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奎尼丁是酸性磷脂双层有序性和流动性的强力扰动剂。

Quinidine is a strong perturber of acidic phospholipid bilayer order and fluidity.

作者信息

Surewicz W K

出版信息

Biochim Biophys Acta. 1982 Nov 8;692(2):315-8. doi: 10.1016/0005-2736(82)90536-3.

Abstract

The effect of an antiarrhythmic drug, quinidine, on the organization of model phospholipid membranes was studied by the spin-labeling technique. Quinidine strongly perturbs the molecular organization of lipid bilayers prepared from acidic phospholipids (phosphatidylserine, phosphatidic acid) and has only a slight effect on neutral phosphatidylcholine membranes. The interaction of the drug with acidic phospholipids manifests itself in a pronounced increase in the order parameter of the region close to the polar surface of the bilayer and in some decrease in its inner hydrocarbon core fluidity. It is suggested that the perturbation in the organization of membrane lipids may contribute to the mechanisms by which quinidine exerts its pharmacological effects.

摘要

采用自旋标记技术研究了抗心律失常药物奎尼丁对模型磷脂膜结构的影响。奎尼丁强烈干扰由酸性磷脂(磷脂酰丝氨酸、磷脂酸)制备的脂质双层的分子结构,而对中性磷脂酰胆碱膜只有轻微影响。该药物与酸性磷脂的相互作用表现为双层膜极性表面附近区域的序参数显著增加,其内部烃核流动性略有降低。有人认为,膜脂质结构的扰动可能有助于奎尼丁发挥其药理作用的机制。

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