Glubokovskaia O I, Kravchenko L S
Biokhimiia. 1979 Jan;44(1):160-5.
The effects of amphotericin B drug containing sodium deoxycholate (DOC) and those of DOC and nistatin on the activities of Na+, K+-ATPase and 5'-nucleotidase of canine kidney plasma membranes were studied. It was found that the activities of Na+, K+-ATPase and 5'-nucleotidase were markedly inhibited only after intravenous injection of amphotericin B, whereas the other agents tested caused no changes in the enzyme activities. Similar results were obtained in vitro. In the presence of amphotericin B the activity of Na+, K+-ATPase was noticeably inhibited already at the antibiotic concentration of 0,1 mkg per mg of membrane protein. It was found that the injection of amphotericin B, DOC and nistatin did not qualitatively or quantitatively affect the phospholipid composition of the plasma membranes. This is indicative of the lack of correlation between the enzyme activities and changes in the phospholipid composition of the plasma membranes under effects of amphotericin B. The pyrimidine derivative--amygluracyl--markedly removes the inhibiting effect of amphotericin B on the enzyme activity of plasma membranes.
研究了含脱氧胆酸钠(DOC)的两性霉素B以及DOC和制霉菌素对犬肾质膜Na⁺,K⁺-ATP酶和5'-核苷酸酶活性的影响。结果发现,仅在静脉注射两性霉素B后,Na⁺,K⁺-ATP酶和5'-核苷酸酶的活性才受到显著抑制,而所测试的其他药物对酶活性没有影响。体外实验也得到了类似结果。在存在两性霉素B的情况下,当抗生素浓度达到每毫克膜蛋白0.1微克时,Na⁺,K⁺-ATP酶的活性就已受到明显抑制。研究发现,注射两性霉素B、DOC和制霉菌素对质膜的磷脂组成在定性或定量方面均无影响。这表明在两性霉素B的作用下,酶活性与质膜磷脂组成的变化之间缺乏相关性。嘧啶衍生物——阿米格鲁酰——能显著消除两性霉素B对质膜酶活性的抑制作用。