酶法合成Kupffer细胞靶向的半乳糖配体  

Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells

作　　者：聂华[1] 程怡[1] 郑品劲[1] 赵菊香[1] 吴琼[1] 

机构地区：[1]广州中医药大学中药学院,广州510006

出　　处：《中国实验方剂学杂志》2013年第10期21-24,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(30772790)

摘　　要：目的:采用酶催化法在非水相介质中合成半乳糖配体。方法:通过IR,质谱,核磁共振(1H-NMR,1C-NMR)对产物结构进行表征;以底物转化率为指标,采用单因素试验考察酶种类、反应介质、酶加入量、底物摩尔比、反应温度等对配体合成的影响。结果:通过表征分析显示经酶的催化反应,半乳糖C1’位的羟基发生了酯化反应,所得产物为目标产物。优选的反应条件为反应介质四氢呋喃(THF)-二甲基亚砜(DMSO)(3∶1),Novozym 435固定化脂肪酶为催化剂,酶加入量600 U.mL-1,半乳糖-硬脂酸乙烯酯的摩尔比1∶4,于55℃反应8 h,半乳糖的转化率达>0%。结论:酶促催化法可用于合成肝靶向脂质体配体。Objective： To synthesize galactose ligand in non-aqueous medium by enzyme-catalyzed method. Method： Structure of the product was confirmed by IR,ESI-MS,1H-NMR and1C-NMR;With conversion rate of substrate as index,effects of enzyme species,reaction medium,the amount of enzyme,molar ratio of substrate,reaction temperature on ligand synthesis was investigated by single factor tests. Result： Characterization by catalytic reaction,C1＇ bit hydroxyl of galactose occurred esterification,the received products was the target product.Optimized reaction conditions were as followings：tetrahydrofuran（THF）-dimethyl sulfoxide（DMSO）3：1 as reaction medium,Novozym 435 immobilized lipase as catalyst,the amount of enzyme of 600 UmL-1,molar ratio of galactose to vinyl stearate at 1：4,and reacted at 55 ℃ for 8 h,the conversion rate of galactose reached more than 70%. Conclusion： Enzyme catalysis method could be used for synthesizing ligand of liver targeted liposomes.

关 键 词：酶促催化 去唾液酸糖蛋白受体 配体 半乳糖 

分 类 号：R283.6[医药卫生—中药学]