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

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%.