Ruifrok P G, Meijer D K
Naunyn Schmiedebergs Arch Pharmacol. 1981 Jun;316(3):266-72. doi: 10.1007/BF00505661.
The transport of a series of charged drugs and other organic ions through lipid bilayers was studied, using single-bilayer liposomes. Monovalent organic cations and organic anions could carry charge into the liposomes independent of the nature of their counter ion. Ion-pair formation, following the addition of an excess of I- or Br-, did not facilitate this transport. However the passage of organic cations and anions across the membrane required the presence of the organic anion tetraphenylborate in the lipid bilayer. This effect of tetraphenylborate is probably due to a lowering of an intra-membrane potential energy hill, the principal barrier for transport, and not to ion-pair formation. It is concluded that organic ions that possess sufficiently lipophilic structures to mask their charged character, can pass lipid bilayers in charged form.
使用单层脂质体研究了一系列带电药物和其他有机离子通过脂质双层的运输。单价有机阳离子和有机阴离子可将电荷带入脂质体,而与它们的抗衡离子的性质无关。加入过量的I-或Br-后形成离子对并不能促进这种运输。然而,有机阳离子和阴离子穿过膜需要脂质双层中存在有机阴离子四苯基硼酸盐。四苯基硼酸盐的这种作用可能是由于降低了膜内势能势垒,这是运输的主要障碍,而不是由于离子对的形成。得出的结论是,具有足够亲脂性结构以掩盖其带电特性的有机离子可以以带电形式穿过脂质双层。