Special Issue "Marine-Derived Biomolecules"

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Natural and Bio-inspired Molecules".

Deadline for manuscript submissions: closed (15 May 2020).

Special Issue Editor

Prof. Dr. Diaa Youssef
Website SciProfiles
Guest Editor
Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia & Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal university, Ismailia 41522, Egypt
Interests: natural products chemistry; biomolecules; structure determination; antitumor and antibiotics of marine origin; microbial natural products; drug discovery; biotechnology; symbiosis in marine organisms; marine toxins; macromolecules of marine origin; chitin

Special Issue Information

Dear Colleagues,

The world’s Oceans have been shown to provide a rich place with great biodiversity and chemical entities with proven bioactivities related to cancer, inflammation, epilepsy, the immunomodulatory system, microbial and parasitic infections, and many others. Currently, there are eight approved drugs of marine origin and more than 22 other chemical entities in different clinical phases. Marine invertebrates and micro-organisms represent the major sources for these compounds.

The advantages of studying organisms from the marine environment lie primarily in the breadth of marine biodiversity and the consequent variety of new chemical structures found among marine natural products. Attesting to the tremendous diversity of marine life is the fact that of the 33 animal phyla, 32 are found in the sea, while only 12 occur on land. The larger genetic pool found in the marine environment has resulted in the synthesis of a wide variety of chemicals that can be exploited in a systematic screening program. Many of the primitive phyla that have evolved over the greatest time in the sea appear to have done so using survival mechanisms based on chemical synthesis. The compounds that are responsible for the successful survival of marine organisms possess significant biological activities that often interfere with the essential growth or biosynthetic mechanisms of competing organisms. These are precisely the types of chemicals that might be expected to be active in cancer-related bioassays. Over many millions of years of evolution, marine animals have evolved molecules with high binding affinities toward intracellular targets. The opportunity to apply these “evolutionarily significant molecules” within a mechanism-based drug discovery program is thus a rational approach to targeted drug discovery.

This Special Issue on “Marine-Derived Biomolecules” in Biomolecules will cover all scopes of bioassay-directed fractionation of extracts, purification, and structure mapping of marine-derived molecules as well as their biological activities. Biomolecules from marine macro-organisms and/or microbes, new assays’ development, metabolomics, and dereplication of compounds will be targeted in this issue.

As a Special Issue Editor, I invite all colleagues who are actively involved in research related to the marine biomolecules to share their latest findings and results with other colleagues working in the same field. I hope that this Special Issue will provide deep insights into the importance of marine-derived biomolecules as a future source for drug discovery. I also hope that this issue will inspire junior scientists to look for the huge biodiversity of the marine environment and its future impact as leading sources for drug discovery and development.

Prof. Dr. Diaa Youssef
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomolecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • marine macro-organisms and micro-organisms
  • bioassay-directed fractionation of extracts
  • development of new assays for targeting biomolecules
  • structure determination of small molecules
  • bioactivity and drug leads of marine origin
  • metabolomics and dereplication of compounds
  • biologically active macromolecules

Published Papers (7 papers)

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Research

Open AccessArticle
Profiling and Role of Bioactive Molecules from Puntius sophore (Freshwater/Brackish Fish) Skin Mucus with Its Potent Antibacterial, Antiadhesion, and Antibiofilm Activities
Biomolecules 2020, 10(6), 920; https://doi.org/10.3390/biom10060920 - 17 Jun 2020
Cited by 1
Abstract
Epidermal fish mucus comprises of diverse bioactive metabolites which plays an immense role in defense mechanisms and other important cellular activities. Primarily, this study aims to screen the unexplored mucus extract of Puntius sophore (P. sophore) for its antagonistic potential against [...] Read more.
Epidermal fish mucus comprises of diverse bioactive metabolites which plays an immense role in defense mechanisms and other important cellular activities. Primarily, this study aims to screen the unexplored mucus extract of Puntius sophore (P. sophore) for its antagonistic potential against common pathogens, which are commonly implicated in foodborne and healthcare associated infections, with effects on their adhesion and biofilm formation. Profiling of the skin mucus was carried out by High Resolution-Liquid Chromatography Mass Spectrometry (HR-LCMS), followed by antibacterial activity and assessment of antibiofilm potency and efficacy on the development, formation, and texture of biofilms. Furthermore, bacterial cell damage, viability within the biofilm, checkerboard test, and cytotoxicity were also evaluated. As a result, P. sophore mucus extract was found to be effective against all tested strains. It also impedes the architecture of biofilm matrix by affecting the viability and integrity of bacterial cells within biofilms and reducing the total exopolysaccharide content. A synergy was observed between P. sophore mucus extract and gentamicin for Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa), and Bacillus subtilis (B. subtilis), whereas, an additive effect for Staphylococcus aureus (S. aureus). Thus, our findings represent the potent bioactivities of P. sophore mucus extract for the first time, which could be explored further as an alternative to antibiotics or chemically synthesized antibiofilm agents. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models
Biomolecules 2020, 10(5), 675; https://doi.org/10.3390/biom10050675 - 27 Apr 2020
Abstract
Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach’s [...] Read more.
Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach’s low pH, enzymatic content, and poor absorption in the gastrointestinal tract. Polymers with marine source like chitosan are commonly used in nanotechnology and drug delivery due to their biocompatibility and special features. This work focuses on the preparation and characterization of mucoadhesive insulin-loaded polymeric nanoparticles. Results showed a suitable mean size for oral administration (<600 nm by dynamic laser scattering), spherical shape, encapsulation efficiency (59.8%), and high recovery yield (80.6%). Circular dichroism spectroscopy demonstrated that protein retained its secondary structure after encapsulation. Moreover, the mucoadhesive potential of the nanoparticles was assessed in silico and the results, corroborated with ex-vivo experiments, showed that using chitosan strongly increases mucoadhesion. Besides, in vitro and in vivo safety assessment of the final formulation were performed, showing no toxicity. Lastly, the insulin-loaded nanoparticles were effective in reducing diabetic rats’ glycemia. Overall, the coating of insulin-loaded nanoparticles with chitosan represents a potentially safe and promising approach to protect insulin and enhance peroral delivery. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
3D Chitin Scaffolds from the Marine Demosponge Aplysina archeri as a Support for Laccase Immobilization and Its Use in the Removal of Pharmaceuticals
Biomolecules 2020, 10(4), 646; https://doi.org/10.3390/biom10040646 - 22 Apr 2020
Cited by 1
Abstract
For the first time, 3D chitin scaffolds from the marine demosponge Aplysina archeri were used for adsorption and immobilization of laccase from Trametes versicolor. The resulting chitin–enzyme biocatalytic systems were applied in the removal of tetracycline. Effective enzyme immobilization was confirmed by [...] Read more.
For the first time, 3D chitin scaffolds from the marine demosponge Aplysina archeri were used for adsorption and immobilization of laccase from Trametes versicolor. The resulting chitin–enzyme biocatalytic systems were applied in the removal of tetracycline. Effective enzyme immobilization was confirmed by scanning electron microscopy. Immobilization yield and kinetic parameters were investigated in detail, in addition to the activity of the enzyme after immobilization. The designed systems were further used for the removal of tetracycline under various process conditions. Optimum process conditions, enabling total removal of tetracycline from solutions at concentrations up to 1 mg/L, were found to be pH 5, temperature between 25 and 35 °C, and 1 h process duration. Due to the protective effect of the chitinous scaffolds and stabilization of the enzyme by multipoint attachment, the storage stability and thermal stability of the immobilized biomolecules were significantly improved as compared to the free enzyme. The produced biocatalytic systems also exhibited good reusability, as after 10 repeated uses they removed over 90% of tetracycline from solution. Finally, the immobilized laccase was used in a packed bed reactor for continuous removal of tetracycline, and enabled the removal of over 80% of the antibiotic after 24 h of continuous use. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
Meridianins and Lignarenone B as Potential GSK3β Inhibitors and Inductors of Structural Neuronal Plasticity
Biomolecules 2020, 10(4), 639; https://doi.org/10.3390/biom10040639 - 21 Apr 2020
Abstract
Glycogen Synthase Kinase 3 (GSK3) is an essential protein, with a relevant role in many diseases such as diabetes, cancer and neurodegenerative disorders. Particularly, the isoform GSK3β is related to pathologies such as Alzheimer’s disease (AD). This enzyme constitutes a very interesting target [...] Read more.
Glycogen Synthase Kinase 3 (GSK3) is an essential protein, with a relevant role in many diseases such as diabetes, cancer and neurodegenerative disorders. Particularly, the isoform GSK3β is related to pathologies such as Alzheimer’s disease (AD). This enzyme constitutes a very interesting target for the discovery and/or design of new therapeutic agents against AD due to its relation to the hyperphosphorylation of the microtubule-associated protein tau (MAPT), and therefore, its contribution to neurofibrillary tangles (NFT) formation. An in silico target profiling study identified two marine molecular families, the indole alkaloids meridianins from the tunicate genus Aplidium, and lignarenones, the secondary metabolites of the shelled cephalaspidean mollusc Scaphander lignarius, as possible GSK3β inhibitors. The analysis of the surface of GSK3β, aimed to find possible binding regions, and the subsequent in silico binding studies revealed that both marine molecular families can act over the ATP and/or substrate binding regions. The predicted inhibitory potential of the molecules from these two chemical families was experimentally validated in vitro by showing a ~50% of increased Ser9 phosphorylation levels of the GSK3β protein. Furthermore, we determined that molecules from both molecular families potentiate structural neuronal plasticity in vitro. These results allow us to suggest that meridianins and lignarenone B could be used as possible therapeutic candidates for the treatment of GSK3β involved pathologies, such as AD. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
Cyclin-Dependent Kinase 5 Inhibitor Butyrolactone I Elicits a Partial Agonist Activity of Peroxisome Proliferator-Activated Receptor γ
Biomolecules 2020, 10(2), 275; https://doi.org/10.3390/biom10020275 - 11 Feb 2020
Abstract
Adiponectin is an adipocyte-derived cytokine having an insulin-sensitizing activity. During the phenotypic screening of secondary metabolites derived from the marine fungus Aspergillus terreus, a poly cyclin-dependent kinase (CDK) inhibitor butyrolactone I affecting CDK1 and CDK5 was discovered as a potent adiponectin production-enhancing [...] Read more.
Adiponectin is an adipocyte-derived cytokine having an insulin-sensitizing activity. During the phenotypic screening of secondary metabolites derived from the marine fungus Aspergillus terreus, a poly cyclin-dependent kinase (CDK) inhibitor butyrolactone I affecting CDK1 and CDK5 was discovered as a potent adiponectin production-enhancing compound in the adipogenesis model of human bone marrow-derived mesenchymal stem cells (hBM-MSCs). CDK5 inhibitors exhibit insulin-sensitizing activities by suppressing the phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ). However, the adiponectin production-enhancing activities of butyrolactone I have not been correlated with the potency of CDK5 inhibitor activities. In a target identification study, butyrolactone I was found to directly bind to PPARγ. In the crystal structure of the human PPARγ, the ligand-binding domain (LBD) in complex with butyrolactone I interacted with the amino acid residues located in the hydrophobic binding pockets of the PPARγ LBD, which is a typical binding mode of the PPARγ partial agonists. Therefore, the adiponectin production-enhancing effect of butyrolactone I was mediated by its polypharmacological dual modulator activities as both a CDK5 inhibitor and a PPARγ partial agonist. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
Transcriptomic Analysis Reveals the Wound Healing Activity of Mussel Myticin C
Biomolecules 2020, 10(1), 133; https://doi.org/10.3390/biom10010133 - 14 Jan 2020
Cited by 3
Abstract
Myticin C is the most studied antimicrobial peptide in the marine mussel Mytilus galloprovincialis. Although it is constitutively expressed in mussel hemocytes and displays antibacterial, antiviral, and chemotactic functions, recent work has suggested that this molecule is mainly activated after tissue injury. [...] Read more.
Myticin C is the most studied antimicrobial peptide in the marine mussel Mytilus galloprovincialis. Although it is constitutively expressed in mussel hemocytes and displays antibacterial, antiviral, and chemotactic functions, recent work has suggested that this molecule is mainly activated after tissue injury. Therefore, the main objective of this work was to characterize the hemocytes’ transcriptomic response after a myticin C treatment, in order to understand the molecular changes induced by this cytokine-like molecule. The transcriptome analysis revealed the modulation of genes related to cellular movement, such as myosin, transgelin, and calponin-like proteins, in agreement with results of functional assays, where an implication of myticin C in the in vitro activation of hemocytes and migration was evidenced. This was also observed in vivo after a tissue injury, when hemocytes, with high concentrations of myticin C, migrated to the damaged area to heal the wound. All these properties allowed us to think about the biotechnological application of these molecules as wound healers. Human keratinocytes and larvae zebrafish models were used to confirm this hypothesis. Accelerated regeneration after a wound or tail fin amputation was observed after treatment with the myticin C peptide, supporting the chemotactic and healing activity of myticin C. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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Open AccessArticle
Cytotoxic Psammaplysin Analogues from the Verongid Red Sea Sponge Aplysinella Species
Biomolecules 2019, 9(12), 841; https://doi.org/10.3390/biom9120841 - 08 Dec 2019
Cited by 1
Abstract
As part of our ongoing interest to identify bioactive chemical entities from marine invertebrates, the Red Sea specimen of the Verongid sponge Aplysinella species was studied. Repeated chromatographic fractionation of the methanolic extract of the sponge and HPLC purification of the cytotoxic fractions [...] Read more.
As part of our ongoing interest to identify bioactive chemical entities from marine invertebrates, the Red Sea specimen of the Verongid sponge Aplysinella species was studied. Repeated chromatographic fractionation of the methanolic extract of the sponge and HPLC purification of the cytotoxic fractions led to the isolation and the identification of two new compounds, psammaplysin Z and 19-hydroxypsammaplysin Z (1 and 2), together with the previously reported psammaplysins A (3) and E (4). The structural determination of 14 was supported by interpretation of their NMR and high-resolution mass spectra. Psammaplysins A and E displayed cytotoxic activity against MBA-MB-231 and HeLa cell lines with IC50 values down to 0.29 µM. On the other hand, psammaplysin Z and 19-hydroxypsammaplysin Z were moderately cytotoxic, indicating the importance of the terminal amine and 2-(methylene)cyclopent-4-ene-1,3-dione moieties in 3 and 4 for potent cytotoxic activity. Full article
(This article belongs to the Special Issue Marine-Derived Biomolecules)
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