Food protein-derived renin-inhibitory peptides: in vitro and in vivo properties

Renin catalyzes the rate-determining step in the renin-angiotensin-aldosterone system that regulates mammalian blood pressure by converting angiotensinogen to angiotensin I (Ang I). Excessive plasma levels of Ang I is a causative factor in hypertension development. Therefore, inhibition of renin activity can lower blood pressure and provide relief from clinical symptoms associated with hypertension. Synthetic compounds are currently the most used group of renin inhibitors; however, only aliskiren is approved as a drug for hypertension treatment. But some negative side effects are associated with aliskiren therapy, which have necessitated the search for alternative natural compounds such as food protein-derived renin-inhibitory peptides with blood pressure-reducing effects. This paper is a concise review of the currently known sources and methods of production of renin-inhibitory peptides including their potential in vitro and in vivo extent of renin inhibition. PRACTICAL APPLICATIONS: Hypertension is a major human chronic disease that leads to severe cardiovascular impairment and ultimately death if not managed properly. Current therapeutic approach to hypertension management involves the use of drugs that inhibit excessive activities of renin and angiotensin converting enzyme (ACE), the two main enzymes that control mammalian blood pressure. Since renin catalyzes a single reaction that is the rate-determining step in the renin-angiotensin system, inhibition of this enzyme activity could be a highly effective strategy for controlling blood pressure without severe negative side effects. However, therapeutic control of renin activity remains difficult with only one approved drug. Some food protein-derived peptides have been found to inhibit renin activity inhibition, which could offer a drug-free treatment for hypertension. Therefore, this review provides a summary of recent developments in the advances and efficacy testing of renin-inhibitory peptides.