Abstract: Renin-angiotensin system (RAS) and kallikrein kinin system (KKS) is a pair of mutually antagonistic system in blood pressure regulation, dissonance of which is considered to be an important factor in the pathogenesis of hypertension, and angiotensin converting enzyme (ACE) is a critical factor affecting the systems.More and more attentions have been paid to the food-derived ACE inhibitory peptides, because of their higher activity of inhibiting ACE, good security, low cost, easy to absorb and obvious antihypertension.In this review, the antihypertensive mechanism, sources, bioavailability, structure-activity relationships, separation and purification methods, activity measurement, functional assessment of ACE inhibitory peptides, and its application prospects were introduced.