Suwalsky M, Sánchez I, Neira F
Faculty of Chemical Sciences, University of Concepción, Chile.
Z Naturforsch C J Biosci. 1993 Nov-Dec;48(11-12):930-8. doi: 10.1515/znc-1993-11-1217.
Asocainol (ASOC) belongs to class I of the antiarrhythmic drugs, i.e., those that exert their action at the level of the sodium channels of the myocardial cell membrane. It has been suggested that their molecular mechanism of action might be through nonspecific interactions with phospholipids that surround the channel proteins. In order to test this hypothesis, ASOC was made to interact with two multibilayer systems, one built-up of dimyristoylphosphatidylcholine (DMPC) and the other of dimyristoylphosphatidylethanolamine (DMPE). These are the type of lipids that are respectively found in the outer and inner monolayers of human erythrocytes. The experiments were carried out in a hydrophobic as well as in a hydrophilic medium below the phospholipid main transition temperatures. The perturbing effect of ASOC upon the bilayer structures was determined by X-ray diffraction. It was found that ASOC was able to fluidize DMPC in both media but not to DMPE.
阿索卡诺（ASOC）属于抗心律失常药物的I类，即那些在心肌细胞膜钠通道水平发挥作用的药物。有人提出，它们的分子作用机制可能是通过与围绕通道蛋白的磷脂进行非特异性相互作用。为了验证这一假设，使ASOC与两个多层系统相互作用，一个由二肉豆蔻酰磷脂酰胆碱（DMPC）构成，另一个由二肉豆蔻酰磷脂酰乙醇胺（DMPE）构成。这些是分别存在于人类红细胞外层和内层单分子层中的脂质类型。实验在低于磷脂主要转变温度的疏水和亲水介质中进行。通过X射线衍射确定了ASOC对双层结构的扰动作用。结果发现，ASOC在两种介质中都能使DMPC流化，但不能使DMPE流化。
