AbstractFood‐derived peptides have garnered significant attention in research due to their multifaceted functionalities, abundant availability, efficient utilization of agricultural by‐products, and environmentally sustainable preparation methods. These peptides play a crucial role in human health, yet their precise mechanisms of action remain largely unexplored, posing challenges in their screening, preparation, and effective application utilizing protein‐based raw materials. This review offers an extensive examination of 19 types of bioactive peptides derived from food. The sources of food‐derived bioactive peptides are well concluded and the classifications are made according to their potential health benefit based on five primary systems: general bodily functions, the nervous system, the cardiovascular system, the metabolic system, and the immune system. This review specifically highlights the multifaceted impacts of tasty peptides on human health, extending beyond their gustatory effects. Furthermore, it explores the interplay between various functions of bioactive peptides, noting a progression from basic to advanced functionalities. Antioxidant activity and the modulation of key enzymes are identified as fundamental actions that are interconnected with other functional properties. This implies that a single bioactive peptide could exhibit multiple beneficial effects. The key role of antioxidant capabilities is underscored based on their broad influence and straightforward assessment. This comprehensive analysis aims to deepen the systematic understanding of the diverse benefits offered by various food‐derived peptides.