EFFECTS OF SALICYLIC-ACID ON THE PERMEABILITY OF THE PLASMA-MEMBRANE OF THE SMALL-INTESTINE OF THE RAT - A FLUORESCENCE SPECTROSCOPIC APPROACH TO ELUCIDATE THE MECHANISM OF PROMOTED DRUG ABSORPTION
EFFECTS OF SALICYLIC-ACID ON THE PERMEABILITY OF THE PLASMA-MEMBRANE OF THE SMALL-INTESTINE OF THE RAT - A FLUORESCENCE SPECTROSCOPIC APPROACH TO ELUCIDATE THE MECHANISM OF PROMOTED DRUG ABSORPTION
复制标题
DOI：
10.1002/jps.2600750511
复制
发表时间：
1986-05-01
影响因子：
3.8
通讯作者：
AWAZU, S
中科院分区：
文献类型：
--
作者：
KAJII, H;HORIE, T;AWAZU, S
水杨酸钠对 1,6-二苯基-1,3,5-己三烯 (DPH)、2-羟基十八烷酸、9-蒽甲酸盐 (2-AS)、12-羟基十八烷酸、9-蒽甲酸盐 (12-AS)、8-苯胺基-1-萘磺酸 (ANS) 荧光偏振的影响 检测标记大鼠小肠刷状缘膜囊泡的2'',4'',5'',7''-四溴-5-马来酰亚胺荧光素二钠盐(EM)。水杨酸离子降低了这些囊泡中ANS和EM的荧光偏振，但对DPH、2-AS和12-AS标记囊泡的荧光偏振没有影响。它还从囊泡中释放了捕获的 6-羧基荧光素（3'',6''-二羟基-3-氧代螺-[邻苯二甲酸-1,9''-呫吨]-6-羧酸）（CF），但没有导致捕获的 CF 从脂质体中泄漏。这些结果表明水杨酸离子通过影响质膜蛋白而不是直接与膜脂相互作用来增加质膜通透性。水杨酸离子对这些囊泡的作用可能会促进体内不可吸收药物的吸收。
The effects of sodium salicylate on the fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH), 2-hydroxyoctadecanoic acid, 9-anthroate (2-AS), 12-hydroxyoctadecanoic acid, 9-anthroate (12-AS), 8-anilino-1-naphthalenesulfonic acid (ANS) and 2'',4'',5'',7''-tetrabromo-5-maleimidofluorescein, disodium salt (EM), with which rat small intestinal brush border membrane vesicles were labeled, were examined. Salicylate ion decreased the fluorescence polarization of ANS and EM in these vesicles, however, it had no influence on the fluorescence polarization of DPH, 2-AS and 12-AS-labeled vesicles. It also released trapped 6-carboxyfluorescein (3'',6''-dihydroxy-3-oxospiro-[phthalan-1,9''-xanthene]-6-carboxylic acid) (CF) from the vesicles, but caused no leakage of trapped CF from liposomes. These results indicate that salicylate ion increases the plasma membrane permeability by effecting the plasma membrane proteins rather than directly interacting with the membrane lipids. The action of salicylate ion on these vesicles could possibly promote nonabsorbable drug absorption in vivo.