In Vitro Assessment of the Bioaccessibility and Hypoglycemic Properties of Essential Amino Acids Blend: Implication for Diabetes Management.

Essential amino acid (EAA) supplementation is often employed in sportive and clinical nutrition due to EAAs' role in muscle mass maintenance and growth. EAAs are also involved in insulin and glucagone regulation in diabetes management, but only few reports investigate their possible implication as dipeptidyl peptidase-IV (DPP-IV) inhibitors and their effect on the stability and secretion of enteroendocrine hormones. A blend of EAAs (called GAF) available as a food supplement, in a specific qualitative and quantitative ratio, was investigated to address its in vitro bioaccessibility, its hypoglycemic properties in vitro and in situ on cellular models, and its safety on intestinal Caco-2 cells.

Integratomic investigation to assess the liver lipidomic and antiinflammatory activity of lupin protein hydrolysate.

Chronic inflammation plays a significant role in the development and progression of metabolic dysfunction-related diseases. This study investigating a protein hydrolysate from Lupinus angustifolius (LPH) in mice model on a western diet (WD) aimed to elucidate its potential beneficial role in improving the lipidomic and anti-inflammatory profile. To achieve this objective, a lipidomic approach in combination with the evaluation of protein level modulation of selected key enzymes that are pivotal involved in the bioactive lipid pathway synthesis/regulation was performed on liver homogenates.

Seaweed () Protein Hydrolyzates: A Valuable Source of Short- and Medium-Chain Peptides with Multifunctional Properties.

The sustainable valorization of infesting marine biomass offers opportunities to address environmental challenges and emerging nutritional needs. This study investigated the invasive red alga as a potential source of bioactive peptides with antihypertensive and antidiabetic properties. Protein hydrolyzates were generated via enzymatic digestion and fractionated by size exclusion chromatography.

Antioxidant and Anti-Inflammatory Activity of a New Formulation of Slow-Release Amino Acids in Human Intestinal Caco-2 Cells.

Phenylalanine (Phe)-free protein substitutes (PSs) are used to provide an adequate intake of amino acids (AAs), except Phe, allowing control of blood Phe levels in patients with Phenylketonuria (PKU). Although indicated as a standard dietary treatment for these patients, free AAs mixtures are not absorbed as natural proteins, thus creating an oxidized and inflamed state in the intestine. Nowadays, PSs on the market also include slow-release amino acids (SR-AAs) formulas.

Ultrasonicated Atlantic herring side streams as source of multifunctional bioactive and bioavailable peptides.

This study demonstrates the effectiveness of ultrasonication, as a pre-treatment technology, coupled to enzymatic hydrolysis of herring side streams, yielding multifunctional peptide mixtures with antioxidant, hypotensive (ACE inhibitory activity), and hypoglycemic (DPP-IV inhibitory and GLP-1 enhancer activity) properties. The ultrasound pre-treatment modulates the biological activity of the hydrolysates, enhancing certain bioactive properties (antioxidant, ACE inhibitory, and GLP-1 enhancer activities, respectively) while reducing others (DPP-IV inhibitory activity). The study also highlights the importance of simulating gastrointestinal digestion and using Caco-2 cells to assess the bioaccessibility, intestinal bioavailability, and metabolic resistance of herring peptides.

Antioxidant Activity and DPP-IV Inhibitory Effect of Fish Protein Hydrolysates Obtained from High-Pressure Pretreated Mixture of Rainbow Trout () and Atlantic Salmon () Rest Raw Material.

The use of fish rest raw material for the production of fish protein hydrolysates (FPH) through enzymatic hydrolysis has received significant interest in recent decades. Peptides derived from fish proteins are known for their enhanced bioactivity which is mainly influenced by their molecular weight. Studies have shown that novel technologies, such as high-pressure processing (HPP), can effectively modify protein structures leading to increased biological activity.

Ultrasonication coupled to enzymatic hydrolysis of soybean okara proteins for producing bioactive and bioavailable peptides.

This work was aimed to explore the antioxidative properties, bioavailability and the safety of bioactive peptides obtained by the enzymatic hydrolysis of ultrasound-treated (UO) and untreated (nUO) soybean okara proteins. Particularly, the peptidomic profiles of both hydrolysates were examined using an untargeted metabolomics technique for suspect screening that was specifically designed for the profiling of short-chain peptides and relied on ultra-high-performance liquid chromatography coupled to high-resolution mass spectrometry (UHPLC-HRMS) and bioinformatics. Next, both UO and nUO hydrolysates reduce Dipeptidyl peptidase-IV (DPP-IV) enzyme activity until 39.

PCSK9 inhibitors: a patent review 2018-2023.

Introduction: Proprotein convertase subtilisin/kexin 9 (PCSK9) plays a crucial role in breaking down the hepatic low-density lipoprotein receptor (LDLR), thereby influencing the levels of circulating low-density lipoprotein cholesterol (LDL-C). Consequently, inhibiting PCSK9 through suitable ligands has been established as a validated therapeutic strategy for combating hypercholesterolemia and cardiovascular diseases.

Area Covered: Patent literature claiming novel compounds inhibiting PCSK9 disclosed from 2018 to June 2023 available in the espacenet database, which contains more than 150 million patent documents from over 100 patent-granting authorities worldwide.

Olive ( L.) Seed as New Source of Cholesterol-Lowering Bioactive Peptides: Elucidation of Their Mechanism of Action in HepG2 Cells and Their Trans-Epithelial Transport in Differentiated Caco-2 Cells.

The production of olive oil has important economic repercussions in Mediterranean countries but also a considerable impact on the environment. This production generates enormous quantities of waste and by-products, which can be exploited as new raw materials to obtain innovative ingredients and therefore make the olive production more sustainable. In a previous study, we decided to foster olive seeds by generating two protein hydrolysates using food-grade enzymes, alcalase (AH) and papain (PH).

Glycomacropeptide (GMP) rescued the oxidative and inflammatory activity of free L-AAs in human Caco-2 cells: New insights that support GMP as a valid and health-promoting product for the dietary management of phenylketonuria (PKU) patients.

Phenylketonuria represents the most prevalent inborn error of amino acid metabolism. In early diagnosed patients adequate and continued dietary treatment results in a good neurologic outcome. However, due to the natural protein and phenylalanine-restricted diet, oxidative stress represents a concern in phenylketonuric patients.

Plant bioactive peptides for cardiovascular disease prevention.

Cardiovascular disease (CVD) is a major cause of deaths in industrialized countries and a constantly growing cause of morbidity and mortality worldwide Hypercholesterolemia is one of the main risk factors for CVD progression that may be prevented by lifestyle changes, including diet. This chapter will discuss the role of peptides from plants (soybean, lupin, cowpea, hempseed, and rice bran) sources with pleotropic activity for the prevention of CVD. Overall, the bioactivity that will be mainly discussed it is the hypocholesterolemic one.

Bioavailability Assessment of an Iron Formulation Using Differentiated Human Intestinal Caco-2 Cells.

In recent years, there has been growing interest in exploring alternative and innovative delivery systems to improve the efficacy of iron supplements, satisfying iron needs and lowering side effects. To address this issue, this study aimed at demonstrating the advantages of Ferro Supremo formulation (composed of encapsulated iron, vitamins, and micronutrients), in terms of capacity to improve iron intestinal absorption, in comparison with standard FeSO. Hence, differentiated Caco-2 cells have been used for assessing the in vitro bioavailability and safety of FS and FeSO.

Computational Mechanics of Form-Fitting 3D-Printed Lattice-Based Wrist-Hand Orthosis for Motor Neuron Disease.

Motor neuron disease (MND) patients often experience hand-wrist muscle atrophy resulting in severe social consequences and hampering their daily activities. Although hand-wrist orthosis is commonly used to assist weakened muscles, its effectiveness is limited due to the rapid progression of the disease and the need for customization to suit individual patient requirements. To address these challenges, this study investigates the application of three-dimensional (3D) printing technology to design and fabricate two lattice structures inspired by silkworm cocoons, using poly-ε-caprolactone as feedstock material.

MOMAST Reduces the Plasmatic Lipid Profile and Oxidative Stress and Regulates Cholesterol Metabolism in a Hypercholesterolemic Mouse Model: The of a Sustainable and Innovative Antioxidant and Hypocholesterolemic Ingredient.

MOMAST is a patented natural phenolic complex, rich in tyrosol (9.0 g/kg, Tyr), hydroxityrosol (43,5 g/kg, OH-Tyr), and verbascoside (5.0 g/Kg), which is obtained from the OVW by-product of the cultivar with potent direct antioxidant activity (measured by DPPH and FRAP assays, respectively).

Physicochemical and functional properties of rainbow trout () hydrolysate.

Due to the continuous growth of the world population, there is an urgent need to find sustainable sources of high-quality protein. Fish side streams rich in essential nutrients and accounting for 60-70% of the whole fish, represent a sustainable source for recovery of valuable protein compounds. The present study aimed at extensive characterization of physicochemical, antioxidant and techno-functional properties of fish protein hydrolysate (FPH) obtained from farmed rainbow trout ().

Evaluation of the multifunctional dipeptidyl-peptidase IV and angiotensin converting enzyme inhibitory properties of a casein hydrolysate using cell-free and cell-based assays.

The objective of the study was the evaluation of the potential pleiotropic effect of a commercial casein hydrolysate (CH). After an analysis of the composition, the BIOPEP-UWM database suggested that these peptides contained numerous sequences with potential inhibitory activities on angiotensin converting enzyme (ACE) and dipeptidyl-peptidase IV (DPP-IV). The anti-diabetic and anti-hypertensive effects of these peptides were thus assessed using either cell-free or cell-based assays.

Computational Design, Synthesis, and Biological Evaluation of Diimidazole Analogues Endowed with Dual PCSK9/HMG-CoAR-Inhibiting Activity.

Proprotein convertase subtilisin/kexin 9 (PCSK9) is responsible for the degradation of the hepatic low-density lipoprotein receptor (LDLR), which regulates circulating cholesterol levels. Consequently, the PCSK9 inhibition is a valuable therapeutic approach for the treatment of hypercholesterolemia and cardiovascular diseases. In our studies, we discovered , a polyimidazole derivative reducing the protein-protein interaction between PCSK9 and LDLR with an IC of 1.

Antioxidant Effect Assessment and Trans Epithelial Analysis of New Hempseed Protein Hydrolysates.

Hempseed () is one of the most promising sources of plant proteins. It contains approximately 24% (/) protein, and edestin accounts for approximately 60-80% (/) of its total proteins. In a framework of research aimed at fostering the proteins recovered from the press cake by-products generated after the extraction of hempseed oil, two hempseed protein hydrolysates (HH1 and HH2) were produced at an industrial level using a mixture of different enzymes from , , and for different times (5 h and 18 h).

Virgin Olive Oil By-Product Valorization: An Insight into the Phenolic Composition of Olive Seed Extracts from Three Cultivars as Sources of Bioactive Molecules.

Olives are very rich in phenolic compounds with important health-promoting properties. The profile and content of phenols in olive pulp and virgin olive oil are strongly influenced by the fruit ripening degree, but little is known concerning the evolution of phenolic compounds in the seed. In this work, the phenolic composition of seed from Tuscan cultivars (Frantoio, Moraiolo, Leccino) was studied over maturation.

Rainbow Trout () as Source of Multifunctional Peptides with Antioxidant, ACE and DPP-IV Inhibitory Activities.

The present study aimed at characterizing the possible biological activities of the multifunctional low molecular weight fractions (<3 kDa) peptides isolated from rainbow trout () obtained by enzymatic hydrolysis. The fish protein hydrolysate (FPH) was tested for its antioxidant property along with its angiotensin converting enzyme (ACE) and dipeptidyl peptidase IV (DPP-IV) inhibitory activities. In particular, the 2,2-diphenyl-1-picrylhydrazyl (DPPH), the ferric reducing antioxidant power (FRAP), the oxygen radical absorbance capacity (ORAC) assay and the 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) assays were carried out for the evaluation of the in vitro antioxidant activity.

Valorization of the Antioxidant Effect of Mantua PGI Pear By-Product Extracts: Preparation, Analysis and Biological Investigation.

For improving the management of the production chain of PGI Mantua pears (which comprises many varieties, including Abate Fetel), applying the cardinal principles of circular economy and sustainability, the fruits with diseases or defects were recovered for producing dried rounds of pears from the Abate Fetel cultivar, a new product with high nutritional value that extends the remaining life. This process led to the production of secondary and residual by-products, which are mainly composed of the highest and lowest part of the fruits, comprising seeds, pulps, peels and petioles. Hence, this study was focused on the valorization of these secondary by-products of Abate Fetel pears through the production of pear extracts using traditional and "green" extraction methods that involve the use of supercritical CO fluid extraction.

Isolation and functional characterization of hemp seed protein-derived short- and medium-chain peptide mixtures with multifunctional properties for metabolic syndrome prevention.

This study aims to obtain a valuable mixture of short-chain peptides from hempseed as a new ingredient for developing nutraceutical and functional foods useful for preventing metabolic syndrome that represents the major cause of death globally. A dedicated analytical platform based on a purification step by size exclusion chromatography or ultrafiltration membrane and high-resolution mass spectrometry was developed to isolate and comprehensively characterize short-chain peptides leading to the identification of more than 500 short-chain peptides. Our results indicated that the short-chain peptide mixture was about three times more active than the medium-chain peptide mixture and total hydrolysate with respect to measured inhibition of the angiotensin-converting enzyme.