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Special Issue "Target Identification of Marine Products"

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

Deadline for manuscript submissions: closed (30 September 2017)

Special Issue Editors

Guest Editor
Prof. Raffaele Riccio

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, Fisciano, Italy
Website | E-Mail
Interests: bioactive natural products as lead compounds for drug discovery; stereochemical characterization of organic molecules by NMR and computational approaches; molecular mechanism of action of bioactive natural products and ligand-receptor interactions; target identification of bioactive natural products by chemical proteomics and computational approaches
Guest Editor
Prof. Maria Chiara Monti

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, Fisciano, Italy
Website | E-Mail
Interests: targets and off-targets identification of bioactive natural products by chemical proteomics; characterization of protein-ligand complexes by orthogonal biophysical appraoches; structural analysis of proteins and small molecules by mass spectrometry

Special Issue Information

Dear Colleagues,

Marine natural products hold an exceptional chemical diversity representing a vast library of novel scaffolds with broad pharmacological properties useful in the drug discovery process. Indeed, over time, they have evolved to obtain optimum interaction with their receptors to better achieve their biological effects. Although their therapeutic potential is usually evaluated in high-throughput assays and sometimes in preclinical and clinical trials, very often their intracellular and extracellular targets and interaction profile remain unknown. Since the research of new marine bio-inspired drugs is presently moving toward a rationalization in which chemistry and biology are joined into a targeted approach, as Guest Editors, we would like to call scientists to report their results in the field of target identification of bioactive marine natural products.

Prof. Raffaele Riccio
Prof. Maria Chiara Monti
Guest Editors

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. 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 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

  • bioactive marine natural products
  • marine drugs
  • target identification
  • target discovery
  • chemical proteomics

Published Papers (5 papers)

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Research

Open AccessArticle Discovering the Biological Target of 5-epi-Sinuleptolide Using a Combination of Proteomic Approaches
Mar. Drugs 2017, 15(10), 312; doi:10.3390/md15100312
Received: 28 July 2017 / Revised: 29 September 2017 / Accepted: 9 October 2017 / Published: 13 October 2017
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Abstract
Sinuleptolide and its congeners are diterpenes with a norcembranoid skeleton isolated from the soft coral genus Sinularia. These marine metabolites are endowed with relevant biological activities, mainly associated with cancer development. 5-epi-sinuleptolide has been selected as a candidate for target
[...] Read more.
Sinuleptolide and its congeners are diterpenes with a norcembranoid skeleton isolated from the soft coral genus Sinularia. These marine metabolites are endowed with relevant biological activities, mainly associated with cancer development. 5-epi-sinuleptolide has been selected as a candidate for target discovery studies through the application of complementary proteomic approaches. Specifically, a combination of conventional chemical proteomics based on affinity chromatography, coupled with high-resolution mass spectrometry and bioinformatics, as well as drug affinity responsive target stability (DARTS), led to a clear identification of actins as main targets for 5-epi-sinuleptolide. Subsequent in-cell assays, performed with cytochalasin D as reference compound, gave information on the ability of 5-epi-sinuleptolide to disrupt the actin cytoskeleton by loss of actin fibers and formation of F-actin amorphous aggregates. These results suggest the potential application of 5-epi-sinuleptolide as a useful tool in the study of the molecular processes impaired in several disorders in which actin is thought to play an essential role. Full article
(This article belongs to the Special Issue Target Identification of Marine Products)
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Open AccessArticle Quantification of Representative Ciguatoxins in the Pacific Using Quantitative Nuclear Magnetic Resonance Spectroscopy
Mar. Drugs 2017, 15(10), 309; doi:10.3390/md15100309
Received: 8 September 2017 / Revised: 29 September 2017 / Accepted: 9 October 2017 / Published: 12 October 2017
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Abstract
The absolute quantification of five toxins involved in ciguatera fish poisoning (CFP) in the Pacific was carried out by quantitative 1H-NMR. The targeted toxins were ciguatoxin-1B (CTX1B), 52-epi-54-deoxyciguatoxin-1B (epideoxyCTX1B), ciguatoxin-3C (CTX3C), 51-hydroxyciguatoxin-3C (51OHCTX3C), and ciguatoxin-4A (CTX4A). We first calibrated the residual protons
[...] Read more.
The absolute quantification of five toxins involved in ciguatera fish poisoning (CFP) in the Pacific was carried out by quantitative 1H-NMR. The targeted toxins were ciguatoxin-1B (CTX1B), 52-epi-54-deoxyciguatoxin-1B (epideoxyCTX1B), ciguatoxin-3C (CTX3C), 51-hydroxyciguatoxin-3C (51OHCTX3C), and ciguatoxin-4A (CTX4A). We first calibrated the residual protons of pyridine-d5 using certified reference material, 1,4-BTMSB-d4, prepared the toxin solutions with the calibrated pyridin-d5, measured the 1H-NMR spectra, and quantified the toxin using the calibrated residual protons as the internal standard. The absolute quantification was carried out by comparing the signal intensities between the selected protons of the target toxin and the residual protons of the calibrated pyridine-d5. The proton signals residing on the ciguatoxins (CTXs) to be used for quantification were carefully selected for those that were well separated from adjacent signals including impurities and that exhibited an effective intensity. To quantify CTX1B and its congeners, the olefin protons in the side chain were judged appropriate for use. The quantification was achievable with nano-molar solutions. The probable errors for uncertainty, calculated on respective toxins, ranged between 3% and 16%. The contamination of the precious toxins with nonvolatile internal standards was thus avoided. After the evaporation of pyridine-d5, the calibrated CTXs were ready for use as the reference standard in the quantitative analysis of ciguatoxins by LC/MS. Full article
(This article belongs to the Special Issue Target Identification of Marine Products)
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Open AccessArticle Chemical Synthesis of Marine-Derived Sulfoglycolipids, a New Class of Molecular Adjuvants
Mar. Drugs 2017, 15(9), 288; doi:10.3390/md15090288
Received: 27 July 2017 / Revised: 29 August 2017 / Accepted: 11 September 2017 / Published: 20 September 2017
PDF Full-text (1511 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Vaccines play a primary role in the protection of human health by preventing infectious and chronic diseases. Recently we have reported 1,2-O-distearoyl-3-O-β-d-sulfoquinovosylglycerol (β-SQDG18), here named Sulfavant A (1), which shows promising properties as a new
[...] Read more.
Vaccines play a primary role in the protection of human health by preventing infectious and chronic diseases. Recently we have reported 1,2-O-distearoyl-3-O-β-d-sulfoquinovosylglycerol (β-SQDG18), here named Sulfavant A (1), which shows promising properties as a new molecular adjuvant in in vitro and in vivo tests. In the present manuscript, we provide full details about a synthetic strategy for the preparation of 1, including a discussion of chemical determinants of the activity and the major technical hurdles we faced during the study. Synthesis of Sulfavant A (1) is achieved by a versatile procedure based on a trichloroacetimidate methodology and peracetate sugar precursors. The final design opens possibilities for the preparation of a series of interesting analogs for further pharmacological optimization and development, including derivatives containing different saturated and polyunsaturated fatty acids (e.g., 17 and 22). Full article
(This article belongs to the Special Issue Target Identification of Marine Products)
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Open AccessArticle Myticalins: A Novel Multigenic Family of Linear, Cationic Antimicrobial Peptides from Marine Mussels (Mytilus spp.)
Mar. Drugs 2017, 15(8), 261; doi:10.3390/md15080261
Received: 27 July 2017 / Revised: 11 August 2017 / Accepted: 18 August 2017 / Published: 22 August 2017
PDF Full-text (7630 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The application of high-throughput sequencing technologies to non-model organisms has brought new opportunities for the identification of bioactive peptides from genomes and transcriptomes. From this point of view, marine invertebrates represent a potentially rich, yet largely unexplored resource for de novo discovery due
[...] Read more.
The application of high-throughput sequencing technologies to non-model organisms has brought new opportunities for the identification of bioactive peptides from genomes and transcriptomes. From this point of view, marine invertebrates represent a potentially rich, yet largely unexplored resource for de novo discovery due to their adaptation to diverse challenging habitats. Bioinformatics analyses of available genomic and transcriptomic data allowed us to identify myticalins, a novel family of antimicrobial peptides (AMPs) from the mussel Mytilus galloprovincialis, and a similar family of AMPs from Modiolus spp., named modiocalins. Their coding sequence encompasses two conserved N-terminal (signal peptide) and C-terminal (propeptide) regions and a hypervariable central cationic region corresponding to the mature peptide. Myticalins are taxonomically restricted to Mytiloida and they can be classified into four subfamilies. These AMPs are subject to considerable interindividual sequence variability and possibly to presence/absence variation. Functional assays performed on selected members of this family indicate a remarkable tissue-specific expression (in gills) and broad spectrum of activity against both Gram-positive and Gram-negative bacteria. Overall, we present the first linear AMPs ever described in marine mussels and confirm the great potential of bioinformatics tools for the de novo discovery of bioactive peptides in non-model organisms. Full article
(This article belongs to the Special Issue Target Identification of Marine Products)
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Open AccessArticle Anti-Coagulant and Anti-Thrombotic Properties of Blacklip Abalone (Haliotis rubra): In Vitro and Animal Studies
Mar. Drugs 2017, 15(8), 240; doi:10.3390/md15080240
Received: 14 June 2017 / Revised: 24 July 2017 / Accepted: 27 July 2017 / Published: 4 August 2017
PDF Full-text (616 KB) | HTML Full-text | XML Full-text
Abstract
Sulphated polysaccharides with anti-thrombotic and anti-coagulant activities have been found in various marine biota. In this study, a previously characterised anti-thrombotic and anti-coagulant extract from blacklip abalone was fractionated by anion exchange chromatography (AEC), pooled (on a sulphated polysaccharide basis) and administered to
[...] Read more.
Sulphated polysaccharides with anti-thrombotic and anti-coagulant activities have been found in various marine biota. In this study, a previously characterised anti-thrombotic and anti-coagulant extract from blacklip abalone was fractionated by anion exchange chromatography (AEC), pooled (on a sulphated polysaccharide basis) and administered to Wistar rats via oral gavage (N = 8) for assessment as an oral therapeutic. To ensure that the preparation had anti-coagulant activity prior to oral administration, it was assessed in rat blood by thromboelastography (TEG) significantly increasing reaction (R) time (or time until clot formation). Following in vitro confirmation of anti-coagulant activity, 40 mg of the preparation was orally administered to rats with blood samples collected at 2, 4, and 6 h post-gavage. Assessment of all blood samples by TEG showed some prolongation of R time from 355 to 380 s after 4 h. Dosing of the post-gavage blood samples with the abalone preparation to confirm anti-thrombotic activity in vitro revealed residual anti-coagulant activity, further suggesting that oral administration did increase anti-coagulant potential in the collected blood but that bioavailability was low. Assessment of tissues and haematological parameters showed no obvious harmful effects of the abalone preparation in animals. In summary, even though oral administration of fractionated and pooled blacklip abalone extract to rats delayed clotting after 4 h, bioavailability of the preparation appeared to be low and may be more appropriate for intravenous administration as an anti-thrombotic or anti-coagulant therapeutic. Full article
(This article belongs to the Special Issue Target Identification of Marine Products)
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