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Bioactive Peptides in Human Health and Disease

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (31 August 2022) | Viewed by 27563

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Dr. Serena Martini

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Guest Editor

Department of Life Sciences, University of Modena and Reggio Emilia, Via Amendola 2, 42100 Reggio Emilia, Italy
Interests: polyphenols; digestion; bioactive peptides
Special Issues, Collections and Topics in MDPI journals

Dr. Davide Tagliazucchi

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Guest Editor

Department of Life Sciences, University of Modena and Reggio Emilia, 42121 Reggio, Italy
Interests: biological activity of (poly)phenols and their corresponding metabolites produced in the body; study of the molecular mechanisms of interaction between (poly)phenols and enzymes; identification and bioactivity of peptides produced after digestion of dietary protein
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Dietary habits and sedentary lifestyle are widely established to be the major risk factors for the development of long-term chronic conditions, such as cardiovascular diseases, type-2 diabetes and cancer. In this framework, where consumer’s food choices are even more influenced by an ever-growing awareness on nutritional, environmental, and healthy aspects, the presence and identification of natural bioactive compounds are gaining increasing attention in the scientific community.

In recent years, scientific interest in bioactive peptides and their potential health benefits are greatly increased within the framework of health-promoting functional foods. The search for bioactive peptides has expanded exponentially due to the increased incidence of metabolic and cardiovascular diseases. Bioactive peptides showed different bio-functional properties and they can be used as additional components in functional foods, nutraceuticals, food-grade bio-preservatives, cosmetics, and pharmaceuticals. They may have important physiological functions, such as anti-hypertensive, anti-microbial, anti-thrombotic, immunomodulatory, opioid, antioxidant, and mineral binding activities.

This Special Issue, entitled “Bioactive Peptides in Human Health and Disease”, aims to collect research and review papers focusing on several aspects that are related to bioactive peptides and human health, including their in vitro and in vivo role in the prevention and treatment of chronic diseases, bioaccessibility and bioavailability, release and biological characterization of novel bioactive peptides, and in vitro mechanistic studies.

Dr. Serena Martini
Prof. Dr. Davide Tagliazucchi
Guest Editors

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Keywords

diabetes
cardiovascular diseases
peptidomics
food digestion
protein hydrolysates
antihypertensive peptides
antioxidant peptides

Published Papers (11 papers)

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Editorial

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4 pages, 187 KiB

Open AccessEditorial

Bioactive Peptides in Human Health and Disease

by Serena Martini and Davide Tagliazucchi

Int. J. Mol. Sci. 2023, 24(6), 5837; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24065837 - 19 Mar 2023

Cited by 5 | Viewed by 1191

Abstract

Bioactive peptides are defined as short amino acid sequences that may have specific physiological functions, ultimately affecting human health and protecting against the development of several diseases [...] Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

Research

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18 pages, 3676 KiB

Open AccessArticle

Definition and Characterization of SOX11-Derived T Cell Epitopes towards Immunotherapy of Glioma

by Yibin Liu, Anna Keib, Brigitte Neuber, Lei Wang, Angelika B. Riemer, Maria Bonsack, Angela Hückelhoven-Krauss, Anita Schmitt, Carsten Müller-Tidow and Michael Schmitt

Int. J. Mol. Sci. 2023, 24(3), 1943; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24031943 - 18 Jan 2023

Cited by 4 | Viewed by 1609

Abstract

The transcription factor SOX11 is a tumor-associated antigen with low expression in normal cells, but overexpression in glioblastoma (GBM). So far, conventional surgery, chemotherapy, and radiotherapy have not substantially improved the dismal prognosis of relapsed/refractory GBM patients. Immunotherapy is considered a promising strategy against GBM, but there is a fervent need for better immunotargets in GBM. To this end, we performed an in silico prediction study on SOX11, which primarily yielded ten promising HLA-A*0201-restricted peptides derived from SOX11. We defined a novel peptide FMACSPVAL, which had the highest score according to in silico prediction (6.02 nM by NetMHC-4.0) and showed an exquisite binding affinity to the HLA-A*0201 molecule in the peptide-binding assays. In the IFN-γ ELISPOT assays, FMACSPVAL demonstrated a high efficiency for generating SOX11-specific CD8⁺ T cells. Nine out of thirty-two healthy donors showed a positive response to SOX11, as assessed by the ELISPOT assays. Therefore, this novel antigen peptide epitope seems to be promising as a target for T cell-based immunotherapy in GBM. The adoptive transfer of in vitro elicited SOX11-specific CD8⁺ T cells constitutes a potential approach for the treatment of GBM patients. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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15 pages, 483 KiB

Open AccessArticle

ACP-ADA: A Boosting Method with Data Augmentation for Improved Prediction of Anticancer Peptides

by Sadik Bhattarai, Kyu-Sik Kim, Hilal Tayara and Kil To Chong

Int. J. Mol. Sci. 2022, 23(20), 12194; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232012194 - 13 Oct 2022

Cited by 6 | Viewed by 1941

Abstract

Cancer is the second-leading cause of death worldwide, and therapeutic peptides that target and destroy cancer cells have received a great deal of interest in recent years. Traditional wet experiments are expensive and inefficient for identifying novel anticancer peptides; therefore, the development of an effective computational approach is essential to recognize ACP candidates before experimental methods are used. In this study, we proposed an Ada-boosting algorithm with the base learner random forest called ACP-ADA, which integrates binary profile feature, amino acid index, and amino acid composition with a 210-dimensional feature space vector to represent the peptides. Training samples in the feature space were augmented to increase the sample size and further improve the performance of the model in the case of insufficient samples. Furthermore, we used five-fold cross-validation to find model parameters, and the cross-validation results showed that ACP-ADA outperforms existing methods for this feature combination with data augmentation in terms of performance metrics. Specifically, ACP-ADA recorded an average accuracy of 86.4% and a Mathew’s correlation coefficient of 74.01% for dataset ACP740 and 90.83% and 81.65% for dataset ACP240; consequently, it can be a very useful tool in drug development and biomedical research. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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18 pages, 8079 KiB

Open AccessArticle

The Therapeutic Potential of Naturally Occurring Peptides in Counteracting SH-SY5Y Cells Injury

by Renata Perlikowska, Joana Silva, Celso Alves, Patrícia Susano and Rui Pedrosa

Int. J. Mol. Sci. 2022, 23(19), 11778; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms231911778 - 04 Oct 2022

Cited by 5 | Viewed by 1722

Abstract

Peptides have revealed a large range of biological activities with high selectivity and efficiency for the development of new drugs, including neuroprotective agents. Therefore, this work investigates the neuroprotective properties of naturally occurring peptides, endomorphin-1 (EM-1), endomorphin-2 (EM-2), rubiscolin-5 (R-5), and rubiscolin-6 (R-6). We aimed at answering the question of whether well-known opioid peptides can counteract cell injury in a common in vitro model of Parkinson’s disease (PD). Antioxidant activity of these four peptides was evaluated by the 2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging activity, oxygen radical absorbance capacity (ORAC), and ferric-reducing antioxidant power (FRAP) assays, while neuroprotective effects were assessed in a neurotoxic model induced by 6-hydroxydopamine (6-OHDA) in a human neuroblastoma cell line (SH-SY5Y). The mechanisms associated with neuroprotection were investigated by the determination of mitochondrial membrane potential (MMP), reactive oxygen species (ROS) production, and Caspase-3 activity. Among the tested peptides, endomorphins significantly prevented neuronal death induced by 6-OHDA treatment, decreasing MMP (EM-1) or Caspase-3 activity (EM-2). Meanwhile, R-6 showed antioxidant potential by FRAP assay and exhibited the highest capacity to recover the neurotoxicity induced by 6-OHDA via attenuation of ROS levels and mitochondrial dysfunction. Generally, we hypothesize that peptides’ ability to suppress the toxic effect induced by 6-OHDA may be mediated by different cellular mechanisms. The protective effect caused by endomorphins results in an antiapoptotic effect (mitochondrial protection and decrease in Caspase-3 activity), while R-6 potency to increase a cell’s viability seems to be mediated by reducing oxidative stress. Our results may provide new insight into neurodegeneration and support the short peptides as a potent drug candidate to treat PD. However, further studies should be conducted on the detailed mechanisms of how tested peptides could suppress neuronal injuries. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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22 pages, 2326 KiB

Open AccessArticle

In Vivo and In Vitro Comparison of the DPP-IV Inhibitory Potential of Food Proteins from Different Origins after Gastrointestinal Digestion

by Léa Fleury, Barbara Deracinois, Camille Dugardin, Alice B. Nongonierma, Richard J. FitzGerald, Christophe Flahaut, Benoit Cudennec and Rozenn Ravallec

Int. J. Mol. Sci. 2022, 23(15), 8365; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23158365 - 28 Jul 2022

Cited by 5 | Viewed by 2266

Abstract

Dipeptidyl-peptidase IV (DPP-IV) plays an essential role in glucose metabolism by inactivating incretins. In this context, food-protein-derived DPP-IV inhibitors are promising glycemic regulators which may act by preventing the onset of type 2 diabetes in personalized nutrition. In this study, the DPP-IV-inhibitory potential of seven proteins from diverse origins was compared for the first time in vitro and in vivo in rat plasma after the intestinal barrier (IB) passage of the indigested proteins. The DPP-IV-inhibitory potentials of bovine hemoglobin, caseins, chicken ovalbumin, fish gelatin, and pea proteins were determined in rat plasma thirty minutes after oral administration. In parallel, these proteins, together with bovine whey and gluten proteins, were digested using the harmonized INFOGEST protocol adapted for proteins. The DPP-IV half-maximal inhibitory concentration (IC₅₀) was determined in situ using Caco-2 cells. The DPP-IV-inhibitory activity was also measured after IB passage using a Caco2/HT29-MTX mixed-cell model. The peptide profiles were analyzed using reversed-phase high-performance liquid chromatography tandem mass spectrometry (RP-HPLC-MS/MS) with MS data bioinformatics management, and the IC₅₀ of the identified peptides was predicted in silico. The in vitro and in vivo DPP-IV-inhibitory activity of the proteins differed according to their origin. Vegetable proteins and hemoglobin yielded the highest DPP-IV-inhibitory activity in vivo. However, no correlation was found between the in vivo and in vitro results. This may be partially explained by the differences between the peptidome analysis and the in silico predictions, as well as the study complexity. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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14 pages, 37803 KiB

Open AccessArticle

Antamanide Analogs as Potential Inhibitors of Tyrosinase

by Claudia Honisch, Matteo Gazziero, Roberto Dallocchio, Alessandro Dessì, Davide Fabbri, Maria Antonietta Dettori, Giovanna Delogu and Paolo Ruzza

Int. J. Mol. Sci. 2022, 23(11), 6240; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23116240 - 02 Jun 2022

Cited by 5 | Viewed by 1774

Abstract

The tyrosinase enzyme, which catalyzes the hydroxylation of monophenols and the oxidation of o-diphenols, is typically involved in the synthesis of the dark product melanin starting from the amino acid tyrosine. Contributing to the browning of plant and fruit tissues and to the hyperpigmentation of the skin, leading to melasma or age spots, the research of possible tyrosinase inhibitors has attracted much interest in agri-food, cosmetic, and medicinal industries. In this study, we analyzed the capability of antamanide, a mushroom bioactive cyclic decapeptide, and some of its glycine derivatives, compared to that of pseudostellarin A, a known tyrosinase inhibitor, to hinder tyrosinase activity by using a spectrophotometric method. Additionally, computational docking studies were performed in order to elucidate the interactions occurring with the tyrosinase catalytic site. Our results show that antamanide did not exert any inhibitory activity. On the contrary, the three glycine derivatives AG9, AG6, and AOG9, which differ from each other by the position of a glycine that substitutes phenylalanine in the parent molecule, improving water solubility and flexibility, showed tyrosinase inhibition by spectrophotometric assays. Analytical data were confirmed by computational studies. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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20 pages, 3398 KiB

Open AccessArticle

Structural Requirements for the Binding of a Peptide to Prohibitins on the Cell Surface of Monocytes/Macrophages

by Qindong Zhang, Anniken Olberg and Mouldy Sioud

Int. J. Mol. Sci. 2022, 23(8), 4282; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23084282 - 13 Apr 2022

Cited by 5 | Viewed by 2300

Abstract

The screening of phage peptide libraries resulted in the identification of a sequence (named NW peptide, NWYLPWLGTNDW) that specifically binds to human monocytes and macrophages. Although the NW peptide can be used for the targeted delivery of therapeutics without knowledge of its receptor(s), the identification of-its binding partners will support future clinical applications-Here, we used the biotinylated NW peptide for cross-linking cell surface receptor(s) on live cells or as bait in pull-down assays with membrane proteins isolated from monocytes or human THP-1 cells differentiated into macrophages. Proteomic analysis of the captured proteins identified cell surface prohibitins (PHB1 and PHB2) and modified albumin as binding partners. Using flow cytometry and pull-down methods, we demonstrated that PHB1 and PHB2 interact directly with the NW peptide. Confocal imaging showed co-localization of the peptide with PHB1 on the surface of monocytes. Single replacement of either tryptophan or leucine with alanine completely inhibited binding, whereas the replacement of asparagine at position 1 or 10 and aspartic acid at position 11 with alanine did not affect the binding of the peptide variants. Neutral amino acid replacement of tryptophan at positions 2, 6, and 12 with tyrosine or phenylalanine also abolished the binding, implying that the indole ring of tryptophan is indispensable for the NW peptide to bind. Overall, the data suggest that membrane-associated prohibitins might be a useful target for the delivery of therapeutics to monocytes/macrophages and that tryptophan and leucine are key residues for peptide binding. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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25 pages, 6095 KiB

Open AccessArticle

Cationic Peptides and Their Cu(II) and Ni(II) Complexes: Coordination and Biological Characteristics

by Aleksandra Kotynia, Benita Wiatrak, Wojciech Kamysz, Damian Neubauer, Paulina Jawień and Aleksandra Marciniak

Int. J. Mol. Sci. 2021, 22(21), 12028; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222112028 - 06 Nov 2021

Cited by 7 | Viewed by 2113

Abstract

Antimicrobial peptides are a promising group of compounds used for the treatment of infections. In some cases, metal ions are essential to activate these molecules. Examples of metalloantibiotics are, for instance, bleomycin and dermcidin. This study is focused on three new pseudopeptides with potential biological activity. The coordination behavior of all ligands with Cu(II) and Ni(II) ions has been examined. Various analytical methods such as potentiometric titration, UV-Vis and CD spectroscopies, and mass spectrometry were used. All compounds are convenient chelators for metal ion-binding. Two of the ligands tested have histidine residues. Surprisingly, imidazole nitrogen is not involved in the coordination of the metal ion. The N-terminal amino group, Dab side chains, and amide nitrogen atoms of the peptide bonds coordinated Cu(II) and Ni(II) in all the complexes formed. The cytotoxicity of three pseudopeptides and their complexes was evaluated. Moreover, their other model allowed for assessing the attenuation of LPS-induced cytotoxicity and anti-inflammatory activities were also evaluated, the results of which revealed to be very promising. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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10 pages, 2320 KiB

Open AccessArticle

A Collection of Designed Peptides to Target SARS-CoV-2 Spike RBD—ACE2 Interaction

by Narcis Fernandez-Fuentes, Ruben Molina and Baldo Oliva

Int. J. Mol. Sci. 2021, 22(21), 11627; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222111627 - 27 Oct 2021

Cited by 7 | Viewed by 1919

Abstract

The angiotensin-converting enzyme 2 (ACE2) is the receptor used by SARS-CoV and SARS-CoV-2 coronaviruses to attach to cells via the receptor-binding domain (RBD) of their viral spike protein. Since the start of the COVID-19 pandemic, several structures of protein complexes involving ACE2 and RBD as well as monoclonal antibodies and nanobodies have become available. We have leveraged the structural data to design peptides to target the interaction between the RBD of SARS-CoV-2 and ACE2 and SARS-CoV and ACE2, as contrasting exemplar, as well as the dimerization surface of ACE2 monomers. The peptides were modelled using our original method: PiPreD that uses native elements of the interaction between the targeted protein and cognate partner(s) that are subsequently included in the designed peptides. These peptides recapitulate stretches of residues present in the native interface plus novel and highly diverse conformations surrogating key interactions at the interface. To facilitate the access to this information we have created a freely available and dedicated web-based repository, PepI-Covid19 database, providing convenient access to this wealth of information to the scientific community with the view of maximizing its potential impact in the development of novel therapeutic and diagnostic agents. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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Review

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30 pages, 2819 KiB

Open AccessReview

Vasopressin and Its Analogues: From Natural Hormones to Multitasking Peptides

by Mladena Glavaš, Agata Gitlin-Domagalska, Dawid Dębowski, Natalia Ptaszyńska, Anna Łęgowska and Krzysztof Rolka

Int. J. Mol. Sci. 2022, 23(6), 3068; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23063068 - 12 Mar 2022

Cited by 21 | Viewed by 7545

Abstract

Human neurohormone vasopressin (AVP) is synthesized in overlapping regions in the hypothalamus. It is mainly known for its vasoconstricting abilities, and it is responsible for the regulation of plasma osmolality by maintaining fluid homeostasis. Over years, many attempts have been made to modify this hormone and find AVP analogues with different pharmacological profiles that could overcome its limitations. Non-peptide AVP analogues with low molecular weight presented good affinity to AVP receptors. Natural peptide counterparts, found in animals, are successfully applied as therapeutics; for instance, lypressin used in treatment of diabetes insipidus. Synthetic peptide analogues compensate for the shortcomings of AVP. Desmopressin is more resistant to proteolysis and presents mainly antidiuretic effects, while terlipressin is a long-acting AVP analogue and a drug recommended in the treatment of varicose bleeding in patients with liver cirrhosis. Recently published results on diverse applications of AVP analogues in medicinal practice, including potential lypressin, terlipressin and ornipressin in the treatment of SARS-CoV-2, are discussed. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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21 pages, 1502 KiB

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Prospects and Applications of Natural Blood-Derived Products in Regenerative Medicine

by Joanna Wessely-Szponder, Joanna Zdziennicka, Andrzej Junkuszew, Michał Latalski, Michał Świeca and Tomasz Szponder

Int. J. Mol. Sci. 2022, 23(1), 472; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23010472 - 31 Dec 2021

Cited by 6 | Viewed by 2038

Abstract

Currently, there are a number of therapeutic schemes used for the treatment of various types of musculoskeletal disorders. However, despite the use of new treatment options, therapeutic failure remains common due to impaired and delayed healing, or implant rejection. Faced with this challenge, in recent years regenerative medicine started looking for alternative solutions that could additionally support tissue regeneration. This review aims to outline the functions and possible clinical applications of, and future hopes associated with, using autologous or heterologous products such as antimicrobial peptides (AMPs), microvesicles (MVs), and neutrophil degranulation products (DGP) obtained from circulating neutrophils. Moreover, different interactions between neutrophils and platelets are described. Certain products released from neutrophils are critical for interactions between different immune cells to ensure adequate tissue repair. By acting directly and indirectly on host cells, these neutrophil-derived products can modulate the body’s inflammatory responses in various ways. The development of new formulations based on these products and their clinically proven success would give hope for significant progress in regenerative therapy in human and veterinary medicine. Full article

(This article belongs to the Special Issue Bioactive Peptides in Human Health and Disease)

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