Tomita M, Hayashi M, Horie T, Ishizawa T, Awazu S
Department of Biopharmaceutics, Tokyo College of Pharmacy, Japan.
Pharm Res. 1988 Dec;5(12):786-9. doi: 10.1023/a:1015992819290.
The effects of sodium caprate and sodium caprylate on transcellular permeation routes were examined in rats. The release of membrane phospholipids was significantly increased only by caprate, while protein release did not change from the control in the presence of caprate or caprylate, indicating that the extent of membrane disruption was insufficient to account for enhanced permeation. Using brush border membrane (BBM) vesicles prepared from colon, with their protein and lipid component labeled by fluorescent probes, the perturbing actions of caprate and caprylate toward the membrane were examined by fluorescence polarization. Caprate interacted with membrane protein and lipids, and caprylate mainly with protein, causing perturbation to the membrane. The release of 5(6)-carboxyfluorescein previously included in BBM vesicles was increased by caprate but not by caprylate. These results suggest that caprate enhances permeability via the transcellular route through membrane perturbation.
在大鼠中研究了癸酸钠和辛酸钠对跨细胞渗透途径的影响。仅癸酸盐显著增加了膜磷脂的释放，而在存在癸酸盐或辛酸盐的情况下，蛋白质释放与对照相比没有变化，这表明膜破坏程度不足以解释渗透增强的原因。使用从结肠制备的刷状缘膜（BBM）囊泡，其蛋白质和脂质成分用荧光探针标记，通过荧光偏振研究了癸酸盐和辛酸盐对膜的扰动作用。癸酸盐与膜蛋白和脂质相互作用，而辛酸盐主要与蛋白质相互作用，从而对膜造成扰动。先前包含在BBM囊泡中的5（6）-羧基荧光素的释放因癸酸盐而增加，但不因辛酸盐而增加。这些结果表明，癸酸盐通过膜扰动增强跨细胞途径的通透性。
