Hiruma R, Yamaguchi A, Sawai T
FEBS Lett. 1984 May 21;170(2):268-72. doi: 10.1016/0014-5793(84)81326-5.
The lipid-bilayer permeability of cephalosporins was extensively suppressed by addition of lipopolysaccharide to liposomal membrane in proportion to the hydrophobicity of the drugs. This suggests that the polysaccharide chain layer contributes to the barrier function. The importance of the polysaccharide chain in the barrier function was also supported by the fact that the permeability to Rd-type lipopolysaccharide-containing liposomes showed essentially the same dependency on the hydrophobicity of the cephalosporins as that of the lipopolysaccharide-free liposomes. In this case the permeability of the cephalosporins was proportional to their hydrophobicity. Similar lipopolysaccharide effect was also observed in the permeation of penicillins.
通过向脂质体膜中添加脂多糖,头孢菌素的脂质双层通透性会根据药物的疏水性而被广泛抑制。这表明多糖链层有助于屏障功能。多糖链在屏障功能中的重要性也得到了以下事实的支持:对含Rd型脂多糖的脂质体的通透性对头孢菌素疏水性的依赖性与不含脂多糖的脂质体基本相同。在这种情况下,头孢菌素的通透性与其疏水性成正比。在青霉素的渗透中也观察到了类似的脂多糖效应。