Chahwala S B, Harpur E S
Res Commun Chem Pathol Pharmacol. 1982 Jan;35(1):63-78.
An investigation was made of the effect of aminoglycoside antibiotics on Na+-K+ ATPase to determine whether their toxicity might be attributable to an inhibition of this enzyme. Three preparations were used: human erythrocyte ghosts; microsomal fractions of the cortex and outer medulla of the guinea-pig kidney; rat isolated renal tubules. In all three preparations marked inhibition of Na+-K+ ATPase (50-100%) was seen only at very high concentrations of drug (10(-2)M). Although aminoglycoside antibiotics are known to accumulate to high concentrations in vivo, particularly in the renal cortex, it is argued that these findings suggest that an effect on Na+-K+ ATPase is unlikely to be their primary mechanism of toxicity.
对氨基糖苷类抗生素对钠钾ATP酶的作用进行了研究，以确定其毒性是否可能归因于对该酶的抑制作用。使用了三种制剂：人红细胞血影；豚鼠肾皮质和外髓质的微粒体部分；大鼠离体肾小管。在所有这三种制剂中，仅在非常高的药物浓度（10⁻²M）下才观察到钠钾ATP酶受到显著抑制（50 - 100%）。尽管已知氨基糖苷类抗生素在体内会蓄积至高浓度，尤其是在肾皮质中，但有人认为这些发现表明对钠钾ATP酶的作用不太可能是其主要毒性机制。
