Synthesis of a lipid conjugate of SO3Le(a) and its enhancement on liposomal binding to activated platelets.
Synthesis of a lipid conjugate of SO3Le(a) and its enhancement on liposomal binding to activated platelets.
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SO3Le(a) 脂质缀合物的合成及其对脂质体与活化血小板结合的增强。
DOI：
10.1021/bc049805c
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发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Guo,Zhongwu
中科院分区：
文献类型：
--
作者：
Yan,Feng;Xue,Jie;Zhu,Junmin;Marchant,RogerE;Guo,Zhongwu
3 '-O-硫酸化莱亚（SO 3莱亚）是选择素的天然寡糖配体之一。SO 3Lea和E-/P-选择素之间的特异性相互作用在炎症过程中至关重要。本文报道了一种高效合成SO 3Lea脂质结合物的方法，并将其与磷脂和胆固醇结合，通过冻融和挤出法制备了SO 3Lea包被脂质体。所得糖脂体的大小（D= 78 nm）和稳定性与不含糖缀合物的脂质体相当。进一步观察到，由于糖脂体上的SO 3Lea与活化血小板上的P-选择素之间的特异性结合，将SO 3Lea掺入脂质体中可显著增强脂质体与活化血小板的粘附。糖脂体构建体可用于抗炎或用于将药物靶向递送至表达E-和P-选择素的内皮细胞。
3‘-O-Sulfated Lea(SO3Lea) is one of the most potent natural oligosaccharide ligands of selectins. The specific interactions between SO3Leaand E-/P-selectins are critical in the inflammation process. This paper described an efficient synthesis of a lipid conjugate of SO3Leaand its combination with phospholipid and cholesterol to form SO3Lea-coated liposomes by the freeze-thaw and extrusion method. The size (D= 78 nm) and stability of the resultant glycoliposomes were comparable to that of liposomes without the glycoconjugate. It was further observed that the incorporation of SO3Leainto liposomes could significantly enhance their adhesion to activated platelets as a result of the specific binding between SO3Leaon the glycoliposome and the P-selectin on activated platelets. The glycoliposome constructs may be useful for antiinflammation or for targeted delivery of drugs to endothelial cells that express E- and P-selectins.