硫酸化岩藻糖基化抗原（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作用。
Synthesis of a lipid conjugate of SO3Le(a) and its enhancement on liposomal binding to activated platelets.
作者信息
Yan Feng, Xue Jie, Zhu Junmin, Marchant Roger E, Guo Zhongwu
机构信息
Department of Chemistry, Case Western Reserve University, 10900 Euclid Avenue, Cleveland, Ohio 44106, USA.
出版信息
Bioconjug Chem. 2005 Jan-Feb;16(1):90-6. doi: 10.1021/bc049805c.
3'-O-Sulfated Le(a) (SO3Le(a)) is one of the most potent natural oligosaccharide ligands of selectins. The specific interactions between SO3Le(a) and E-/P-selectins are critical in the inflammation process. This paper described an efficient synthesis of a lipid conjugate of SO3Le(a) and its combination with phospholipid and cholesterol to form SO3Le(a)-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 SO3Le(a) into liposomes could significantly enhance their adhesion to activated platelets as a result of the specific binding between SO3Le(a) on 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.
3'-O-硫酸化Le(a)（SO3Le(a)）是选择素最有效的天然寡糖配体之一。SO3Le(a)与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。本文描述了一种高效合成SO3Le(a)脂质缀合物的方法，以及通过冻融和挤压法将其与磷脂和胆固醇结合形成SO3Le(a)包被脂质体的过程。所得糖脂质体的大小（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，由于糖脂质体上的SO3Le(a)与活化血小板上的P-选择素之间的特异性结合，将SO3Le(a)掺入脂质体可显著增强其对活化血小板的粘附。糖脂质体构建体可能有助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。
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