线粒体功能破坏作为三氟拉嗪对克氏锥虫杀锥虫作用的基础。
Disruption of mitochondrial function as the basis of the trypanocidal effect of trifluoperazine on Trypanosoma cruzi.
作者信息
Lacuara J L, de Barioglio S R, de Oliva P P, Bernacchi A S, de Culasso A F, Castro J A, Franke de Cazzulo B M, Cazzulo J J
机构信息
Instituto de Fisiologia, Facultad de Ciencias Medicas, Universidad Nacional de Córdoba, Argentina.
出版信息
Experientia. 1991 Jun 15;47(6):612-6. doi: 10.1007/BF01949887.
The tricyclic anti-calmodulin drug trifluoperazine (TFP) inhibited growth and motility of epimastigotes of Trypanosoma cruzi, at concentrations lower than 100 microM, and motility and infectivity of the bloodstream trypomastigote form at 200 microM. Electron microscopy of TFP-treated epimastigotes showed that the major effect was at the mitochondrial level, with gross swelling and disorganization. The oligomycin-sensitive, mitochondrial ATPase was completely inhibited by 20 microM TFP, and the same drug concentration caused a 60% decrease in intracellular ATP content. The results suggest that the trypanocidal effect of TFP may be related more to mitochondrial damage than to the well-known anticalmodulin effect of the drug.
三环类抗钙调蛋白药物三氟拉嗪（TFP）在浓度低于100微摩尔时可抑制克氏锥虫前鞭毛体的生长和运动能力，在200微摩尔时可抑制血液中锥鞭毛体形式的运动能力和感染性。对经TFP处理的前鞭毛体进行电子显微镜观察显示，主要作用发生在线粒体水平，表现为明显肿胀和结构紊乱。寡霉素敏感的线粒体ATP酶被20微摩尔的TFP完全抑制，相同药物浓度导致细胞内ATP含量降低60%。结果表明，TFP的杀锥虫作用可能更多地与线粒体损伤有关，而非该药物广为人知的抗钙调蛋白作用。
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