Structure-function properties of hypolipidemic peptides

Abstract

This review addresses the structure-function properties of hypolipidemic peptides. The cholesterol-lowering peptide (lactostatin: IIAEK) operates via a new regulatory pathway in the calcium-channel-related mitogen-activated protein kinase (MAPK) signaling pathway of cholesterol degradation. The bile acid binding peptide (soystatin, VAWWMY) inhibits the micellar solubility of cholesterol in vitro and cholesterol absorption in vivo. VVYP is the most effective peptide having hypotriglyceridemic action in globin digests. The suppressive effect of globin digest on postprandial hyperlipidemia has been reported in humans. The ability of peptides (KRES, Apolipoprotein A-I mimetic peptides) to interact with lipids, remove LOOH and activate antioxidant enzymes associated with high-density lipoprotein determines their anti-inflammatory and anti-atherogenic properties. The b-conglycinin derived peptides KNPQLR, EITPEKNPQLR, and RKQEEDEDEE QQRE inhibit fatty acid synthase in vitro. These promising findings indicate the need for more conclusive molecular, cellular, and animal and human studies to design innovative new peptides that ameliorate cholesterol and lipid metabolism. Practical applicationsPrevention and amelioration of hypercholesterolemia by dietary regulation are important. Dietary protein and peptides are very useful as regulators of serum cholesterol concentration. Diets low in saturated fat and cholesterol that include soy protein may reduce the risk of heart disease. In Japan, the concept of "food for specified health use" has been introduced for the prevention and treatment of life-style related disease. Thus, peptides derived from food proteins and sources other than food proteins such as peptide-rich functional foods and nutraceutical products, have considerable potential to prevent lifestyle-related diseases, especially hyperlipidemia, as discussed in this review. Furthermore, various strategies have been used for the efficient screening, development, and application of new hypolipidemic peptides. These include the use of phage display (for antiobesity peptide), peptide mimetics (for anti-atherogenic peptide), and molecular targets such as CYP7A1 (for hypocholesterolemic peptide) and prohibitin (for anti-obesity peptide).

Physiologically Active Molecules and Functional Properties of Soybeans in Human Health—A Current Perspective

“…By checking the reabsorption of bile acids within digestive organs, soy peptides (i.e., lactostatin (IIAEK)) can effectively lower blood cholesterol levels, thus effectively decreasing LDL and fat accumulation ( Figure 12 ), which enables their use in preventing and treating arteriosclerosis [ 5 ]. Soy proteins also contain angiotensin-I converting enzyme (ACE-I)-inhibiting peptides that decrease blood pressure levels ( Figure 13 ), as well as antithrombotic peptides that inhibit platelet aggregation [ 149 , 150 ]. The diverse effects of soybean-derived bioactive peptides are summarized in Table 2 .…”

Metabolic Syndrome-Preventive Peptides Derived from Milk Proteins and Their Presence in Cheeses: A Review

“…The ingestion of whey protein was observed to be correlated with a significant reduction in total cholesterol levels in rats fed cholesterol-free and cholesterol-enriched diets [53]. The cholesterol reducing activity of β-lactoglobulin was due to the presence of two major biopeptides, namely lactostatin (IIAEK) and β-lactotensin (HIRL) [54]. According to the literature, consumption of 300 mg IIAEK × kg −1 body weight per day reduced LDL level as well as increased HDL cholesterol level, and fecal steroid excretion.…”

“…Despite the optimistic results, it should be noted that the exact mechanisms of the hypocholesterolemic activity of peptides are still unclear. It is speculated that it might be linked to the amino acid composition, but further research is needed in this respect [54].…”

Effective screening for hypolipidemic bile acid - binding peptides by hierarchical clustering - based catalog array

“…Nagaoka S. et al found for the first time that VAWWMY (soystatin) derive from soybean glycinin acted as an inhibitor of cholesterol absorption in vivo [13]. There are so many in vitro active soypeptides, soystatin is an only in vivo active hypocholesterolemic peptides derived from soybean [14]. Given the growing requirements for daily preventive therapies for lifestyle related diseases, hypolipidemic peptides could yield new avenues for medical dietary interventions.…”

“…Given the growing requirements for daily preventive therapies for lifestyle related diseases, hypolipidemic peptides could yield new avenues for medical dietary interventions. Notably, the use of such naturally occurring peptides should be more safe and effective than protein hydrolysates [14][15][16][17][18], which contain multiple unknown components in addition to the active molecules.…”