Kitagawa Shuji, Hiyama Fuyuko, Kato Miwa, Watanabe Reiho
Nigata University of Pharmacy and Applied Life Sciences, Faculty of Pharmaceutical Sciences, Japan.
J Pharm Pharmacol. 2002 Jun;54(6):773-80. doi: 10.1211/0022357021779113.
We studied the interaction of double-chained cationic surfactants, dimethyldialkylammoniums, (CH3)2N+(CnH2n+1)2, with the lipid bilayer of guinea-pig erythrocytes by observing the haemolysis, aggregation and shape change in the erythrocytes. In the presence of sonicated dispersions of the five dimethyldialkylammoniums tested (n = 10, 12, 14, 16 and 18), haemolysis was induced dose dependently, and at 0.1 mM or higher concentrations, haemolysis was induced more rapidly by dimethyldialkylammoniums with shorter alkyl chains. The cationic surfactants with longer alkyl chains, such as dimethyldipalmitylammonium, induced aggregation of the erythrocytes before haemolysis fully progressed. The vesicles of these long-chain dimethyldialkylammoniums in the presence of phosphatidylcholines with unsaturated fatty acyl chains markedly reduced the haemolysis rates. Furthermore, in the presence of phosphatidylcholines with unsaturated acyl chains the formation of tightly aggregated structures of several erythrocytes was observed. These findings, and analysis by spin label 5-doxylstearic acid, indicate that phosphatidylcholines enriched with unsaturated acyl chains stabilize the cationic vesicles of long-chain dimethyldialkylammoniums and the interaction with the lipid bilayer of erythrocyte membranes as cationic vesicles became prominent.
我们通过观察豚鼠红细胞的溶血、聚集和形状变化，研究了双链阳离子表面活性剂二甲基二烷基铵（(CH3)2N+(CnH2n+1)2）与豚鼠红细胞脂质双层的相互作用。在所测试的五种二甲基二烷基铵（n = 10、12、14、16和18）的超声分散体存在下，溶血呈剂量依赖性诱导，并且在0.1 mM或更高浓度下，烷基链较短的二甲基二烷基铵诱导溶血的速度更快。具有较长烷基链的阳离子表面活性剂，如二甲基二棕榈酰铵，在溶血完全进展之前诱导红细胞聚集。这些长链二甲基二烷基铵的囊泡在含有不饱和脂肪酰链的磷脂酰胆碱存在下，显著降低了溶血速率。此外，在含有不饱和酰链的磷脂酰胆碱存在下，观察到几个红细胞形成紧密聚集的结构。这些发现以及通过自旋标记5-脱氧硬脂酸进行的分析表明，富含不饱和酰链的磷脂酰胆碱稳定了长链二甲基二烷基铵的阳离子囊泡，并且随着阳离子囊泡与红细胞膜脂质双层的相互作用变得突出。
