When screening active compounds by phenotypic assays, we often encounter mitochondrial toxins, which are compounds that can affect mitochondrial functions. In normal cells, these toxins may have relatively low toxicity but can nonetheless show measurable effects even at low concentrations. On the other hand, in animals, mitochondrial toxins can exert severe toxicity. Mitochondrial toxins that act as inhibitors of respiratory chain complexes in oxidative phosphorylation (OXPHOS) are typically avoided during drug discovery efforts, as such compounds can directly promote lethal inhibition of pulmonary respiration. However, mitochondrial toxins could in fact have beneficial therapeutic effects. Anti-cancer strategies that target mitochondrial functions, particularly OXPHOS, have received increasing attention in recent years. In this review article we examine the significance of OXPHOS inhibitors as anti-cancer drug candidates and discuss compounds having microbial origins.

在通过表型分析筛选活性化合物时，我们经常会遇到线粒体毒素，这是一种可以影响线粒体功能的化合物。在正常细胞中，这些毒素可能具有相对较低的毒性，但即使在低浓度下也能显示出可测量的影响。另一方面，在动物中，线粒体毒素会产生严重的毒性。在药物发现过程中通常会避免作为氧化磷酸化 (OXPHOS) 呼吸链复合物抑制剂的线粒体毒素，因为此类化合物可直接促进肺呼吸的致命抑制。然而，线粒体毒素实际上可能具有有益的治疗效果。近年来，针对线粒体功能（尤其是 OXPHOS）的抗癌策略受到越来越多的关注。