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Marine Drugs
Special Issues
Marine Small-Molecule Bioactive Agents and Therapeutic Targets
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Marine Small-Molecule Bioactive Agents and Therapeutic Targets

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (31 January 2019) | Viewed by 23616

Special Issue Editor

Dr. Enrique Barrajón-Catalán

E-Mail Website
Guest Editor
Institute of Research, Development and Innovation in Healthcare Biotechnology of Elche (IDiBE), Miguel Hernández University (UMH), Alicante, Spain
Interests: natural compounds; polyphenols; marine compounds; cancer; antimicrobial; skin; cosmetics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues:

Nowadays, at least one-third of the current top-twenty drugs on the market are derived from a natural source, and approximately 50% of the marketed drugs are classified as naturally-derived or are designed on the basis of natural compounds. Marine biodiversity is huge and is correlated with a wide chemical diversity in their compounds, most of them still unknown or uncharacterized. In fact, it is estimated that only 18% of marine natural products have been discovered so far compared with products of terrestrial organisms.

Small molecules, such as small peptides, polyphenols and terpenoids, are especially interesting due their particular pharmacological and pharmacokinetic properties. This Special Issue is focused in these small molecules from marine origin with special interest in the following topics:

  • New small molecules with pharmacological activity and their molecular targets.
  • Anticancer, antimicrobial and antinflammatory small marine molecules.Use of small marine compounds in other diseases.
  • Use in cosmetic, cosmoceutic and nutraceutic products.
  • Purification, chemical characterization  and structural elucidation.
  • In silico virtual screenings and HTS studies.
  • Pharmakokinetics and bioavailability studies.
  • Preclinical and clinical trials.

The aim of this Special Issue is to collect literature that reflect the actual state-of-the-art and increase our knowledge about marine small molecules and their biological activities.

As Guest Editor of this Special Issue, I cordially invite researchers from all around the world to contribute to this Special Issue by submitting original research articles, long and mini review papers, short notes, and opinions according to their expertise.

Prof. Enrique Barrajón-Catalán
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 submissions that pass pre-check are 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. Marine Drugs 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 2900 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 product
  • small molecule
  • polyphenol
  • peptide
  • cancer
  • antimicrobial
  • antiinflammatory

Published Papers (5 papers)

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Research

20 pages, 2832 KiB  
Article
Antiviral Activity of a Turbot (Scophthalmus maximus) NK-Lysin Peptide by Inhibition of Low-pH Virus-Induced Membrane Fusion
by Alberto Falco, Regla María Medina-Gali, José Antonio Poveda, Melissa Bello-Perez, Beatriz Novoa and José Antonio Encinar
Mar. Drugs 2019, 17(2), 87; https://0-doi-org.brum.beds.ac.uk/10.3390/md17020087 - 01 Feb 2019
Cited by 28 | Viewed by 3499
Abstract
Global health is under attack by increasingly-frequent pandemics of viral origin. Antimicrobial peptides are a valuable tool to combat pathogenic microorganisms. Previous studies from our group have shown that the membrane-lytic region of turbot (Scophthalmus maximus) NK-lysine short peptide (Nkl71–100 [...] Read more.
Global health is under attack by increasingly-frequent pandemics of viral origin. Antimicrobial peptides are a valuable tool to combat pathogenic microorganisms. Previous studies from our group have shown that the membrane-lytic region of turbot (Scophthalmus maximus) NK-lysine short peptide (Nkl71–100) exerts an anti-protozoal activity, probably due to membrane rupture. In addition, NK-lysine protein is highly expressed in zebrafish in response to viral infections. In this work several biophysical methods, such as vesicle aggregation, leakage and fluorescence anisotropy, are employed to investigate the interaction of Nkl71–100 with different glycerophospholipid vesicles. At acidic pH, Nkl71–100 preferably interacts with phosphatidylserine (PS), disrupts PS membranes, and allows the content leakage from vesicles. Furthermore, Nkl71–100 exerts strong antiviral activity against spring viremia of carp virus (SVCV) by inhibiting not only the binding of viral particles to host cells, but also the fusion of virus and cell membranes, which requires a low pH context. Such antiviral activity seems to be related to the important role that PS plays in these steps of the replication cycle of SVCV, a feature that is shared by other families of virus-comprising members with health and veterinary relevance. Consequently, Nkl71–100 is shown as a promising broad-spectrum antiviral candidate. Full article
(This article belongs to the Special Issue Marine Small-Molecule Bioactive Agents and Therapeutic Targets)
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11 pages, 713 KiB  
Article
Ishophloroglucin A, a Novel Phlorotannin for Standardizing the Anti-α-Glucosidase Activity of Ishige okamurae
by BoMi Ryu, Yunfei Jiang, Hyun-Soo Kim, Jee-Min Hyun, Sang-Bin Lim, Yong Li and You-Jin Jeon
Mar. Drugs 2018, 16(11), 436; https://0-doi-org.brum.beds.ac.uk/10.3390/md16110436 - 08 Nov 2018
Cited by 31 | Viewed by 4019
Abstract
Nutraceutical use of algae requires understanding of the diversity and significance of their active compositions for intended activities. Ishige okamurae (I. okamurae) extract is well-known to possess α-glucosidase inhibitory activity; however, studies are needed to investigate its active composition in order [...] Read more.
Nutraceutical use of algae requires understanding of the diversity and significance of their active compositions for intended activities. Ishige okamurae (I. okamurae) extract is well-known to possess α-glucosidase inhibitory activity; however, studies are needed to investigate its active composition in order to standardize its α-glucosidase inhibitory activity. In this study, we observed the intensity of the dominant compounds of each I. okamurae extract harvested between 2016 and 2017, and the different potency of each I. okamurae extract against α-glucosidase. By comparing the anti-α-glucosidase ability of the dominant compounds, a novel Ishophloroglucin A with highest α-glucosidase inhibitory activity was identified and suggested for standardization of anti-α-glucosidase activity in I. okamurae extract. Additionally, a validated analytical method for measurement of Ishophloroglucin A for future standardization of I. okamurae extract was established in this study. We suggest using Ishophloroglucin A to standardize anti-α-glucosidase potency of I. okamurae and propose the significance of standardization based on their composition for effective use of algae as marine-derived nutraceuticals. Full article
(This article belongs to the Special Issue Marine Small-Molecule Bioactive Agents and Therapeutic Targets)
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24 pages, 9108 KiB  
Article
New Mammalian Target of Rapamycin (mTOR) Modulators Derived from Natural Product Databases and Marine Extracts by Using Molecular Docking Techniques
by Verónica Ruiz-Torres, Maria Losada-Echeberría, Maria Herranz-López, Enrique Barrajón-Catalán, Vicente Galiano, Vicente Micol and José Antonio Encinar
Mar. Drugs 2018, 16(10), 385; https://0-doi-org.brum.beds.ac.uk/10.3390/md16100385 - 15 Oct 2018
Cited by 22 | Viewed by 6490
Abstract
Mammalian target of rapamycin (mTOR) is a PI3K-related serine/threonine protein kinase that functions as a master regulator of cellular growth and metabolism, in response to nutrient and hormonal stimuli. mTOR functions in two distinct complexes—mTORC1 is sensitive to rapamycin, while, mTORC2 is insensitive [...] Read more.
Mammalian target of rapamycin (mTOR) is a PI3K-related serine/threonine protein kinase that functions as a master regulator of cellular growth and metabolism, in response to nutrient and hormonal stimuli. mTOR functions in two distinct complexes—mTORC1 is sensitive to rapamycin, while, mTORC2 is insensitive to this drug. Deregulation of mTOR’s enzymatic activity has roles in cancer, obesity, and aging. Rapamycin and its chemical derivatives are the only drugs that inhibit the hyperactivity of mTOR, but numerous side effects have been described due to its therapeutic use. The purpose of this study was to identify new compounds of natural origin that can lead to drugs with fewer side effects. We have used computational techniques (molecular docking and calculated ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) parameters) that have enabled the selection of candidate compounds, derived from marine natural products, SuperNatural II, and ZINC natural products, for inhibitors targeting, both, the ATP and the rapamycin binding sites of mTOR. We have shown experimental evidence of the inhibitory activity of eleven selected compounds against mTOR. We have also discovered the inhibitory activity of a new marine extract against this enzyme. The results have been discussed concerning the necessity to identify new molecules for therapeutic use, especially against aging, and with fewer side effects. Full article
(This article belongs to the Special Issue Marine Small-Molecule Bioactive Agents and Therapeutic Targets)
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19 pages, 16325 KiB  
Article
A Structure- and Ligand-Based Virtual Screening of a Database of “Small” Marine Natural Products for the Identification of “Blue” Sigma-2 Receptor Ligands
by Giuseppe Floresta, Emanuele Amata, Carla Barbaraci, Davide Gentile, Rita Turnaturi, Agostino Marrazzo and Antonio Rescifina
Mar. Drugs 2018, 16(10), 384; https://0-doi-org.brum.beds.ac.uk/10.3390/md16100384 - 14 Oct 2018
Cited by 29 | Viewed by 4901
Abstract
Sigma receptors are a fascinating receptor protein class whose ligands are actually under clinical evaluation for the modulation of opioid analgesia and their use as positron emission tomography radiotracers. In particular, peculiar biological and therapeutic functions are associated with the sigma-2 (σ2 [...] Read more.
Sigma receptors are a fascinating receptor protein class whose ligands are actually under clinical evaluation for the modulation of opioid analgesia and their use as positron emission tomography radiotracers. In particular, peculiar biological and therapeutic functions are associated with the sigma-2 (σ2) receptor. The σ2 receptor ligands determine tumor cell death through apoptotic and non-apoptotic pathways, and the overexpression of σ2 receptors in several tumor cell lines has been well documented, with significantly higher levels in proliferating tumor cells compared to quiescent ones. This acknowledged feature has found practical application in the development of cancer cell tracers and for ligand-targeting therapy. In this context, the development of new ligands that target the σ2 receptors is beneficial for those diseases in which this protein is involved. In this paper, we conducted a search of new potential σ2 receptor ligands among a database of 1517 “small” marine natural products constructed by the union of the Seaweed Metabolite and the Chemical Entities of Biological Interest (ChEBI) Databases. The structures were passed through two filters that were constituted by our developed two-dimensional (2D) and three-dimensional Quantitative Structure-Activity Relationship (3D-QSAR) statistical models, and successively docked upon a σ2 receptor homology model that we built according to the FASTA sequence of the σ2/TMEM97 (SGMR2_HUMAN) receptor. Full article
(This article belongs to the Special Issue Marine Small-Molecule Bioactive Agents and Therapeutic Targets)
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14 pages, 1265 KiB  
Article
Eicosanoid Diversity of Stony Corals
by Helike Lõhelaid and Nigulas Samel
Mar. Drugs 2018, 16(1), 10; https://0-doi-org.brum.beds.ac.uk/10.3390/md16010010 - 03 Jan 2018
Cited by 9 | Viewed by 3879
Abstract
Oxylipins are well-established lipid mediators in plants and animals. In mammals, arachidonic acid (AA)-derived eicosanoids control inflammation, fever, blood coagulation, pain perception and labor, and, accordingly, are used as drugs, while lipoxygenases (LOX), as well as cyclooxygenases (COX) serve as therapeutic targets for [...] Read more.
Oxylipins are well-established lipid mediators in plants and animals. In mammals, arachidonic acid (AA)-derived eicosanoids control inflammation, fever, blood coagulation, pain perception and labor, and, accordingly, are used as drugs, while lipoxygenases (LOX), as well as cyclooxygenases (COX) serve as therapeutic targets for drug development. In soft corals, eicosanoids are synthesized on demand from AA by LOX, COX, and catalase-related allene oxide synthase-lipoxygenase (cAOS-LOX) and hydroperoxide lyase-lipoxygenase (cHPL-LOX) fusion proteins. Reef-building stony corals are used as model organisms for the stress-related genomic studies of corals. Yet, the eicosanoid synthesis capability and AA-derived lipid mediator profiles of stony corals have not been determined. In the current study, the genomic and transcriptomic data about stony coral LOXs, AOS-LOXs, and COXs were analyzed and the eicosanoid profiles and AA metabolites of three stony corals, Acropora millepora, A. cervicornis, and Galaxea fascicularis, were determined by reverse-phase high-performance liquid chromatography (RP-HPLC) coupled with MS-MS and a radiometric detector. Our results confirm that the active LOX and AOS-LOX pathways are present in Acropora sp., which correspond to the genomic/sequence data reported earlier. In addition, LOX, AOS-LOX, and COX products were detected in the closely related species G. fascicularis. In conclusion, the functional 8R-LOX and/or AOS-LOX pathways are abundant among corals, while COXs are restricted to certain soft and stony coral lineages. Full article
(This article belongs to the Special Issue Marine Small-Molecule Bioactive Agents and Therapeutic Targets)
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