己二醇桥联胆甾半乳糖苷的合成
Synthesis of amphiphilic cholesterylated galactosides for hepatocyte targeting liposome
作者：范江;海俐;唐磊;吴勇;
Author：
收稿日期： 年卷（期）页码：2006,(05):-419-421
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：肝靶向;胆甾半乳糖苷衍生物;合成
Key words：
基金项目：教育部博士点基金(批准号:20050610085)
中文摘要
目的合成具有脂水两性的肝靶向脂质体配体胆甾半乳糖苷衍生物。方法将胆固醇3位羟基与己二醇的双甲磺酸酯成醚后再碘代,随后与2,3,4,6-四-O-乙酰基-1-硫代-β-D-吡喃半乳糖成硫醚得到糖苷,经甲醇钠处理脱掉乙酰基得目标物。结果合成了1个胆甾半乳糖苷衍生物。结论合成衍生物及中间体的结构经1HNMR、IR、MS确证。
参考文献
[1]Audouy SAL,Lou FMH,LeijH,et al.In vivocharacteristics ofcation ic liposom es as delivery vectors for gene therapy[J].PharmRes,2002,19(11):1599-1605.
[2]Kawakam i S,Yamash ita F,N ish ikawaM,et a.l Asialoglycopro-tein receptor-m ed iated gene transfer using novel galactosylatedcation ic liposom es[J].B iochem and B iophys Res Commun,1998,252(1):78-83.
[3]Hai L,Sun X,W u Y,et a.l Synthesis of amph iph ilic hepatocytetargeting cholesterylated th iogalactosides[J].Ch in Chem Let,2005,16(8):1021-1023.
[4]Sun X,Hai L,W u Y,et al.Targeted gene delivery to hepatomacells using galactosylated liposom e-polycation-DNA comple-xes(LPD)[J].J D rug Target,2005,13(2):121-128.
[5]Stocker R J.The asialoglycoprotein receptor relationsh ips betweenstructure,function,and expression[J].Physiol Rev,1995,75(3):591-633.
[6]Roelen HCPF,B ijsterbosch MK,Bakkeren HF,et a.l W ater-solub le cholesteryl-contain ing phosphoroth ioate monogalacto-sides:synthesis,properties,and use in lowering b lood cholester-ol by d irecting plasma proteins to the liver[J].J M ed Chem,1991,34(11):1036-1042.
[7]L i Y,Hesse Manfred.The syntheses of cyclic sperm ine alka-loids:analogues of buchnerine and budmunch ia-m ine C[J].Helvetica Ch im ica Acta,2003,86(2):310-323.
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