Surewicz W K, Jozwiak Z
Biochem Pharmacol. 1983 May 1;32(9):1467-71. doi: 10.1016/0006-2952(83)90467-7.
The influence of an antiarrhythmic drug, quinidine, on the physical state of membrane phospholipids was investigated using model membranes, liposomes. Turbidimetric measurements on liposomes prepared from neutral (dipalmitoyl phosphatidylcholine) and acidic (dipalmitoyl phosphatidic acid) phospholipids showed that quinidine reduces the temp of the gel to liquid-crystalline phase transition and broadens the temp range of the transition. The effect of quinidine on the thermal behaviour of model membranes depends on both the pH and the type of phospholipids used. It is markedly stronger for acidic than for neutral phospholipids, suggesting the importance of electrostatic effects in drug-membrane interaction. The ability of quinidine to interact with the lipid bilayer was confirmed by permeability measurements with the use of a self-quenched fluorescent compound, calcein. It is suggested that quinidine-phospholipid interaction may contribute to the mechanisms by which the drug exerts its physiological and pharmacological effects.
使用模型膜脂质体研究了抗心律失常药物奎尼丁对膜磷脂物理状态的影响。对由中性（二棕榈酰磷脂酰胆碱）和酸性（二棕榈酰磷脂酸）磷脂制备的脂质体进行的比浊测量表明，奎尼丁降低了凝胶到液晶相转变的温度，并拓宽了转变的温度范围。奎尼丁对模型膜热行为的影响取决于pH值和所用磷脂的类型。对于酸性磷脂，其作用明显强于中性磷脂，这表明静电效应在药物与膜相互作用中很重要。通过使用自猝灭荧光化合物钙黄绿素进行渗透性测量，证实了奎尼丁与脂质双层相互作用的能力。有人提出，奎尼丁与磷脂的相互作用可能有助于药物发挥其生理和药理作用的机制。
