Szögyi M, Cserháti T
Institute of Biophysics, Semmelweis University of Medicine, Budapest, Hungary.
J Pharm Biomed Anal. 1993 Jul;11(7):563-8. doi: 10.1016/0731-7085(93)80006-m.
The effect of 17 monoamine oxidase inhibitory drugs (propargylamine derivatives) on the phase transition parameters of some synthetic phospholipids has been studied by differential scanning calorimetry. The drugs modified the thermal behaviour of phospholipids proving the existence of phospholipid-drug interactions. Phosphatidylethanolamine, phosphatidylcholine and phosphatidic acid equally interact with the monoamine oxidase inhibitory drugs. Significant correlations were found between the change of the phase transition parameters of phospholipids and the hydrophilic and hydrophobic molecular parameters of drugs. Calculations suggest that both hydrophilic (between the head group of phospholipids and the polar propargylamine group of drugs) and hydrophobic (between the apolar fatty acid chains of phospholipids and the lipophilic substructures of drugs) forces are involved in the phospholipid-drug interaction. Chloro substitution in the hydrophobic moiety of drugs enhances considerably the strength of interaction.
通过差示扫描量热法研究了17种单胺氧化酶抑制药物（炔丙胺衍生物）对某些合成磷脂相变参数的影响。这些药物改变了磷脂的热行为，证明了磷脂与药物之间存在相互作用。磷脂酰乙醇胺、磷脂酰胆碱和磷脂酸与单胺氧化酶抑制药物的相互作用相同。发现磷脂相变参数的变化与药物的亲水和疏水分子参数之间存在显著相关性。计算表明，磷脂与药物的相互作用涉及亲水作用力（磷脂的头部基团与药物的极性炔丙胺基团之间）和疏水作用力（磷脂的非极性脂肪酸链与药物的亲脂性亚结构之间）。药物疏水部分的氯取代显著增强了相互作用的强度。
