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Special Issue "Progress on Marine Natural Products as Lead Compounds"

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

Deadline for manuscript submissions: 31 July 2018

Special Issue Editors

Guest Editor
Prof. Dr. Ana Lourenço

LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal
Website | E-Mail
Interests: phytochemistry; marine metabolites; bioactive metabolites; organic chemistry
Guest Editor
Dr. Patrícia Máximo

LAQV, REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal
Website | E-Mail
Interests: phytochemistry; marine metabolites; structure identification; organic chemistry

Special Issue Information

Dear Colleagues,

The development of therapeutic lead molecules encompasses many steps in different scientific areas. All converge to make headway to more efficient and available compounds. This Special Issue intends to cover progresses in molecular structures of different scaffolds that include the discovery of new compounds, the production by marine microorganisms cultures of compounds traditionally known from other sources, the knowledge of chemical diversity and bioactivity, together with synthetic approaches to produce active compounds from inactive ones, the study of the beneficial effects of compounds present in crude-drugs focused in preclinical and clinical studies, and the exploration of marine natural products by computational methodologies.

Prof. Dr. Ana Lourenço
Dr. Patrícia Máximo
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

  • natural products
  • natural products analogs
  • biological activity
  • microbial production
  • marine Crude-drugs
  • preclinical and clinical studies
  • computer aided drug-discovery

Published Papers (4 papers)

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Research

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Open AccessFeature PaperArticle Chloro-Furanocembranolides from Leptogorgia sp. Improve Pancreatic Beta-Cell Proliferation
Mar. Drugs 2018, 16(2), 49; https://doi.org/10.3390/md16020049
Received: 20 December 2017 / Revised: 19 January 2018 / Accepted: 29 January 2018 / Published: 2 February 2018
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Abstract
Two new chloro-furanocembranolides (1, 2) and two new 1,4-diketo cembranolides (3, 4) were isolated from the crude extract of Leptogorgia sp. together with a new seco-furanocembranolide (5) and the known Z-deoxypukalide (6
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Two new chloro-furanocembranolides (1, 2) and two new 1,4-diketo cembranolides (3, 4) were isolated from the crude extract of Leptogorgia sp. together with a new seco-furanocembranolide (5) and the known Z-deoxypukalide (6), rubifolide (7), scabrolide D (8) and epoxylophodione (9). Their structures were determined based on spectroscopic evidence. Four compounds: 1, 2, 7 and 8 were found to activate the proliferation of pancreatic insulin-producing (beta) cells. Full article
(This article belongs to the Special Issue Progress on Marine Natural Products as Lead Compounds)
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Open AccessArticle Antimicrobial and Anti-Proliferative Effects of Skin Mucus Derived from Dasyatis pastinaca (Linnaeus, 1758)
Mar. Drugs 2017, 15(11), 342; https://doi.org/10.3390/md15110342
Received: 31 July 2017 / Revised: 9 October 2017 / Accepted: 25 October 2017 / Published: 1 November 2017
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Abstract
Resistance to chemotherapy occurs in various diseases (i.e., cancer and infection), and for this reason, both are very difficult to treat. Therefore, novel antimicrobial and chemotherapic drugs are needed for effective antibiotic therapy. The aim of the present study was to assess the
[...] Read more.
Resistance to chemotherapy occurs in various diseases (i.e., cancer and infection), and for this reason, both are very difficult to treat. Therefore, novel antimicrobial and chemotherapic drugs are needed for effective antibiotic therapy. The aim of the present study was to assess the antimicrobial and anti-proliferative effects of skin mucus derived from Dasyatis pastinaca (Linnaeus, 1758). Our results showed that skin mucus exhibited a significant and specific antibacterial activity against Gram-negative bacteria but not against Gram-positive bacteria. Furthermore, we also observed a significant antifungal activity against some strains of Candida spp. Concerning anti-proliferative activity, we showed that fish mucus was specifically toxic for acute leukemia cells (HL60) with an inhibition of proliferation in a dose dependent manner (about 52% at 1000 μg/mL of fish skin mucous, FSM). Moreover, we did not observe effects in healthy cells, in neuroblastoma cells (SH-SY5Y), and multiple myeloma cell lines (MM1, U266). Finally, it exhibited strong expression and activity of chitinase which may be responsible, at least in part, for the aforementioned results. Full article
(This article belongs to the Special Issue Progress on Marine Natural Products as Lead Compounds)
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Open AccessArticle Marine-Derived 2-Aminoimidazolone Alkaloids. Leucettamine B-Related Polyandrocarpamines Inhibit Mammalian and Protozoan DYRK & CLK Kinases
Mar. Drugs 2017, 15(10), 316; https://doi.org/10.3390/md15100316
Received: 30 August 2017 / Revised: 28 September 2017 / Accepted: 12 October 2017 / Published: 17 October 2017
Cited by 1 | PDF Full-text (1869 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and Clathrina. The phylogeny of these sponges and the wide scope of 2-aminoimidazolone alkaloids they produce are reviewed in this article. The origin
[...] Read more.
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and Clathrina. The phylogeny of these sponges and the wide scope of 2-aminoimidazolone alkaloids they produce are reviewed in this article. The origin (invertebrate cells, associated microorganisms, or filtered plankton), physiological functions, and natural molecular targets of these alkaloids are largely unknown. Following the identification of leucettamine B as an inhibitor of selected protein kinases, we synthesized a family of analogues, collectively named leucettines, as potent inhibitors of DYRKs (dual-specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases) and potential pharmacological leads for the treatment of several diseases, including Alzheimer’s disease and Down syndrome. We assembled a small library of marine sponge- and ascidian-derived 2-aminoimidazolone alkaloids, along with several synthetic analogues, and tested them on a panel of mammalian and protozoan kinases. Polyandrocarpamines A and B were found to be potent and selective inhibitors of DYRKs and CLKs. They inhibited cyclin D1 phosphorylation on a DYRK1A phosphosite in cultured cells. 2-Aminoimidazolones thus represent a promising chemical scaffold for the design of potential therapeutic drug candidates acting as specific inhibitors of disease-relevant kinases, and possibly other disease-relevant targets. Full article
(This article belongs to the Special Issue Progress on Marine Natural Products as Lead Compounds)
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Review

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Open AccessFeature PaperReview Computational Methodologies in the Exploration of Marine Natural Product Leads
Mar. Drugs 2018, 16(7), 236; https://doi.org/10.3390/md16070236
Received: 14 June 2018 / Revised: 2 July 2018 / Accepted: 6 July 2018 / Published: 13 July 2018
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Abstract
Computational methodologies are assisting the exploration of marine natural products (MNPs) to make the discovery of new leads more efficient, to repurpose known MNPs, to target new metabolites on the basis of genome analysis, to reveal mechanisms of action, and to optimize leads.
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Computational methodologies are assisting the exploration of marine natural products (MNPs) to make the discovery of new leads more efficient, to repurpose known MNPs, to target new metabolites on the basis of genome analysis, to reveal mechanisms of action, and to optimize leads. In silico efforts in drug discovery of NPs have mainly focused on two tasks: dereplication and prediction of bioactivities. The exploration of new chemical spaces and the application of predicted spectral data must be included in new approaches to select species, extracts, and growth conditions with maximum probabilities of medicinal chemistry novelty. In this review, the most relevant current computational dereplication methodologies are highlighted. Structure-based (SB) and ligand-based (LB) chemoinformatics approaches have become essential tools for the virtual screening of NPs either in small datasets of isolated compounds or in large-scale databases. The most common LB techniques include Quantitative Structure–Activity Relationships (QSAR), estimation of drug likeness, prediction of adsorption, distribution, metabolism, excretion, and toxicity (ADMET) properties, similarity searching, and pharmacophore identification. Analogously, molecular dynamics, docking and binding cavity analysis have been used in SB approaches. Their significance and achievements are the main focus of this review. Full article
(This article belongs to the Special Issue Progress on Marine Natural Products as Lead Compounds)
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