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Special Issue "Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery"

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

Deadline for manuscript submissions: 20 June 2019

Special Issue Editor

Guest Editor
Dr. Rob Keyzers

1. School of Chemical & Physical Sciences, and Center For Biodiscovery, Victoria University of Wellington, Wellington 6012, New Zealand
2. Maurice Wilkins Centre for Molecular Biodiscovery, Auckland, New Zealand
Website 1 | Website 2 | E-Mail
Phone: +64 4 4635117
Interests: Identification of novel; biologically active marine natural products; metabolomics of marine organisms; chemical ecology; spectroscopic identification of complex molecules

Special Issue Information

Dear Colleagues,

From the potential human harm caused by the exquisitely potent dinoflagellate cytotoxins, maitotoxin and brevetoxin, through the knowledge gained regarding cellular function and metabolism from the use of latrunculin and laulimalide, right through to new blockbuster anticancer drugs like Eribulin mesylate and Trabectedin, the bioassay-guided isolation of new marine natural products has informed science and helped save many lives over the past half century. The new and exciting molecules sourced from the marine environment are varied in structure and, most importantly, the wide ranging and diverse potent bioactivities they possess. With a significantly greater number of phyla represented in our marine environments than that found on land, the sheer biodiversity found in the oceans, coupled with difficulties, and hence opportunities for obtaining marine organisms, continue to make investigations of marine natural products a lucrative area for medicinal and biochemical research.

Given the great value still waiting to be discovered from the life within our planet’s oceans, as the Guest Editor of this Special Issue of Marine Drugs, I personally invite you to contribute your latest research describing bioassay-guided isolation and identification of novel, bioactive marine natural products, from any marine-based organisms.

Dr. Rob Keyzers
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 2000 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

  • Biological activity
  • Phenotypic assay
  • Enzyme inhibition assay
  • Mode of action
  • Isolation
  • Structural elucidation
  • Bioassay guided fractionation

Published Papers (6 papers)

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Research

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Open AccessArticle Antioxidant and Neuroprotective Potential of the Brown Seaweed Bifurcaria bifurcata in an in vitro Parkinson’s Disease Model
Mar. Drugs 2019, 17(2), 85; https://doi.org/10.3390/md17020085
Received: 17 December 2018 / Revised: 21 January 2019 / Accepted: 23 January 2019 / Published: 1 February 2019
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Abstract
Bifurcaria bifurcata is a marine brown seaweed mainly found on the Atlantic coast. Herein, we report the antioxidant and neuroprotective activities of seven fractions (F1–F7) obtained by normal phase chromatography from the B. bifurcata dichloromethane extract, as well as of its two major [...] Read more.
Bifurcaria bifurcata is a marine brown seaweed mainly found on the Atlantic coast. Herein, we report the antioxidant and neuroprotective activities of seven fractions (F1–F7) obtained by normal phase chromatography from the B. bifurcata dichloromethane extract, as well as of its two major isolated diterpenes. Total phenolic content of fractions was determined by the Folin–Ciocalteu method, while antioxidant activity was evaluated by the DPPH, ORAC, and FRAP assays. Neuroprotective effects were evaluated in a neurotoxic model induced by 6-hydroxydopamine (6-OHDA) in a human neuroblastoma cell line (SH-SY5Y), while the mechanisms associated to neuroprotection were investigated by the determination of mitochondrial membrane potential, H2O2 production, Caspase-3 activity, and by observation of DNA fragmentation. Fractions F4 and F5 exhibited the best neuroprotective and antioxidant activities, respectively. F4 fraction prevented changes in mitochondrial potential, and induced a reduction of H2O2 levels production and an increase in cell viability, suggesting that it may contain multi-target compounds acting on different pathways. Hence, this fraction was subjected to purification steps, affording the known diterpenes eleganolone and eleganonal. Both compounds exhibited antioxidant potential, being interesting candidates for further neuroprotective studies. Full article
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Open AccessArticle Anti-Acanthamoeba Activity of Brominated Sesquiterpenes from Laurencia johnstonii
Mar. Drugs 2018, 16(11), 443; https://doi.org/10.3390/md16110443
Received: 22 October 2018 / Revised: 7 November 2018 / Accepted: 9 November 2018 / Published: 11 November 2018
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Abstract
Focused on our interest to develop novel antiparasistic agents, the present study was aimed to evaluate the biological activity of an extract of Laurencia johnstonii collected in Baja California Sur, Mexico, against an Acantamoeba castellanii Neff strain. Bioassay-guided fractionation allowed us to identify [...] Read more.
Focused on our interest to develop novel antiparasistic agents, the present study was aimed to evaluate the biological activity of an extract of Laurencia johnstonii collected in Baja California Sur, Mexico, against an Acantamoeba castellanii Neff strain. Bioassay-guided fractionation allowed us to identify the amoebicidal diastereoisomers α-bromocuparane (4) and α-isobromocuparane (5). Furthermore, bromination of the inactive laurinterol (1) and isolaurinterol (2) yielded four halogenated derivatives, (6)–(9), which improved the activity of the natural sesquiterpenes. Among them, the most active compound was 3α-bromojohnstane (7), a sesquiterpene derivative which possesses a novel carbon skeleton johnstane. Full article
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Open AccessArticle Anti-MRSA Sesquiterpenes from the Semi-Mangrove Plant Myoporum bontioides A. Gray
Mar. Drugs 2018, 16(11), 438; https://doi.org/10.3390/md16110438
Received: 15 October 2018 / Revised: 31 October 2018 / Accepted: 5 November 2018 / Published: 8 November 2018
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Abstract
The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. [...] Read more.
The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. Gray, which led to the isolation of two new sesquiterpene alkaloids (1 and 2) and six known furanosesquiterpenes (38). Their structures were elucidated on the basis of extensive analysis of their 1D, 2D NMR and mass spectroscopic data. These two new alkaloids (1 and 2) displayed potent anti-MRSA activity with MIC value of 6.25 μg/mL. This is the first report of sesquiterpene alkaloids from the plants of Myoporum genus and their anti-MRSA activity. Full article
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Open AccessArticle Cytotoxic Tetrahydroxanthone Dimers from the Mangrove-Associated Fungus Aspergillus versicolor HDN1009
Mar. Drugs 2018, 16(9), 335; https://doi.org/10.3390/md16090335
Received: 22 August 2018 / Revised: 10 September 2018 / Accepted: 12 September 2018 / Published: 14 September 2018
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Abstract
Three new tetrahydroxanthone dimers, 5-epi-asperdichrome (1), versixanthones N (2), and O (3), were isolated from the mangrove-derived fungus Aspergillus versicolor HDN1009. Their structures, including the absolute configurations, were elucidated by NMR, HRMS, and circular dichroism [...] Read more.
Three new tetrahydroxanthone dimers, 5-epi-asperdichrome (1), versixanthones N (2), and O (3), were isolated from the mangrove-derived fungus Aspergillus versicolor HDN1009. Their structures, including the absolute configurations, were elucidated by NMR, HRMS, and circular dichroism (CD) experiments. Among them, compound 1 was the second example of tetrahydroxanthone dimers, which dimerized by a rare diaryl ether linkage and showed promising antibacterial activities against Vibrio parahemolyticus, Bacillus subtilis, Mycobacterium phlei, and Pseudomonas aeruginosa, with MIC values ranging from 100 μM to 200 μM; whilst compounds 2 and 3 exhibited extensive cytotoxicities against five cancer cell lines (HL-60, K562, H1975, MGC803, and HO-8910), with IC50 values ranging from 1.7 μM to 16.1 μM. Full article
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Open AccessArticle Mycophenolic Acid Derivatives with Immunosuppressive Activity from the Coral-Derived Fungus Penicillium bialowiezense
Mar. Drugs 2018, 16(7), 230; https://doi.org/10.3390/md16070230
Received: 12 June 2018 / Revised: 3 July 2018 / Accepted: 4 July 2018 / Published: 7 July 2018
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Abstract
Mycophenolic acid (MPA) is a potent inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitor for immunosuppressive chemotherapy. Most importantly, as the 2-morpholinoethyl ester prodrug of MPA, mycophenolate mofetil (MMF) is a well-known immunosuppressant used to prevent rejection in organ transplantations. Nevertheless, due to its frequently occurred side [...] Read more.
Mycophenolic acid (MPA) is a potent inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitor for immunosuppressive chemotherapy. Most importantly, as the 2-morpholinoethyl ester prodrug of MPA, mycophenolate mofetil (MMF) is a well-known immunosuppressant used to prevent rejection in organ transplantations. Nevertheless, due to its frequently occurred side effects, searching for new therapeutic agents is ongoing. In our current work, by virtue of efficient bioassay-guided fractionation and purification, eleven mycophenolic acid derivatives, including five previously unreported metabolites (37) and six known compounds (1, 2, and 811), were obtained from the coral-derived fungus Penicillium bialowiezense. Their structures were elucidated by means of extensive spectroscopic analyses (including 1D and 2D NMR and HRESIMS data) and comparison of the NMR and other physical data with those reported in the literature in the case of the known compounds. All the isolates 111 were evaluated for the immunosuppressive activity, and 13 showed potent IMPDH2 inhibitory potency with IC50 values of 0.84–0.95 μM, which were comparable to that of MPA (the positive control), while 410 showed significant inhibitory potency with IC50 values of 3.27–24.68 μM. All the MPA derivatives showed promising immunosuppressive activity, endowing them as potential drug leads for organ transplantations and autoimmune related diseases. Full article
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Review

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Open AccessReview Current Screening Methodologies in Drug Discovery for Selected Human Diseases
Mar. Drugs 2018, 16(8), 279; https://doi.org/10.3390/md16080279
Received: 7 August 2018 / Accepted: 11 August 2018 / Published: 14 August 2018
Cited by 1 | PDF Full-text (393 KB) | HTML Full-text | XML Full-text
Abstract
The increase of many deadly diseases like infections by multidrug-resistant bacteria implies re-inventing the wheel on drug discovery. A better comprehension of the metabolisms and regulation of diseases, the increase in knowledge based on the study of disease-born microorganisms’ genomes, the development of [...] Read more.
The increase of many deadly diseases like infections by multidrug-resistant bacteria implies re-inventing the wheel on drug discovery. A better comprehension of the metabolisms and regulation of diseases, the increase in knowledge based on the study of disease-born microorganisms’ genomes, the development of more representative disease models and improvement of techniques, technologies, and computation applied to biology are advances that will foster drug discovery in upcoming years. In this paper, several aspects of current methodologies for drug discovery of antibacterial and antifungals, anti-tropical diseases, antibiofilm and antiquorum sensing, anticancer and neuroprotectors are considered. For drug discovery, two different complementary approaches can be applied: classical pharmacology, also known as phenotypic drug discovery, which is the historical basis of drug discovery, and reverse pharmacology, also designated target-based drug discovery. Screening methods based on phenotypic drug discovery have been used to discover new natural products mainly from terrestrial origin. Examples of the discovery of marine natural products are provided. A section on future trends provides a comprehensive overview on recent advances that will foster the pharmaceutical industry. Full article
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