Vidal M, Sainte-Marie J, Philippot J R, Bienvenue A
EMBO J. 1985 Oct;4(10):2461-7. doi: 10.1002/j.1460-2075.1985.tb03957.x.
We describe a method for the covalent coupling of low-density lipoproteins (LDL) to the surface of small unilamellar vesicles, and the delivery of the liposome content to leukemic L2C lymphocytes in vitro. We demonstrate the stability of the linkage between LDL and liposomes, the preservation of vesicle integrity and the affinity of the LDL for their specific receptors after the coupling reaction. Hygromycin B, an impermeant inhibitor of protein synthesis, was encapsulated in the targeted liposomes, and delivered into the cytoplasm of leukemic L2C lymphocytes by the LDL pathway, as demonstrated by the lethal effect on cells measured by 51chromium-release assay.
我们描述了一种将低密度脂蛋白(LDL)共价偶联到小单层囊泡表面的方法,以及在体外将脂质体内容物递送至白血病L2C淋巴细胞的方法。我们证明了LDL与脂质体之间连接的稳定性、囊泡完整性的保留以及偶联反应后LDL对其特异性受体的亲和力。潮霉素B是一种蛋白质合成的非渗透性抑制剂,被包裹在靶向脂质体中,并通过LDL途径递送至白血病L2C淋巴细胞的细胞质中,这通过51铬释放试验测量的对细胞的致死作用得以证明。