Umeki S
Department of Medicine, Toshida-Kai Kumeda Hospital, Osaka, Japan.
Comp Biochem Physiol B Biochem Mol Biol. 1995 Apr;110(4):817-21. doi: 10.1016/0305-0491(94)00203-7.
The effects of gentamycin on the NADPH oxidase (EC 1.6.99.6) from human neutrophils in both whole-cell and fully soluble (cell-free) systems were investigated. Gentamycin was found to inhibit, concentration-dependently, the superoxide generation of neutrophils exposed to phorbol myristate acetate in a whole-cell system and the activation of superoxide-generating NADPH oxidase by sodium dodecyl sulfate in a cell-free system. The concentrations of the drug required for 50% inhibition of the oxidase (IC50) were 150 microM in the whole-cell system and 10 microM in the cell-free system. In addition, in the cell-free system, the drug did not change the Km value for NADPH of the oxidase. However, gentamycin did not the superoxide generation of NADPH oxidase after its activation in the cell-free system, suggesting that the drug do not have superoxide-scavenger action. These results suggest that gentamycin, an aminoglycoside antibiotic, may exhibit an anti-inflammatory action due to inhibition of neutrophil NADPH oxidase activation.
研究了庆大霉素在全细胞和完全可溶（无细胞）系统中对人中性粒细胞NADPH氧化酶（EC 1.6.99.6）的影响。发现在全细胞系统中，庆大霉素浓度依赖性地抑制暴露于佛波醇肉豆蔻酸酯乙酸盐的中性粒细胞的超氧化物生成；在无细胞系统中，庆大霉素抑制十二烷基硫酸钠对超氧化物生成型NADPH氧化酶的激活。在全细胞系统中抑制氧化酶50%（IC50）所需的药物浓度为150微摩尔，在无细胞系统中为10微摩尔。此外，在无细胞系统中，该药物并未改变氧化酶对NADPH的Km值。然而，庆大霉素在无细胞系统中激活后，并不会影响NADPH氧化酶的超氧化物生成，这表明该药物不具有超氧化物清除作用。这些结果表明，氨基糖苷类抗生素庆大霉素可能由于抑制中性粒细胞NADPH氧化酶激活而表现出抗炎作用。
