Dumont S, Muller C D, Schuber F, Bartholeyns J
Département d'Immunologie et d'Immunopharmacologie, UER de Pharmacie, Université Louis Pasteur, Illkirch-Graffenstaden, France.
Anticancer Res. 1990 Jan-Feb;10(1):155-60.
Neo-mannosylated liposomes have been prepared by coupling a mannose derivative bearing a hydrophilic spacer arm to preformed large unilamellar liposomes containing 4-(p-maleimidophenyl) butyryl-phosphatidylethanolamine. Lipopolysaccharide (LPS) was encapsulated in normal or neo-mannosylated liposomes; the neo-mannosylated vesicles showed specificity for the in vitro activation to toxicity of macrophages only in the case of differentiated macrophages presenting mannose receptors at their surface. In vivo, LPS entrapped in neo-mannosylated vesicles showed a reduced toxicity for animals hypersensitive to LPS. Moreover targeting of LPS to tissue macrophages with neo-mannosylated liposomes induced regression of experimental solid tumors in mice (EMT6 sarcoma, 3LL carcinoma) and was effective on lung metastases.
通过将带有亲水性间隔臂的甘露糖衍生物偶联到含有4-（对-马来酰亚胺苯基）丁酰磷脂酰乙醇胺的预制大单层脂质体上，制备了新甘露糖基化脂质体。脂多糖（LPS）被包裹在正常或新甘露糖基化脂质体中；仅在表面呈现甘露糖受体的分化巨噬细胞的情况下，新甘露糖基化囊泡对巨噬细胞体外激活毒性具有特异性。在体内，包裹在新甘露糖基化囊泡中的LPS对LPS过敏的动物毒性降低。此外，用新甘露糖基化脂质体将LPS靶向组织巨噬细胞可诱导小鼠实验性实体瘤（EMT6肉瘤、3LL癌）消退，并对肺转移有效。
