Abstract: Primary structure of milk-derived antihypertension peptides and antioxidative peptides have some important effect on their function.The composition of peptides, types, the content of hydrophobic amino acids and their position how to affect on their activity, were reviewed, and the novel bioactive peptides identificated in recent years was also summarized.Bioactivities was significantly influenced by the structure and composition of peptides, therefore, the study on primary structure-bioactive relationship of milk-derived bioactive peptides would provide information for obtaining efficient bioactive peptides in the future.