下酯化率可达95%以上。Objective To synthesize cholesteryl vinyl hemi-sebacate from cholesterol and divinyl sebacate in non aqueous phase. Methods TLC, MS, and NMR were used to identify the structure of production; the technological conditions of enzymatic esterification were determined through orthogonal test. Results The best condition： isooctane 5 mL, reaction temperature 35 ℃, reaction time 24 h, Candida rugosa Lipase 10 mg/mL, molar ratio of cholesterol to divinyl sebacate 1 ： 6. Conclusion The highest esterification rate is above 95%.

关 键 词：胆固醇 去唾液酸糖蛋白受体 酶催化 CANDIDA RUGOSA LIPASE 胆固醇癸二酸单烯酯 

分 类 号：R283.6[医药卫生—中药学]