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用离子载体抗生素和亲脂性麻醉剂对红细胞膜流动性的扰动。

Perturbation of the fluidity of the erythrocyte membrane with ionophoric antibiotics and lipophilic anaesthetics.

作者信息

Abu-Salah K M

机构信息

Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.

出版信息

Biochem Pharmacol. 1991 Oct 24;42(10):1947-51. doi: 10.1016/0006-2952(91)90594-u.

Abstract

The fluidity of the rat erythrocyte membrane was evaluated by measurement of excimer fluorescence of an intra-molecular forming fluorophore, 1,3-di(1-pyrenyl)propane. The polyene ionophoric antibiotics, amphotericin B and nystatin, were found to fluidize the erythrocyte membrane, as assessed by the increase in the excimer/monomer fluorescence intensity ratio, by 42 and 13%, respectively, compared with control samples. In contrast, of the peptide ionophoric antibiotics, valinomycin demonstrated about twice the effect which gramicidin A had on depressing the fluidity of the erythrocyte membrane. On the other hand, the general lipophilic anaesthetics, propanidid and althesin, led to an increase, by 70 and 32%, respectively, while the local anaesthetic, procaine, led to a decrease by 20%, in the fluidity of the erythrocyte membrane. These results were explained in the light of the partition coefficients determined for these drugs in decane and native membranes, their affinities for specific membrane components and the changes which they induce in the permeability properties of erythrocyte and other biological membranes.

摘要

通过测量分子内形成荧光团1,3 - 二(1 - 芘基)丙烷的准分子荧光来评估大鼠红细胞膜的流动性。发现多烯离子载体抗生素两性霉素B和制霉菌素可使红细胞膜流动性增加,通过准分子/单体荧光强度比的增加来评估,与对照样品相比,分别增加了42%和13%。相比之下,在肽类离子载体抗生素中,缬氨霉素对红细胞膜流动性的降低作用约为短杆菌肽A的两倍。另一方面,一般的亲脂性麻醉剂丙泮尼地和阿法沙龙分别使红细胞膜流动性增加70%和32%,而局部麻醉剂普鲁卡因使红细胞膜流动性降低20%。根据这些药物在正癸烷和天然膜中测定的分配系数、它们对特定膜成分的亲和力以及它们在红细胞和其他生物膜通透性特性中引起的变化来解释这些结果。

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