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Special Issue "Marine Natural Product Discovery: Innovative Strategies and Future Trends"

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

Deadline for manuscript submissions: closed (31 January 2017)

Special Issue Editor

Guest Editor
Dr. Sylvia Urban

School of Applied Sciences (Applied Chemistry), RMIT University (City Campus), GPO Box 2476V, Melbourne 3001, Victoria, Australia
Website1 | Website2 | Website3 | E-Mail
Phone: +61 3 9925 3376
Fax: +61 3 9925 3747
Interests: marine and terrestrial natural products chemistry; isolation and structural characterization; NMR spectroscopy; analytical separation methodologies

Special Issue Information

Dear Colleagues,

In the pursuit of new bioactive natural products, the demand to rapidly identify compounds present, in ever decreasing amounts, in complex crude extracts, has become a limiting factor. You are invited to contribute to this Special Issue, the focus of which is the implementation, development and future trends arising from the use of innovative strategies to discover new bioactive marine natural products.

Dr. Sylvia Urban
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. 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

  • marine natural products
  • chemical profiling
  • dereplication
  • extraction methodologies
  • hyphenated technologies
  • bioactivity
  • bio-discovery

Published Papers (7 papers)

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Research

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Open AccessArticle Bioactive Potential of Marine Macroalgae from the Central Red Sea (Saudi Arabia) Assessed by High-Throughput Imaging-Based Phenotypic Profiling
Mar. Drugs 2017, 15(3), 80; doi:10.3390/md15030080
Received: 3 February 2017 / Revised: 15 March 2017 / Accepted: 16 March 2017 / Published: 20 March 2017
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Abstract
Marine algae represent an important source of novel natural products. While their bioactive potential has been studied to some extent, limited information is available on marine algae from the Red Sea. This study aimed at the broad discovery of new bioactivities from a
[...] Read more.
Marine algae represent an important source of novel natural products. While their bioactive potential has been studied to some extent, limited information is available on marine algae from the Red Sea. This study aimed at the broad discovery of new bioactivities from a collection of twelve macroalgal species from the Central Red Sea. We used imaging-based High-Content Screening (HCS) with a diverse spectrum of cellular markers for detailed cytological profiling of fractionated algal extracts. The cytological profiles for 3 out of 60 algal fractions clustered closely to reference inhibitors and showed strong inhibitory activities on the HIV-1 reverse transcriptase in a single-enzyme biochemical assay, validating the suggested biological target. Subsequent chemical profiling of the active fractions of two brown algal species by ultra-high resolution mass spectrometry (FT-ICR-MS) revealed possible candidate molecules. A database query of these molecules led us to groups of compounds with structural similarities, which are suggested to be responsible for the observed activity. Our work demonstrates the versatility and power of cytological profiling for the bioprospecting of unknown biological resources and highlights Red Sea algae as a source of bioactives that may serve as a starting point for further studies. Full article
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Open AccessArticle Sterols from Thai Marine Sponge Petrosia (Strongylophora) sp. and Their Cytotoxicity
Mar. Drugs 2017, 15(3), 54; doi:10.3390/md15030054
Received: 20 January 2017 / Revised: 16 February 2017 / Accepted: 17 February 2017 / Published: 23 February 2017
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Abstract
Eight new sterols (15 and 1113), together with eight known compounds (610 and 1416) were isolated from marine sponge Petrosia sp. The structures of these compounds were elucidated on the basis
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Eight new sterols (15 and 1113), together with eight known compounds (610 and 1416) were isolated from marine sponge Petrosia sp. The structures of these compounds were elucidated on the basis of extensive spectroscopic analysis. The cytotoxicity of some compounds against a panel of human cancer cell lines is also reported. Full article
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Open AccessArticle Time Course Exo-Metabolomic Profiling in the Green Marine Macroalga Ulva (Chlorophyta) for Identification of Growth Phase-Dependent Biomarkers
Mar. Drugs 2017, 15(1), 14; doi:10.3390/md15010014
Received: 28 August 2016 / Revised: 23 December 2016 / Accepted: 3 January 2017 / Published: 10 January 2017
Cited by 1 | PDF Full-text (5393 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The marine green macroalga Ulva (Chlorophyta) lives in a mutualistic symbiosis with bacteria that influence growth, development, and morphogenesis. We surveyed changes in Ulva’s chemosphere, which was defined as a space where organisms interact with each other via compounds, such as infochemicals,
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The marine green macroalga Ulva (Chlorophyta) lives in a mutualistic symbiosis with bacteria that influence growth, development, and morphogenesis. We surveyed changes in Ulva’s chemosphere, which was defined as a space where organisms interact with each other via compounds, such as infochemicals, nutrients, morphogens, and defense compounds. Thereby, Ulva mutabilis cooperates with bacteria, in particular, Roseovarius sp. strain MS2 and Maribacter sp. strain MS6 (formerly identified as Roseobacter sp. strain MS2 and Cytophaga sp. strain MS6). Without this accompanying microbial flora, U. mutabilis forms only callus-like colonies. However, upon addition of the two bacteria species, in effect forming a tripartite community, morphogenesis can be completely restored. Under this strictly standardized condition, bioactive and eco-physiologically-relevant marine natural products can be discovered. Solid phase extracted waterborne metabolites were analyzed using a metabolomics platform, facilitating gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-mass spectrometry (LC-MS) analysis, combined with the necessary acquisition of biological metadata. Multivariate statistics of the GC-MS and LC-MS data revealed strong differences between Ulva’s growth phases, as well as between the axenic Ulva cultures and the tripartite community. Waterborne biomarkers, including glycerol, were identified as potential indicators for algal carbon source and bacterial-algal interactions. Furthermore, it was demonstrated that U. mutabilis releases glycerol that can be utilized for growth by Roseovarius sp. MS2. Full article
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Open AccessArticle The Potential Exploitation of the Mediterranean Invasive Alga Caulerpa cylindracea: Can the Invasion Be Transformed into a Gain?
Mar. Drugs 2016, 14(11), 210; doi:10.3390/md14110210
Received: 29 July 2016 / Revised: 8 November 2016 / Accepted: 9 November 2016 / Published: 15 November 2016
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Abstract
Recently, there is a growing interest towards the development of strategies for invasive seaweed control and exploitation as source of secondary metabolites. Here, we investigated the potential of exploitation in biotechnology and recycling options in eradication programs of the lipidic extract of the
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Recently, there is a growing interest towards the development of strategies for invasive seaweed control and exploitation as source of secondary metabolites. Here, we investigated the potential of exploitation in biotechnology and recycling options in eradication programs of the lipidic extract of the Mediterranean invasive seaweed Caulerpa cylindracea (Chlorophyta). The chemical characterization was carried out by means of multinuclear and multidimensional NMR spectroscopy. The fatty acid profile of C. cylindracea assessed the presence of several types of molecules known for antioxidant activity such as carotenoids, chlorophylls, pheophytins, and sterols. The NMR spectroscopy showed also the characteristic signals of saturated, unsaturated, and free fatty acids as well as other metabolites including the biopolymer polyhydroxybutyrate. The lipidic extract exerted an antioxidant activity corresponding to 552.14 ± 69.13 mmol Trolox equivalent/g (ORAC) and to 70.3 ± 2.67 mmol Trolox equivalent/g (TEAC). The extract showed an antibacterial activity against several Vibrio species, suggesting its potential use in the control of diseases in mariculture. Our results show that C. cylindracea, representing a critical hazard in coastal areas, could be transformed into a gain supporting specific management actions to reduce the effects of human pressures. Full article
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Open AccessArticle Dichotocejpins A–C: New Diketopiperazines from a Deep-Sea-Derived Fungus Dichotomomyces cejpii FS110
Mar. Drugs 2016, 14(9), 164; doi:10.3390/md14090164
Received: 3 August 2016 / Revised: 2 September 2016 / Accepted: 5 September 2016 / Published: 9 September 2016
Cited by 3 | PDF Full-text (1596 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Three new diketopiperazines, dichotocejpins A–C (13), together with eight known analogues (411), were isolated from the culture of the deep-sea sediment derived fungus Dichotomomyces cejpii FS110. Their structures, including absolute configurations, were elucidated by a
[...] Read more.
Three new diketopiperazines, dichotocejpins A–C (13), together with eight known analogues (411), were isolated from the culture of the deep-sea sediment derived fungus Dichotomomyces cejpii FS110. Their structures, including absolute configurations, were elucidated by a combination of HRESIMS, NMR, X-ray crystallography, and ECD calculations. Compounds 46, 1011 showed significant cytotoxic activities against MCF-7, NCI-H460, HepG-2, and SF-268 tumor cell lines. Compound 1 exhibited excellent inhibitory activity against α-glucosidase with an IC50 of 138 μM. Full article
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Review

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Open AccessReview From Marine Venoms to Drugs: Efficiently Supported by a Combination of Transcriptomics and Proteomics
Mar. Drugs 2017, 15(4), 103; doi:10.3390/md15040103
Received: 1 February 2017 / Revised: 20 March 2017 / Accepted: 29 March 2017 / Published: 30 March 2017
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Abstract
The potential of marine natural products to become new drugs is vast; however, research is still in its infancy. The chemical and biological diversity of marine toxins is immeasurable and as such an extraordinary resource for the discovery of new drugs. With the
[...] Read more.
The potential of marine natural products to become new drugs is vast; however, research is still in its infancy. The chemical and biological diversity of marine toxins is immeasurable and as such an extraordinary resource for the discovery of new drugs. With the rapid development of next-generation sequencing (NGS) and liquid chromatography–tandem mass spectrometry (LC-MS/MS), it has been much easier and faster to identify more toxins and predict their functions with bioinformatics pipelines, which pave the way for novel drug developments. Here we provide an overview of related bioinformatics pipelines that have been supported by a combination of transcriptomics and proteomics for identification and function prediction of novel marine toxins. Full article
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Open AccessReview Quorum Sensing Inhibitors from the Sea Discovered Using Bacterial N-acyl-homoserine Lactone-Based Biosensors
Mar. Drugs 2017, 15(3), 53; doi:10.3390/md15030053
Received: 27 January 2017 / Revised: 15 February 2017 / Accepted: 16 February 2017 / Published: 23 February 2017
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Abstract
Marine natural products with antibiotic activity have been a rich source of drug discovery; however, the emergence of antibiotic-resistant bacterial strains has turned attention towards the discovery of alternative innovative strategies to combat pathogens. In many pathogenic bacteria, the expression of virulence factors
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Marine natural products with antibiotic activity have been a rich source of drug discovery; however, the emergence of antibiotic-resistant bacterial strains has turned attention towards the discovery of alternative innovative strategies to combat pathogens. In many pathogenic bacteria, the expression of virulence factors is under the regulation of quorum sensing (QS). QS inhibitors (QSIs) present a promising alternative or potential synergistic treatment since they disrupt the signaling pathway used for intra- and interspecies coordination of expression of virulence factors. This review covers the set of molecules showing QSI activity that were isolated from marine organisms, including plants (algae), animals (sponges, cnidarians, and bryozoans), and microorganisms (bacteria, fungi, and cyanobacteria). The compounds found and the methods used for their isolation are the emphasis of this review. Full article
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