Background: Over the last years, bioactive antioxidant peptides, extracted from food proteins, have been studied due to their potential as useful tools in the development of new natural drugs and food ingredients. These compounds can be used to decrease oxidative stress and food quality decay, thus being an interesting strategy to reduce economic losses in food production, as well as improve public health. Scope and Approach: Antioxidant peptides are extracted from non-antioxidant precursor proteins from different origin by the activity of either proteolytic microorganisms or isolated enzymes. In the present review, the main sources of bioactive peptides will be discussed. Moreover, the current strategies to obtain these compounds as well as their health benefits and in vivo biological effects will be evaluated. Considerations for further research and development of strategies to increase the knowledge about this underexplored activity of peptides will be also considered.