Improving Health-Promoting Effects of Food-Derived Bioactive Peptides through Rational Design and Oral Delivery Strategies

Abstract

Over the last few decades, scientific interest in food-derived bioactive peptides has grown as an alternative to pharmacological treatments in the control of lifestyle-associated diseases, which represent a serious health problem worldwide. Interest has been directed towards the control of hypertension, the management of type 2 diabetes and oxidative stress. Many food-derived antihypertensive peptides act primarily by inhibiting angiotensin I-converting enzyme (ACE), and to a lesser extent, renin enzyme activities. Antidiabetic peptides mainly inhibit dipeptidyl peptidase-IV (DPP-IV) activity, whereas antioxidant peptides act through inactivation of reactive oxygen species, free radicals scavenging, chelation of pro-oxidative transition metals and promoting the activities of intracellular antioxidant enzymes. However, food-derived bioactive peptides have intrinsic weaknesses, including poor chemical and physical stability and a short circulating plasma half-life that must be addressed for their application as nutraceuticals or in functional foods. This review summarizes the application of common pharmaceutical approaches such as rational design and oral delivery strategies to improve the health-promoting effects of food-derived bioactive peptides. We review the structural requirements of antihypertensive, antidiabetic and antioxidant peptides established by integrated computational methods and provide relevant examples of effective oral delivery systems to enhance solubility, stability and permeability of bioactive peptides.

Keywords: computational methods; food-derived bioactive peptides; functional foods; hypertension; nutraceuticals; oral delivery strategies; oxidative stress; rationally designed peptides; structural requirements; type 2 diabetes.

Figure 1

Main targets of food-derived bioactive peptides in the management of hypertension, type 2 diabetes and oxidative stress.

Figure 2

Pharmaceutical approaches to solve the main challenges of food-derived bioactive peptides for the development of functional foods and nutraceuticals.

Figure 3

Preferred amino acid residues within the sequence of angiotensin I-converting enzyme (ACE) inhibitory di- and tripeptides (a), dipeptidyl peptidase-IV (DPP-IV) inhibitory dipeptides (b) and antioxidant tripeptides (c). Font size indicates the most favorable residues for each position.