脑靶向脂质体配体葡萄糖-胆甾偶联物的设计与合成
Design and synthesis of glucose-cholesterol as ligand for brain targeting liposomes
作者：李海姣;樊维;李贤坤;余永国;吴勇;
Author：
收稿日期： 年卷（期）页码：2010,25(03):-251-253
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：脑靶向;脂质体配体;葡萄糖-胆甾偶联物;葡萄糖转运蛋白1;合成
Key words：
基金项目：国家自然科学基金资助项目(批准号:30672537)
中文摘要
目的合成具有酯水两性的脑靶向脂质体配体葡萄糖-胆固醇偶联物。方法将胆固醇3位羟基与对甲苯磺酰氯成酯后,与乙二醇取代,并氧化制得2-(5-胆甾烯-3-β-氧基)-1-乙酸,再与1,2,3,4-四-O-三甲硅基-β-D-吡喃葡萄糖在缩合剂DCC的作用下成酯,由三氟乙酸四氢呋喃溶液脱保护后得到目标配体。结果合成了1个葡萄糖胆甾偶联物。结论目标化合物以及重要中间体均经IR、1HNMR、MS等确证。
英文摘要
[1]Begley DJ.Understanding and circumventing the blood-brain barrier[J].Cta Paediatr Supp,2003,92:83-91.
[2]William MP.Blood-brain barrier drug targeting:the future of brain drug development[J].Mol Intervention,2003,3:90-105.
[3]Brightman MW.Blood-brain barrier delivery[J].Drug DiscToday,2007,12:54-61.
[4]Manna JCL,Harik SI.Regional comparisons of brain glucose in-flux[J].Brain Res,1985,326:299-305.
[5]Caridad F,Ofelia N,Emilia R.Synthesis and biological studies of glycosyl dopamine derivatives as potential antiparkinsonian agents[J].Carbohydr Res,2000,327:353-365.
[6]Therese H,Monique S,Kostas A,et al.Synthesis of O-methyl-sulfonyl derivatives of-glucose as potential alkylating agents for targeted drug delivery to the brain.Evaluation of their interaction with the human erythrocyte GLUT1hexose transporter[J].Carbo-hydr Res,1997,299:15-21.
[7]Soon WA,Jung IJ,Dae CK,et al.Combined type liquid crystalline poly(oxy-1,4-phenyleneoxyterephthaloyl)s bearing cholesterol Pendants attached through polymethylene spacers[J].Macromole-cules,2001,34:5342.
[8]Bhattacharya S,Krishnan GY.Membrane formation from oxyethyl-ene bearing cationic cholesterol derivatives[J].Indian J Chem,Sect B,2001,10:891-894.
上一条：GC-MS分析东北玉簪中的超临界CO_2萃取物
下一条：一种基于硫胺素二硫化物传递系统的5-Fu脑靶向前药的合成
【关闭】
