Mitochondria-Targeted Antioxidants and Cancer

Antioxidant therapy in cancer is gaining momentum after witnessing a striking success of mitochondria-targeted antioxidants in oxidative stress-mediated pathologies. Mitochondria are major source of cellular reactive oxygen species which are generated during oxidative phosphorylation. This makes mitochondria as one of the key targets for antioxidant cancer therapy. Mitochondrial oxidative stress can be targeted by either conjugating antioxidants to lipophilic cation such as triphenylphosphonium or peptide-based antioxidant mitochondrial targeting. Mitochondria-targeted antioxidants accumulate 100-to 1000-fold in mitochondrial matrix based on the high mitochondrial membrane potential (150-180 mV). In this chapter, we discussed how targeting antioxidants to mitochondria improved their anticancer activity and opened new avenues of cancer management.