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Peptides for Health Benefits

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 July 2018) | Viewed by 90653

Special Issue Editors


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Guest Editor
Instituto de Investigación en Ciencias de la Alimentación (CIAL), Consejo Superior de Investigaciones Científicas (CSIC). c/ Nicolás Cabrera 9, 28049 Madrid, Spain
Interests: bioactive peptides; food proteins; multifuncionality; digestion; bioavailability; inflammation-associated diseases; chemopreventive activity; peptidomics; antioxidant activity
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Institute of Food Science, Technology and Nutrition (ICTAN), Spanish National Research Council (CSIC), Jose Antonio Novais 10, 28040 Madrid, Spain
Interests: grains; peptides; phenolic compounds; nutritional characterization; protein quality and digestibility; bioavailability of food compounds; bioactivity; germination; fermentation; enzymatic treatments
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, peptides have received increased interest by the pharmaceutical industry. The high potency, specificity and good safety profile are the main strengths of bioactive peptides as new and promising therapies that may fill the gap between small molecules and protein drugs. These positive attributes of peptides, along with advances in drug delivery technologies, have afforded a renewed interest in the discovery, optimization and development of peptides as pharmacological therapy. Among bioactive peptides, those released from food protein sources have acquired importance as nutraceutical and active components in functional foods because they are known to possess regulatory functions that can lead to health benefits.

This Special Issue, “Peptides for Health Benefits”, will cover a selection of recent research papers, reviews, short communications, as well as perspectives in the field of bioactive peptides. It aims to cover all aspects of peptide research in relation to health promotion. In particular, this Special Issue emphasizes current knowledge and research trends concerning bioactive peptides, including identification and quantification of peptides from new sources, methods for their production and purification, structure-function relationships, mechanisms of action, development of novel in vitro and in vivo assays for the evaluation of their bioactivity, physiological evidence to support health benefits, and peptide stability, bioavailability, and sensory (or techno-functional) properties. Papers regarding the development of new drugs, functional foods or nutraceuticals based on bioactive peptides will be also taken into consideration.

Dr. Blanca Hernandez-Ledesma
Dr. Cristina Martínez-Villaluenga
Guest Editors

Manuscript Submission Information

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Keywords

  • Human health
  • Bioactive peptides
  • Food peptides
  • Biological activity
  • Peptidomics
  • In vitro and in vivo assays
  • Identification and characterization
  • Functional foods
  • Peptides-based therapies

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Published Papers (13 papers)

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Research

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15 pages, 1789 KiB  
Article
Identification and In Vivo Characterisation of Cardioactive Peptides in Drosophila melanogaster
by Ronja Schiemann, Kay Lammers, Maren Janz, Jana Lohmann, Achim Paululat and Heiko Meyer
Int. J. Mol. Sci. 2019, 20(1), 2; https://doi.org/10.3390/ijms20010002 - 20 Dec 2018
Cited by 6 | Viewed by 4949
Abstract
Neuropeptides and peptide hormones serve as critical regulators of numerous biological processes, including development, growth, reproduction, physiology, and behaviour. In mammals, peptidergic regulatory systems are complex and often involve multiple peptides that act at different levels and relay to different receptors. To improve [...] Read more.
Neuropeptides and peptide hormones serve as critical regulators of numerous biological processes, including development, growth, reproduction, physiology, and behaviour. In mammals, peptidergic regulatory systems are complex and often involve multiple peptides that act at different levels and relay to different receptors. To improve the mechanistic understanding of such complex systems, invertebrate models in which evolutionarily conserved peptides and receptors regulate similar biological processes but in a less complex manner have emerged as highly valuable. Drosophila melanogaster represents a favoured model for the characterisation of novel peptidergic signalling events and for evaluating the relevance of those events in vivo. In the present study, we analysed a set of neuropeptides and peptide hormones for their ability to modulate cardiac function in semi-intact larval Drosophila melanogaster. We identified numerous peptides that significantly affected heart parameters such as heart rate, systolic and diastolic interval, rhythmicity, and contractility. Thus, peptidergic regulation of the Drosophila heart is not restricted to chronotropic adaptation but also includes inotropic modulation. By specifically interfering with the expression of corresponding peptides in transgenic animals, we assessed the in vivo relevance of the respective peptidergic regulation. Based on the functional conservation of certain peptides throughout the animal kingdom, the identified cardiomodulatory activities may be relevant not only to proper heart function in Drosophila, but also to corresponding processes in vertebrates, including humans. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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14 pages, 4149 KiB  
Article
Dissection of the Structural Features of a Fungicidal Antibody-Derived Peptide
by Thelma A. Pertinhez, Tecla Ciociola, Laura Giovati, Walter Magliani, Silvana Belletti, Luciano Polonelli, Stefania Conti and Alberto Spisni
Int. J. Mol. Sci. 2018, 19(12), 3792; https://doi.org/10.3390/ijms19123792 - 28 Nov 2018
Cited by 5 | Viewed by 2734
Abstract
The synthetic peptide T11F (TCRVDHRGLTF), derived from the constant region of human IgM antibodies, proved to exert a significant activity in vitro against yeast strains, including multidrug resistant isolates. Alanine substitution of positively charged residues led to a decrease in candidacidal activity. A [...] Read more.
The synthetic peptide T11F (TCRVDHRGLTF), derived from the constant region of human IgM antibodies, proved to exert a significant activity in vitro against yeast strains, including multidrug resistant isolates. Alanine substitution of positively charged residues led to a decrease in candidacidal activity. A more dramatic reduction in activity resulted from cysteine replacement. Here, we investigated the conformational properties of T11F and its alanine-substituted derivatives by circular dichroism (CD) and nuclear magnetic resonance (NMR) spectroscopy. Peptide interaction with Candida albicans cells was studied by confocal and scanning electron microscopy. T11F and most of its derivatives exhibited CD spectra with a negative band around 200 nm and a weaker positive band around 218 nm suggesting, together with NMR coupling constants, the presence of a polyproline II (PPII) helix, a conformational motif involved in a number of biological functions. Analysis of CD spectra revealed a critical role for phenylalanine in preserving the PPII helix. In fact, only the F11A derivative presented a random coil conformation. Interestingly, the loss of secondary structure influenced the rate of killing, which turned out to be significantly reduced. Overall, the obtained results suggest that the PPII conformation contributes in characterising the cell penetrating and fungicidal properties of the investigated peptides. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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12 pages, 3320 KiB  
Article
AWRK6, a Novel GLP-1 Receptor Agonist, Attenuates Diabetes by Stimulating Insulin Secretion
by Qiuyu Wang, Chunlin Zhao, Lili Jin, Hanyu Zhang, Qifan Miao, Hongsheng Liu and Dianbao Zhang
Int. J. Mol. Sci. 2018, 19(10), 3053; https://doi.org/10.3390/ijms19103053 - 7 Oct 2018
Cited by 7 | Viewed by 3521
Abstract
Diabetes is a metabolic disorder leading to many complications. The treatment of diabetes mainly depends on hypoglycemic drugs, often with side effects, which drive us to develop novel agents. AWRK6 was a peptide developed from the antimicrobial peptide Dybowskin-2CDYa in our previous study, [...] Read more.
Diabetes is a metabolic disorder leading to many complications. The treatment of diabetes mainly depends on hypoglycemic drugs, often with side effects, which drive us to develop novel agents. AWRK6 was a peptide developed from the antimicrobial peptide Dybowskin-2CDYa in our previous study, and the availability of AWRK6 on diabetes intervention was unknown. Here, in vivo and in vitro experiments were carried out to investigate the effects of AWRK6 against diabetes. In diabetic mice, induced by high-fat diet followed by streptozocin (STZ) administration, the daily administration of AWRK6 presented acute and sustained hypoglycemic effects. The plasma insulin was significantly elevated by AWRK6 during an oral glucose tolerance test (OGTT). The relative β cell mass in diabetic mice was increased by AWRK6 treatment. The body weight and food intake were remarkably reduced by AWRK6 administration. In the mouse pancreatic β cell line Min6 cells, the intracellular calcium concentration was found to be enhanced under the treatment with AWRK6, and protein kinase A (PKA) inhibitor H-89 and Epac2 inhibitor HJC0350 represented inhibitory effects of the insulinotropic function of AWRK6. By FITC-AWRK6 incubation and GLP-1 receptor (GLP-1R) knockdown, AWRK6 proved to be a novel GLP-1R agonist. In addition, AWRK6 showed no toxicity in cell viability and membrane integrity in Min6 cells, and no hypoglycemia risk and no lethal toxicity in mice. In summary, AWRK6 was found as a novel agonist of GLP-1R, which could stimulate insulin secretion to regulate blood glucose and energy metabolism, via cAMP-calcium signaling pathway, without significant toxicity. The peptide AWRK6 might become a novel candidate for diabetes treatment. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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14 pages, 1543 KiB  
Article
Bioactive Peptides from Germinated Soybean with Anti-Diabetic Potential by Inhibition of Dipeptidyl Peptidase-IV, α-Amylase, and α-Glucosidase Enzymes
by Marcela González-Montoya, Blanca Hernández-Ledesma, Rosalva Mora-Escobedo and Cristina Martínez-Villaluenga
Int. J. Mol. Sci. 2018, 19(10), 2883; https://doi.org/10.3390/ijms19102883 - 22 Sep 2018
Cited by 125 | Viewed by 7832
Abstract
Functional foods containing peptides offer the possibility to modulate the absorption of sugars and insulin levels to prevent diabetes. This study investigates the potential of germinated soybean peptides to modulate postprandial glycaemic response through inhibition of dipeptidyl peptidase IV (DPP-IV), salivary α-amylase, and [...] Read more.
Functional foods containing peptides offer the possibility to modulate the absorption of sugars and insulin levels to prevent diabetes. This study investigates the potential of germinated soybean peptides to modulate postprandial glycaemic response through inhibition of dipeptidyl peptidase IV (DPP-IV), salivary α-amylase, and intestinal α-glucosidases. A protein isolate from soybean sprouts was digested by pepsin and pancreatin. Protein digest and peptide fractions obtained by ultrafiltration (<5, 5–10 and >10 kDa) and subsequent semipreparative reverse phase liquid chromatography (F1, F2, F3, and F4) were screened for in vitro inhibition of DPP-IV, α-amylase, maltase, and sucrase activities. Protein digest inhibited DPP-IV (IC50 = 1.49 mg/mL), α-amylase (IC50 = 1.70 mg/mL), maltase, and sucrase activities of α-glucosidases (IC50 = 3.73 and 2.90 mg/mL, respectively). Peptides of 5–10 and >10 kDa were more effective at inhibiting DPP-IV (IC50 = 0.91 and 1.18 mg/mL, respectively), while peptides of 5–10 and <5 kDa showed a higher potency to inhibit α-amylase and α-glucosidases. Peptides in F1, F2, and F3 were mainly fragments from β-conglycinin, glycinin, and P34 thiol protease. The analysis of structural features of peptides in F1–F3 allowed the tentative identification of potential antidiabetic peptides. Germinated soybean protein showed a promising potential to be used as a nutraceutical or functional ingredient for diabetes prevention. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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21 pages, 7809 KiB  
Article
A Dairy-Derived Ghrelinergic Hydrolysate Modulates Food Intake In Vivo
by Ken Howick, Shauna E. Wallace-Fitzsimons, Dalia Kandil, Barbara Chruścicka, Mert Calis, Eoin Murphy, Brian A. Murray, Ayoa Fernandez, Kate M. Barry, Phil M. Kelly, Aoife M. Ryan, John F. Cryan, Brendan T. Griffin and Harriët Schellekens
Int. J. Mol. Sci. 2018, 19(9), 2780; https://doi.org/10.3390/ijms19092780 - 15 Sep 2018
Cited by 5 | Viewed by 4411
Abstract
Recent times have seen an increasing move towards harnessing the health-promoting benefits of food and dietary constituents while providing scientific evidence to substantiate their claims. In particular, the potential for bioactive protein hydrolysates and peptides to enhance health in conjunction with conventional pharmaceutical [...] Read more.
Recent times have seen an increasing move towards harnessing the health-promoting benefits of food and dietary constituents while providing scientific evidence to substantiate their claims. In particular, the potential for bioactive protein hydrolysates and peptides to enhance health in conjunction with conventional pharmaceutical therapy is being investigated. Dairy-derived proteins have been shown to contain bioactive peptide sequences with various purported health benefits, with effects ranging from the digestive system to cardiovascular circulation, the immune system and the central nervous system. Interestingly, the ability of dairy proteins to modulate metabolism and appetite has recently been reported. The ghrelin receptor (GHSR-1a) is a G-protein coupled receptor which plays a key role in the regulation of food intake. Pharmacological manipulation of the growth hormone secretagogue receptor-type 1a (GHSR-1a) receptor has therefore received a lot of attention as a strategy to combat disorders of appetite and body weight, including age-related malnutrition and the progressive muscle wasting syndrome known as cachexia. In this study, a milk protein-derivative is shown to increase GHSR-1a-mediated intracellular calcium signalling in a concentration-dependent manner in vitro. Significant increases in calcium mobilisation were also observed in a cultured neuronal cell line heterologously expressing the GHS-R1a. In addition, both additive and synergistic effects were observed following co-exposure of GHSR-1a to both the hydrolysate and ghrelin. Subsequent in vivo studies monitored standard chow intake in healthy male and female Sprague-Dawley rats after dosing with the casein hydrolysate (CasHyd). Furthermore, the provision of gastro-protected oral delivery to the bioactive in vivo may aid in the progression of in vitro efficacy to in vivo functionality. In summary, this study reports a ghrelin-stimulating bioactive peptide mixture (CasHyd) with potent effects in vitro. It also provides novel and valuable translational data supporting the potential role of CasHyd as an appetite-enhancing bioactive. Further mechanistic studies are required in order to confirm efficacy as a ghrelinergic bioactive in susceptible population groups. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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13 pages, 3431 KiB  
Article
Therapeutic Peptide Amphiphile as a Drug Carrier with ATP-Triggered Release for Synergistic Effect, Improved Therapeutic Index, and Penetration of 3D Cancer Cell Spheroids
by Sheng Lu, Feng Zhao, Qiuxin Zhang and P. Chen
Int. J. Mol. Sci. 2018, 19(9), 2773; https://doi.org/10.3390/ijms19092773 - 14 Sep 2018
Cited by 13 | Viewed by 4746
Abstract
Despite the great progress in the field of drug delivery systems for cancer treatment over the last decade, many challenges still lie ahead, such as low drug loading, deep penetration of tumors, side effects, and the development of drug resistance. A class of [...] Read more.
Despite the great progress in the field of drug delivery systems for cancer treatment over the last decade, many challenges still lie ahead, such as low drug loading, deep penetration of tumors, side effects, and the development of drug resistance. A class of cationic membrane lytic peptides has shown potential as an anticancer agent by inducing cancer cell death via membrane disruption; meanwhile, their intrinsic selectivity renders them as having low cytotoxicity towards noncancerous cells. Here, we report the use of a cationic peptide amphiphile (PA), named PAH6, to load doxorubicin (Dox) that is intercalated in an ATP-binding aptamer-incorporated DNA scaffold. The PA contains a cationic lytic sequence, (KLAKLAK)2, a polyhistidine segment for the “proton sponge” effect, and a hydrophobic alkyl tail to drive the self-assembly. Dox-loaded DNA was found to form a spherical nanocomplex (NC) with PAH6 with particle sizes below 100 nm at various ratios. Since the carrier PAH6 is also a therapeutic agent, the drug loadings of the NC reached up to ~86% within the ratios we tested, and Dox was released from the NC in an ATP-rich environment. In vitro studies indicate that the presence of PAH6 could permeabilize cell membranes and kill cells through fast membrane disruption and depolarization of mitochondrial membranes. The cytotoxicity tests were conducted using A549 nonsmall cell lung cancer cells and NIH-3T3 fibroblast cells. PAH6 showed selectivity towards A549 cells. Significantly, the Dox-DNA/PAH6 NC exhibited a synergistic effect against A549 cells, with the IC50 decreased up to ~90% for Dox and ~69% for PAH6 when compared to the IC50 values of the two components, respectively. Furthermore, the selectivity of PAH6 conferred to the complex an improved therapeutic index between A549 and NIH-3T3 cells. A 3D-cultured A549 spheroid model was adopted to test the capability of Dox-DNA/PAH6 for tumor penetration. The PAH6 or Dox-DNA/PAH6 complex was found to break the spheroids into pieces, while Dox-treated spheroids maintained their shapes. In summary, this work provides a new strategy for constructing nanomedicines using therapeutic agents to meet the features required by anticancer treatment. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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12 pages, 3325 KiB  
Article
A Synthetic Peptide AWRK6 Alleviates Lipopolysaccharide-Induced Liver Injury
by Lili Jin, Qiuyu Wang, Hanyu Zhang, Sijia Tai, Hongsheng Liu and Dianbao Zhang
Int. J. Mol. Sci. 2018, 19(9), 2661; https://doi.org/10.3390/ijms19092661 - 7 Sep 2018
Cited by 11 | Viewed by 4128
Abstract
During lipopolysaccharide (LPS)-induced sepsis, the liver plays central roles in toxins phagocytosis and clearance to protect the whole body. The liver cells were constantly irritated by LPS which leads to liver injury. While most anti-LPS agents showed little clinical activity against LPS-induced liver [...] Read more.
During lipopolysaccharide (LPS)-induced sepsis, the liver plays central roles in toxins phagocytosis and clearance to protect the whole body. The liver cells were constantly irritated by LPS which leads to liver injury. While most anti-LPS agents showed little clinical activity against LPS-induced liver injury. Here, the protective effects of the synthetic peptide AWRK6 against LPS-induced liver injury have been investigated in vivo and in vitro. In mice liver homogenate, LPS administration elevated ALT (alanine aminotransferase), iNOS (inducible nitric oxide synthase) and repressed SOD (superoxide dismutase) activities and these changes were remarkably reversed by AWRK6. Histologically, AWRK6 effectively alleviated the histological changes and repressed LPS-induced neutrophils infiltration. By TUNEL assay on liver sections, AWRK6 was proven to inhibit apoptosis induced by LPS in mice livers, which was also verified by the protein levels of cleaved-caspase 9, Bax and Bcl-2. In addition, by in vitro study using HepG2 cells, AWRK6 was found to recover the LPS-reduced cell viability and reduce LPS-induced apoptosis. For mechanisms, AWRK6 was demonstrated to alleviate the LPS-induced phosphorylation of ERK, JNK and p38 MAPK, indicating the involvement of MAPKs in the protection of AWRK6 against liver injury. In summary, we have found the synthetic peptide AWRK6 as a promising novel agent for LPS-induced liver injury, by inhibiting cell apoptosis through MAPK signaling pathways, which might bring new strategies for the treatment of acute and chronic liver injuries. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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14 pages, 1775 KiB  
Article
Antioxidant Properties of Buffalo-Milk Dairy Products: A β-Lg Peptide Released after Gastrointestinal Digestion of Buffalo Ricotta Cheese Reduces Oxidative Stress in Intestinal Epithelial Cells
by Manuela Giovanna Basilicata, Giacomo Pepe, Simona Adesso, Carmine Ostacolo, Marina Sala, Eduardo Sommella, Maria Carmina Scala, Antonella Messore, Giuseppina Autore, Stefania Marzocco and Pietro Campiglia
Int. J. Mol. Sci. 2018, 19(7), 1955; https://doi.org/10.3390/ijms19071955 - 4 Jul 2018
Cited by 41 | Viewed by 5516
Abstract
Redox signaling regulates different gastrointestinal (G.I.) epithelium functions. At the intestinal level, the loss of redox homeostasis in intestinal epithelial cells (IECs) is responsible for the pathogenesis and development of a wide diversity of G.I. disorders. Thus, the manipulation of oxidative stress in [...] Read more.
Redox signaling regulates different gastrointestinal (G.I.) epithelium functions. At the intestinal level, the loss of redox homeostasis in intestinal epithelial cells (IECs) is responsible for the pathogenesis and development of a wide diversity of G.I. disorders. Thus, the manipulation of oxidative stress in IECs could represent an important pharmacological target for different diseases. In this study, peptides released from in vitro gastro intestinal digestion of different buffalo-milk commercial dairy products were identified and evaluated for their bioactive properties. In particular, six G.I. digests of dairy products were tested in a model of oxidative stress for IECs. Among them, buffalo ricotta cheese was the most active and the presence of an abundant β-lactoglobulin peptide (YVEELKPTPEGDL, f:60-72) was also revealed. The antioxidant potential of the identified peptide was also evaluated in a model of hydrogen peroxide (H2O2)-induced oxidative stress in the IEC-6 cell line. The peptide was able to reduce ROS release, while, on the other hand, it increased nuclear factor (erythroid-derived 2)-like 2 (Nrf2) activation and the expression of antioxidant cytoprotective factors, such as heme oxygenase 1 (HO-1), NAD(P)H:quinone oxidoreductase 1 (NQO1), and superoxide dismutase (SOD). These results indicate that buffalo ricotta cheese-isolated peptide could have potential in the treatment of some gastrointestinal disorders. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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15 pages, 7898 KiB  
Article
Amyloid Beta Peptide Is Released during Thrombosis in the Skin
by Lilia Y. Kucheryavykh, Yuriy V. Kucheryavykh, A. Valance Washington and Mikhail Y. Inyushin
Int. J. Mol. Sci. 2018, 19(6), 1705; https://doi.org/10.3390/ijms19061705 - 8 Jun 2018
Cited by 14 | Viewed by 6113
Abstract
While it is known that amyloid beta (Aβ) deposits are found in different tissues of both Alzheimer’s disease (AD) patients and healthy individuals, there remain questions about the physiological role of these deposits, the origin of the Aβ peptide, and the mechanisms of [...] Read more.
While it is known that amyloid beta (Aβ) deposits are found in different tissues of both Alzheimer’s disease (AD) patients and healthy individuals, there remain questions about the physiological role of these deposits, the origin of the Aβ peptide, and the mechanisms of its localization to the tissues. Using immunostaining with specific antibodies, as well as enzyme-linked immunosorbent assay, this study demonstrated Aβ40 peptide accumulation in the skin during local experimental photothrombosis in mice. Specifically, Aβ peptide accumulation was concentrated near the dermal blood vessels in thrombotic skin. It was also studied whether the released peptide affects microorganisms. Application of Aβ40 (4 µM) to the external membrane of yeast cells significantly increased membrane conductance with no visible effect on mouse host cells. The results suggest that Aβ release in the skin is related to skin injury and thrombosis, and occurs along with clotting whenever skin is damaged. These results support the proposition that Aβ release during thrombosis serves as part of a natural defense against infection. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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18 pages, 8343 KiB  
Article
Tryptophan-Containing Dual Neuroprotective Peptides: Prolyl Endopeptidase Inhibition and Caenorhabditis elegans Protection from β-Amyloid Peptide Toxicity
by Paloma Manzanares, Roberto Martínez, Sandra Garrigues, Salvador Genovés, Daniel Ramón, Jose F. Marcos and Patricia Martorell
Int. J. Mol. Sci. 2018, 19(5), 1491; https://doi.org/10.3390/ijms19051491 - 16 May 2018
Cited by 12 | Viewed by 4458
Abstract
Neuroprotective peptides represent an attractive pharmacological strategy for the prevention or treatment of age-related diseases, for which there are currently few effective therapies. Lactoferrin (LF)-derived peptides (PKHs) and a set of six rationally-designed tryptophan (W)-containing heptapeptides (PACEIs) were characterized as prolyl endopeptidase (PEP) [...] Read more.
Neuroprotective peptides represent an attractive pharmacological strategy for the prevention or treatment of age-related diseases, for which there are currently few effective therapies. Lactoferrin (LF)-derived peptides (PKHs) and a set of six rationally-designed tryptophan (W)-containing heptapeptides (PACEIs) were characterized as prolyl endopeptidase (PEP) inhibitors, and their effect on β-amyloid peptide (Aβ) toxicity in a Caenorhabditis elegans model of Alzheimer’s disease (AD) was evaluated. Two LF-derived sequences, PKH8 and PKH11, sharing a W at the C-terminal end, and the six PACEI heptapeptides (PACEI48L to PACEI53L) exhibited significant in vitro PEP inhibition. The inhibitory peptides PKH11 and PACEI50L also alleviated Aβ-induced paralysis in the in vivo C. elegans model of AD. Partial or total loss of the inhibitory effect on PEP was achieved by the substitution of W residues in PKH11 and PACEI50L and correlated with the loss of protection against Aβ toxicity, pointing out the relevance of W on the neuroprotective activity. Further experiments suggest that C. elegans protection might not be mediated by an antioxidant mechanism but rather by inhibition of Aβ oligomerization and thus, amyloid deposition. In conclusion, novel natural and rationally-designed W-containing peptides are suitable starting leads to design effective neuroprotective agents. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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12 pages, 3887 KiB  
Article
AWRK6, A Synthetic Cationic Peptide Derived from Antimicrobial Peptide Dybowskin-2CDYa, Inhibits Lipopolysaccharide-Induced Inflammatory Response
by Qiuyu Wang, Lili Jin, Huan Wang, Sijia Tai, Hongsheng Liu and Dianbao Zhang
Int. J. Mol. Sci. 2018, 19(2), 600; https://doi.org/10.3390/ijms19020600 - 17 Feb 2018
Cited by 20 | Viewed by 4414
Abstract
Lipopolysaccharides (LPS) are major outer membrane components of Gram-negative bacteria and produce strong inflammatory responses in animals. Most antibiotics have shown little clinical anti-endotoxin activity while some antimicrobial peptides have proved to be effective in blocking LPS. Here, the anti-LPS activity of the [...] Read more.
Lipopolysaccharides (LPS) are major outer membrane components of Gram-negative bacteria and produce strong inflammatory responses in animals. Most antibiotics have shown little clinical anti-endotoxin activity while some antimicrobial peptides have proved to be effective in blocking LPS. Here, the anti-LPS activity of the synthetic peptide AWRK6, which is derived from antimicrobial peptide dybowskin-2CDYa, has been investigated in vitro and in vivo. The positively charged α-helical AWRK6 was found to be effective in blocking the binding of LBP (LPS binding protein) with LPS in vitro using ELISA. In a murine endotoxemia model, AWRK6 offered satisfactory protection efficiency against endotoxemia death, and the serum levels of LPS, IL-1β, IL-6, and TNF-α were found to be attenuated using ELISA. Further, histopathological analysis suggested that AWRK6 could improve the healing of liver and lung injury in endotoxemia mice. The results of real-time PCR and Western blotting showed that AWRK6 significantly reversed LPS-induced TLR4 overexpression and IκB depression, as well as the enhanced IκB phosphorylation. Additionally, AWRK6 did not produce any significant toxicity in vivo and in vitro. In summary, AWRK6 showed efficacious protection from LPS challenges in vivo and in vitro, by blocking LPS binding to LBP, without obvious toxicity, providing a promising strategy against LPS-induced inflammatory responses. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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Review

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18 pages, 975 KiB  
Review
Peptides as Therapeutic Agents for Inflammatory-Related Diseases
by Sara La Manna, Concetta Di Natale, Daniele Florio and Daniela Marasco
Int. J. Mol. Sci. 2018, 19(9), 2714; https://doi.org/10.3390/ijms19092714 - 11 Sep 2018
Cited by 100 | Viewed by 8211
Abstract
Inflammation is a physiological mechanism used by organisms to defend themselves against infection, restoring homeostasis in damaged tissues. It represents the starting point of several chronic diseases such as asthma, skin disorders, cancer, cardiovascular syndrome, arthritis, and neurological diseases. An increasing number of [...] Read more.
Inflammation is a physiological mechanism used by organisms to defend themselves against infection, restoring homeostasis in damaged tissues. It represents the starting point of several chronic diseases such as asthma, skin disorders, cancer, cardiovascular syndrome, arthritis, and neurological diseases. An increasing number of studies highlight the over-expression of inflammatory molecules such as oxidants, cytokines, chemokines, matrix metalloproteinases, and transcription factors into damaged tissues. The treatment of inflammatory disorders is usually linked to the use of unspecific small molecule drugs that can cause undesired side effects. Recently, many efforts are directed to develop alternative and more selective anti-inflammatory therapies, several of them imply the use of peptides. Indeed, peptides demonstrated as elected lead compounds toward several targets for their high specificity as well as recent and innovative synthetic strategies. Several endogenous peptides identified during inflammatory responses showed anti-inflammatory activities by inhibiting, reducing, and/or modulating the expression and activity of mediators. This review aims to discuss the potentialities and therapeutic use of peptides as anti-inflammatory agents in the treatment of different inflammation-related diseases and to explore the importance of peptide-based therapies. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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13 pages, 234 KiB  
Review
Regenerative and Protective Actions of the GHK-Cu Peptide in the Light of the New Gene Data
by Loren Pickart and Anna Margolina
Int. J. Mol. Sci. 2018, 19(7), 1987; https://doi.org/10.3390/ijms19071987 - 7 Jul 2018
Cited by 52 | Viewed by 28312
Abstract
The human peptide GHK (glycyl-l-histidyl-l-lysine) has multiple biological actions, all of which, according to our current knowledge, appear to be health positive. It stimulates blood vessel and nerve outgrowth, increases collagen, elastin, and glycosaminoglycan synthesis, as well as supports [...] Read more.
The human peptide GHK (glycyl-l-histidyl-l-lysine) has multiple biological actions, all of which, according to our current knowledge, appear to be health positive. It stimulates blood vessel and nerve outgrowth, increases collagen, elastin, and glycosaminoglycan synthesis, as well as supports the function of dermal fibroblasts. GHK’s ability to improve tissue repair has been demonstrated for skin, lung connective tissue, boney tissue, liver, and stomach lining. GHK has also been found to possess powerful cell protective actions, such as multiple anti-cancer activities and anti-inflammatory actions, lung protection and restoration of chronic obstructive pulmonary disease (COPD) fibroblasts, suppression of molecules thought to accelerate the diseases of aging such as NFκB, anti-anxiety, anti-pain and anti-aggression activities, DNA repair, and activation of cell cleansing via the proteasome system. Recent genetic data may explain such diverse protective and healing actions of one molecule, revealing multiple biochemical pathways regulated by GHK. Full article
(This article belongs to the Special Issue Peptides for Health Benefits)
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