The inhibition of the enzyme acetylcholinesterase (AChE) is a frequently used therapeutic option to treat Alzheimer's disease (AD). By decreasing the levels of acetylcholine degradation in the synaptic space, some cognitive functions of patients suffering from this disease are significantly improved. Rivastigmine is one of the most widely used AChE inhibitors. The objective of this work was to determine the effects of this drug on human erythrocytes, which have a type of AChE in the cell membrane. To that end, human erythrocytes and molecular models of its membrane constituted by dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidylethanolamine (DMPE) were used. They correspond to classes of phospholipids present in the outer and inner monolayers of the human erythrocyte membrane, respectively. The experimental results obtained by X-ray diffraction and differential scanning calorimetry (DSC) indicated that rivastigmine molecules were able to interact with both phospholipids. Fluorescence spectroscopy results showed that rivastigmine produce a slight change in the acyl chain packing order and a weak displacement of the water molecules of the hydrophobic-hydrophilic membrane interface. On the other hand, observations by scanning electron microscopy (SEM) showed that the drug changed the normal biconcave shape of erythrocytes in stomatocytes (cup-shaped cells) and echinocytes (speculated shaped).

中文翻译：

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抗阿尔茨海默病药物利凡斯的明与人红细胞相互作用的体外研究。

抑制乙酰胆碱酯酶（AChE）的酶是治疗阿尔茨海默氏病（AD）的常用方法。通过降低突触空间中乙酰胆碱降解的水平，患有该疾病的患者的某些认知功能得到了显着改善。Rivastigmine是最广泛使用的AChE抑制剂之一。这项工作的目的是确定这种药物对人红细胞的影响，后者在细胞膜中具有一种AChE。为此，使用了人红细胞及其膜的分子模型，其由二肉豆蔻酰基磷脂酰胆碱（DMPC）和二肉豆蔻酰基磷脂酰乙醇胺（DMPE）组成。它们分别对应于人类红细胞膜的外单层和内单层中存在的磷脂类别。通过X射线衍射和差示扫描量热法（DSC）获得的实验结果表明，卡巴拉汀分子能够与两种磷脂相互作用。荧光光谱结果表明，卡巴拉汀在酰基链堆积顺序上产生微小变化，并且疏水-亲水膜界面的水分子位移较弱。另一方面，通过扫描电子显微镜（SEM）的观察表明，该药物改变了口气细胞（杯状细胞）和棘突细胞（推测形状）中红细胞的正常双凹形状。荧光光谱结果表明，卡巴拉汀在酰基链堆积顺序上产生微小变化，并且疏水-亲水膜界面的水分子位移较弱。另一方面，通过扫描电子显微镜（SEM）的观察表明，该药物改变了口气细胞（杯状细胞）和棘突细胞（推测形状）中红细胞的正常双凹形状。荧光光谱结果表明，卡巴拉汀在酰基链堆积顺序上产生微小变化，并且疏水-亲水膜界面的水分子位移较弱。另一方面，通过扫描电子显微镜（SEM）的观察表明，该药物改变了口气细胞（杯状细胞）和棘突细胞（推测形状）中红细胞的正常双凹形状。