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胆固醇-聚乙二醇-胰岛素偶联物的合成
引用本文:杨莉,伍晓春,钱珊,赵敏,吴勇.胆固醇-聚乙二醇-胰岛素偶联物的合成[J].四川大学学报(自然科学版),2010,47(4):859-862.
作者姓名:杨莉  伍晓春  钱珊  赵敏  吴勇
作者单位:1. 四川大学华西药学院,成都,610041
2. 四川师范大学化学与材料科学学院,成都,610066
基金项目:国家自然科学基金(30672537);高等学校博士学科点专项科研基金(20050610085)
摘    要:选择了胰岛素受体为作用靶点,设计并合成了用于新型肝靶向药物传递系统的脂质体配体,以赋予脂质体的双重靶向性.以聚乙二醇2000(2)和胆固醇衍生物(3)为起始原料,经过Williamson成醚反应、酰化反应,最后与胰岛素缩合得目标化合物(1).所得目标物(1)分子量经MALDI-TOF确证.

关 键 词:肝靶向药物  胰岛素受体  脂质体配体  合成

Synthesis of cholesterol-polyglycol-insulin conjugate
YANG Li,WU Xiao-Chun,QIAN Shan,ZHAO Min,WU Yong.Synthesis of cholesterol-polyglycol-insulin conjugate[J].Journal of Sichuan University (Natural Science Edition),2010,47(4):859-862.
Authors:YANG Li  WU Xiao-Chun  QIAN Shan  ZHAO Min  WU Yong
Institution:School of Pharmacy, Sichuan University;Chemistry and Material College, Sichuan Normal University;School of Pharmacy, Sichuan University;School of Pharmacy, Sichuan University;School of Pharmacy, Sichuan University
Abstract:Insulin receptor was chosen for targeting site, a new kind of ligand for liposome in drug delivery system was designed and synthesized to endue dual functions of the liposome. PEG2000 was chosen as starting material, after etherficiation by Williamson etherficiation reaction, acylation, conjugation with insulin to obtain the target compound. The molecule weight of the ligand was confirmed by MALDI-TOF.
Keywords:hepatic targeting drug  insulin receptor  ligand of liposome  synthesis
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