Abstract: Hypertension is a major threat to health and food-derived angiotensin-converting enzyme inhibitory peptides (ACEIPs) have been recognized as potential alternatives to synthetic angiotensin-converting enzyme (ACE) inhibitors in the treatment of hypertension due to their high safety and non-toxicity. A large number of antihypertensive peptides with in vitro ACE inhibitory activity have been isolated and identified, but only a few of them including Ile-Pro-Pro (IPP), Val-Pro-Pro (VPP), and Leu-Pro-Pro (LPP) have been confirmed to be clinically effective for humans. Originally isolated from fermented milk, the three peptides are collectively called lactotripeptides. Several antihypertensive functional foods based on lactotripeptides have been marketed in many overseas countries and their efficacy has been fully verified, but such products are yet not available in China. In this context, the functions, safety, production methods, and new sources of the lactotripeptides are reviewed and patents concerning them are summarized herein. This review is expected to provide valuable information for the development of third-generation antihypertensive functional foods in China.

Key words: hypertension; antihypertensive peptides; lactotripeptides; clinical efficacy; safety; production methods