Despite widespread applications for cancer treatment, chemotherapy is restricted by several limitations, including low targeting specificity, acquired drug resistance, and concomitant adverse side effects. It remains challenging to overcome these drawbacks. Herein, we report a new bioenergetic approach for treating cancer efficiently. As a proof‐of‐concept, we construct activatable mitochondria‐targeting organoarsenic prodrugs from organoarsenic compounds and traditional chemotherapeutics. These prodrugs could accomplish selective delivery and controlled release of both therapeutic agents to mitochondria, which synergistically promote mitochondrial ROS production and induce mitochondrial DNA damage, finally leading to mitochondria‐mediated apoptosis of cancer cells. Our in vitro and in vivo experiments reveal the excellent anticancer efficacy of these prodrugs, underscoring the encouraging outlook of this strategy for effective cancer therapy.

中文翻译：

---

可激活的线粒体靶向有机砷前药，用于生物能癌症治疗。

尽管在癌症治疗中有广泛的应用，化学疗法仍受到一些限制的限制，包括低靶向特异性，获得性耐药性以及随之而来的不良副作用。克服这些缺点仍然具有挑战性。在此，我们报告了一种有效治疗癌症的新生物能方法。作为概念验证，我们从有机砷化合物和传统化学疗法中构建了靶向线粒体的有机砷前药。这些前药可以完成两种治疗剂向线粒体的选择性递送和控制释放，从而协同促进线粒体ROS的产生并诱导线粒体DNA损伤，最终导致线粒体介导的癌细胞凋亡。