Lasfargues A, Charon D, Trigalo F, Ledur A, Szabo L, Chaby R
Cell Immunol. 1986 Mar;98(1):8-17. doi: 10.1016/0008-8749(86)90262-5.
Informations on the structural features implicated in the macrophage-dependent cytostatic activity of "lipid A" preparations were obtained by the use of 15 synthetic glycolipids. Four structural requirements were identified: the presence of a reducing glucosamine unit; the presence of a free hydroxyl group on amide-linked 3-hydroxytetradecanoic acids, and the absence of free hydroxyl groups at positions 3 and 6 of the glucosamine. The monosaccharide resembling the reducing unit of the "lipid A backbone," which fulfills these criteria, had the highest cytostatic activity, whereas the compound possessing the substitution pattern of the nonreducing moiety was inactive.
通过使用15种合成糖脂,获得了与“脂质A”制剂的巨噬细胞依赖性细胞生长抑制活性相关的结构特征信息。确定了四个结构要求:存在还原性葡糖胺单元;酰胺连接的3-羟基十四烷酸上存在游离羟基,且葡糖胺的3位和6位不存在游离羟基。符合这些标准的类似于“脂质A主链”还原性单元的单糖具有最高的细胞生长抑制活性,而具有非还原性部分取代模式的化合物则无活性。