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游离脂肪酸对脂质体对咪唑类抗真菌药物敏感性的影响。

Effect of free fatty acids on liposome susceptibility to imidazole antifungals.

作者信息

Sud I J, Chou D L, Feingold D S

出版信息

Antimicrob Agents Chemother. 1979 Nov;16(5):660-3. doi: 10.1128/AAC.16.5.660.

Abstract

The presence of free fatty acids in liposome model membranes sensitizes these membranes to the action of the imidazole antifungals, clotrimazole, micronazole, and sulconazole. Unsaturation of the fatty acids is an important variable; the effect of linoleic and oleic acids is much greater than that of stearic acid. The imidazoles differ somewhat in action, with clotrimazole potency greatest both on membranes with and without fatty acids. Sulconazole has very little activity on membranes without fatty acids even at the highest concentrations tested. The data are discussed with reference to the susceptibility of various cells to the imidazoles and the specificity of imidazole action. A modification of the enzymatic method generally used for assay of marker glucose with liposome systems is also presented.

摘要

脂质体模型膜中游离脂肪酸的存在使这些膜对咪唑类抗真菌药(克霉唑、咪康唑和硫康唑)的作用敏感。脂肪酸的不饱和程度是一个重要变量;亚油酸和油酸的作用远大于硬脂酸。咪唑类药物的作用略有不同,克霉唑在有脂肪酸和无脂肪酸的膜上效力均最强。即使在测试的最高浓度下,硫康唑对无脂肪酸的膜也几乎没有活性。结合各种细胞对咪唑类药物的敏感性和咪唑类作用的特异性对数据进行了讨论。还介绍了一种对脂质体系统中通常用于测定标记葡萄糖的酶法的改进方法。

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