Mitochondria targeted cancer therapy using ethidium derivatives

In this study, we reported on two novel fluorescent ethidium derivatives of MTP1 and MTP2 for selective and efficient cancer therapy. MTP1 and MTP2 exhibited cancer cell targeting and subsequent mitochondria targeting and imaging abilities. Moreover, both MTP1 and MTP2 would induce mitochondria depolarization and so along with a series of cascaded biochemical effects including the reduction of ATP production, destruction of intracellular redox potential balance and release of mitochondria cytochrome C (Cyt C), which could finally trigger caspase-dependent cell apoptosis. More interestingly, both MTP1 and MTP2 demonstrated significant cancer suppression abilities in vitro and in vivo, which presented a new paradigm for the development of unique anti-cancer agent candidates in precise and efficient cancer theranostics.