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目的用酶促催化乳糖酸与十八胺合成一种可用于镶嵌脂质体表面的去唾液酸糖蛋白靶向配体修饰物。方法通过红外光谱(IR)、质谱(ESI-MS)和核磁共振(1H-NMR)对产物结构进行确证,并对酶种类、反应介质、酶的加入量、底物摩尔比、反应温度等影响因素进行考察。结果二甲基亚砜作为反应介质;Novozym 435固定化脂肪酶作为催化剂、酶加入量为400U.mL-1、乳糖酸和十八胺的摩尔比为2∶1、40℃下反应24 h,十八胺的转化率可达99%以上。结论酶促催化法可用来合成肝靶向脂质体配体。
OBJECTIVE: To synthesize an asialoglycoprotein targeting ligand modifier that can be used to encapsulate the surface of liposomes by enzymatically catalyzed lactobionic acid and octadecylamine. Methods The structure of the product was confirmed by IR, ESI-MS and 1H-NMR. The effects of enzyme type, reaction medium, amount of enzyme, molar ratio of substrate and reaction temperature Factors to investigate. Results dimethyl sulfoxide as the reaction medium; Novozym 435 immobilized lipase as a catalyst, enzyme dosage 400U.mL-1, lactobionic acid and octadecylamine molar ratio of 2: 1, 40 ° C for 24 h, Octadecylamine conversion rate of up to 99%. Conclusion Enzymatic catalysis can be used to synthesize liver targeting liposome ligands.