Sastrasinh M, Weinberg J M, Humes H D
Life Sci. 1982 Jun 28;30(26):2309-15. doi: 10.1016/0024-3205(82)90258-2.
The effect of the nephrotoxic aminoglycoside antibiotic, gentamicin, on calcium uptake by renal cortical mitochondria was assessed in vitro. Gentamicin was found to be a competitive inhibitor of mitochondrial Ca++ uptake. This effect displayed a dose response with a Ki of 233 microM and occurred at gentamicin concentrations below those that inhibit mitochondrial electron transport. These results further demonstrate the potential for gentamicin to alter membrane function and thereby contribute to toxic cell injury via its interactions with divalent cations.
在体外评估了肾毒性氨基糖苷类抗生素庆大霉素对肾皮质线粒体摄取钙的影响。发现庆大霉素是线粒体摄取钙离子的竞争性抑制剂。这种作用呈现剂量反应,其抑制常数(Ki)为233微摩尔,且在低于抑制线粒体电子传递的庆大霉素浓度下就会出现。这些结果进一步证明了庆大霉素通过与二价阳离子相互作用改变膜功能并进而导致毒性细胞损伤的可能性。