丙氨酸肽脂的合成与脂质体制备  

Synthesis of alanine type peptide lipids and preparation of liposome

作　　者：姜强[1] 刘宝全[1] 熊文[1] 王剑锋[1] 范圣第[1] 

机构地区：[1]大连民族大学生命科学学院国家民委-教育部生物技术与资源利用重点实验室,辽宁大连116600

出　　处：《化学研究与应用》2015年第5期649-653,共5页Chemical Research and Application

基　　金：国家自然科学基金项目(21172028;21372037)资助;教育部高校自主基金项目(DC12010105)资助

摘　　要：以十六酸、十六烷基胺、Boc保护丙氨酸、6-溴己酰氯、三甲胺为主要原料,通过EDC(1-乙基-(3-二甲基氨基丙基)碳二亚胺)缩合、氢化锂铝还原酰胺形成胺等反应合成丙氨酸肽脂,最终得率为39.9%,高分离温度(35℃)可提高产物得率。丙氨酸肽脂不需要胆固醇与辅助类脂可独立形成脂质体,通过激光粒度仪、透射电子显微镜进行初步检测,脂质体平均粒径为97.4±15.5nm,表面电位为+63.53±1.53 m V。A cationic lipid（[N,N-dihexadecyl-Nα-[6-（trimethylammonio）hexanoyl]-alaninamide bromide],N＋C5Ala2C16,ala-nine type peptide lipid） was synthesized with the major raw materials such as palmitic acid,hexadecylamine,Boc-alanine,6-bromo-hexanoyl chloride and trimethylamine by the method of 1-ethyl-（3-dimethylaminopropyl）carbodiimide hydrochloride（EDC）conden-sation reaction, lithium aluminum hydride reduction reaction. The best yield was 39. 9%under the high separation temperature （35℃）. The liposomes were prepared with alanine type peptide lipid without any other lipoids such cholesterol and help lipids. The average size was 97. 4±15. 5nm detected using a laser particle size analyzer,the average surface potential voltage was＋63. 53± 1. 53 mV and the shape of liposome was spherical under the transmission electron microscopy.

关 键 词：丙氨酸肽脂 脂质体 合成 

分 类 号：O623.738[理学—有机化学]