Calcaterra N B, Vicario L R, Roveri O A
Centro de Estudios Fotosintéticos y Bioquímicos, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina.
Biochem Pharmacol. 1988 Jul 1;37(13):2521-7. doi: 10.1016/0006-2952(88)90241-9.
Suramin, a drug intensively used in the chemotherapy of African trypanosomiasis and onchocerciasis, is currently being tested in clinical trials for AIDS treatment. Its effects on mitochondrial energy metabolism in mammals were studied. At low concentrations it inhibited ATP synthesis and ATPase activity in submitochondrial particles, as well as ADP-stimulated oxygen consumption and the uncoupler-stimulated ATPase activity in intact rat liver mitochondria. At higher concentrations it also inhibited uncoupled electron transport in both submitochondrial particles and intact mitochondria. From comparison of the kinetic patterns of those inhibitions, evidence suggesting that the adenine nucleotide translocase may be another target for the action of suramin was obtained. The relevance of these findings to the understanding of the biochemical basis of suramin toxicity is discussed.
苏拉明是一种广泛用于治疗非洲锥虫病和盘尾丝虫病的化疗药物，目前正在进行治疗艾滋病的临床试验。研究了它对哺乳动物线粒体能量代谢的影响。低浓度时，它抑制亚线粒体颗粒中的ATP合成和ATP酶活性，以及完整大鼠肝线粒体中ADP刺激的氧消耗和解偶联剂刺激的ATP酶活性。高浓度时，它还抑制亚线粒体颗粒和完整线粒体中的解偶联电子传递。通过比较这些抑制作用的动力学模式，获得了表明腺嘌呤核苷酸转位酶可能是苏拉明作用的另一个靶点的证据。讨论了这些发现与理解苏拉明毒性的生化基础的相关性。
