Suwalsky M, Villena F, Bagnara M, Sotomayor C P
Faculty of Chemical Sciences, University of Concepción, Chile.
Z Naturforsch C J Biosci. 1995 Jul-Aug;50(7-8):527-34. doi: 10.1515/znc-1995-7-810.
Quinidine (QUIN) is one of the most important and efficient antiarrhythmic drugs (AAD). It belongs to class I, which are the drugs that exert their action at the level of the sodium channels in the membrane of the myocard. Several hypotheses support the idea that the molecular mechanism of action of the AAD is via nonspecific interactions with phospholipids sited in the neighborhood of the channels. In order to probe the validity of these hypotheses, QUIN was made to interact with the phospholipids dimyristoylphosphadidylcholine (DMPC) and dimyristoylphosphatidylethanolamine (DMPE). These interactions were performed in a hydrophobic and a hydrophilic medium under a wide range of molar ratios. The resulting products were analyzed by X-ray diffraction. QUIN solutions were also made to interact with DMPC liposomes, which were studied by fluorescent spectroscopy. Finally, human erythrocytes which were incubated with QUIN solutions were observed by scanning electron microscopy. The results of these experiments proved that QUIN indeed interacted with phospholipid bilayers.
奎尼丁（QUIN）是最重要且有效的抗心律失常药物（AAD）之一。它属于I类药物，这类药物在心肌细胞膜的钠通道水平发挥作用。有几种假说支持抗心律失常药物的分子作用机制是通过与通道附近的磷脂发生非特异性相互作用这一观点。为了探究这些假说的有效性，使奎尼丁与磷脂二肉豆蔻酰磷脂酰胆碱（DMPC）和二肉豆蔻酰磷脂酰乙醇胺（DMPE）相互作用。这些相互作用在疏水和亲水介质中于广泛的摩尔比下进行。通过X射线衍射分析所得产物。还使奎尼丁溶液与DMPC脂质体相互作用，并通过荧光光谱法对其进行研究。最后，通过扫描电子显微镜观察用奎尼丁溶液孵育的人红细胞。这些实验结果证明奎尼丁确实与磷脂双层发生了相互作用。
