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抗炎药物双氯芬酸对人红细胞的体外结构效应及细胞膜分子模型

Structural effects in vitro of the anti-inflammatory drug diclofenac on human erythrocytes and molecular models of cell membranes.

作者信息

Suwalsky Mario, Manrique Marcela, Villena Fernando, Sotomayor Carlos P

机构信息

University of Concepción, Chile.

出版信息

Biophys Chem. 2009 Apr;141(1):34-40. doi: 10.1016/j.bpc.2008.12.010. Epub 2008 Dec 31.

Abstract

Diclofenac, a nonsteroidal anti-inflammatory drug (NSAID), has been widely investigated in terms of its pharmacological action, but less is known about its effects on cell membranes and particularly on those of human erythrocytes. In the present work, the structural effects on the human erythrocyte membrane and molecular models have been investigated and reported. This report presents the following evidence that diclofenac interacts with red cell membranes: a) X-ray diffraction and fluorescence spectroscopy of phospholipid bilayers showed that diclofenac interacted with a class of lipids found in the outer moiety of the erythrocyte membrane; b) in isolated unsealed human erythrocyte membranes (IUM) the drug induced a disordering effect on the acyl chains of the membrane lipid bilayer; c) in scanning electron microscopy (SEM) studies on human erythrocytes it was observed that the drug induced changes different from the normal biconcave morphology of most red blood cells. This is the first time in which structural effects of diclofenac on the human erythrocyte membrane have been described.

摘要

双氯芬酸是一种非甾体抗炎药(NSAID),人们已对其药理作用进行了广泛研究,但对其对细胞膜尤其是对人类红细胞膜的影响却知之甚少。在本研究中,已对双氯芬酸对人类红细胞膜的结构影响及分子模型进行了研究并予以报道。本报告提供了以下证据证明双氯芬酸与红细胞膜相互作用:a)磷脂双层的X射线衍射和荧光光谱显示双氯芬酸与红细胞膜外层发现的一类脂质相互作用;b)在分离的未密封人类红细胞膜(IUM)中,该药物对膜脂质双层的酰基链产生了无序化作用;c)在对人类红细胞的扫描电子显微镜(SEM)研究中观察到,该药物诱导的变化不同于大多数红细胞正常的双凹形态。这是首次描述双氯芬酸对人类红细胞膜的结构影响。

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