Global health concerns are clearly evidenced by cardiovascular disease, kidney damage, and heart attacks. Antihypertensive synthetic drugs, including angiotensin-converting enzyme (ACE) inhibitors, effectively control hypertension but with unpleasant side effects. In recent decades, studies on the role of food-derived compounds have provided a positive contribution to ACE regulation. Here, the research progress of plant food-derived phenolic compounds as ACE inhibitors is reviewed. A survey of bioactive compounds of plant food is presented to broaden the source scope of natural ACE inhibitors. A consecutive understanding of plant-derived ACE inhibitors classification, inhibition mechanism, structure-activity relationship, and bioavailability are scientifically organized. The emerging evidence highlights areas that need further research, including those related to molecular structure, bioaccessibility, and interactions with gut microflora. Future research on such topics may encourage basic research and clinic application to exploit these plant food constituents as novel ACE inhibitors.
Keywords: ACE inhibition; bioavailability in vivo; mechanism of action; plant food-derived phenolic compounds; structure and activity relationship.