Mauceri Alessandro, Borocci Stefano, Galantini Luciano, Giansanti Luisa, Mancini Giovanna, Martino Antonio, Salvati Manni Livia, Sperduto Claudio
Dipartimento di Chimica, Università degli Studi di Roma "Sapienza" , P.le A. Moro 5, 00185 Roma, Italy.
Langmuir. 2014 Sep 30;30(38):11301-6. doi: 10.1021/la502946t. Epub 2014 Sep 16.
The specificity of carbohydrate-lectin interaction has been reported as an attractive strategy for drug delivery in cancer therapy because of the high levels of lectins in several human malignancies. A novel cationic glucosylated amphiphile was therefore synthesized, as a model system, to attribute specificity toward d-glucose receptors to liposome formulations. Fluorescence experiments demonstrated that the monomeric glucosylated amphiphile is capable of interacting with fluorescently labeled concanavalin A, a D-glucose specific plant lectin. The interaction of concanavalin A with liposomes composed of a phospholipid and the glucosylated amphiphile was demonstrated by agglutination observed by optical density and dynamic laser light scattering measurements, thus paving the way to the preparation of other glycosilated amphiphiles differing for the length of polyoxyethylenic spacer, the sugar moieties, and/or the length of the hydrophobic chain.
由于几种人类恶性肿瘤中凝集素水平较高,碳水化合物-凝集素相互作用的特异性已被报道为癌症治疗中药物递送的一种有吸引力的策略。因此,合成了一种新型阳离子糖基化两亲物作为模型系统,以使脂质体制剂对d-葡萄糖受体具有特异性。荧光实验表明,单体糖基化两亲物能够与荧光标记的伴刀豆球蛋白A(一种D-葡萄糖特异性植物凝集素)相互作用。通过光密度和动态激光光散射测量观察到的凝集作用,证明了伴刀豆球蛋白A与由磷脂和糖基化两亲物组成的脂质体之间的相互作用,从而为制备其他在聚氧乙烯间隔长度、糖部分和/或疏水链长度方面不同的糖基化两亲物铺平了道路。