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Marine Drugs
Special Issues
Marine Antiparasitic Agents
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Marine Antiparasitic Agents

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Marine Pharmacology".

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 14663

Special Issue Editors

Dr. Saccoccia Fulvio

E-Mail Website
Guest Editor
National Research Council, Rome, Italy
Interests: schistosomiasis; biochemistry; HDACs inhibitors; crystallography; phylogenetics; drug discovery; drug repurposing
Special Issues, Collections and Topics in MDPI journals
Dr. Carla Fernandes

E-Mail Website
Guest Editor
1. Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
2. Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal
Interests: medicinal chemistry; organic chemistry; chiral bioactive substances; enantioselective studies; chirality; chromatography
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Marine compounds have been demonstrated to exert a wide number of therapeutic effects, and their use has been proposed against tumor, genetic disease, bacteria, viruses and other infectious diseases, as coadjuvants or new drugs. Additionally, a wide number of naturally occurring marine drugs have been demonstrated to exert therapeutic effects against many parasites, affecting both humans and animals. Nevertheless, there is a growing interest in natural extracts used in traditional medicine, which are under consideration as therapeutic agents in the treatment of infectious diseases. We are pleased to announce a Special Issue of Marine Drugs entitled “Marine Antiparasitic Drugs”. This Special Issue has the rather ambitious purpose of collecting a pool of original research and review papers focused on the use of agents  from marine sources, displaying a broad or specific antiparasitic activity, with a special interest in those agents which have been obtained with procedures safe for human health and with an eco-friendly footprint. To this aim, there is interest in agents obtained with extractions using naturally occurring solvents such as edible oils, or others coming from natural sources which may be regarded as suitable in view of an economic return for the original country affected by endemic parasitosis, considering that many naturally occurring parasites are found in some of the poorest regions of the world. Marine compounds are also interesting models for molecular modifications and/or total synthesis to obtain more potent compounds, with improved antiparasitic properties and in higher quantity. We also welcome manuscripts describing the synthesis of marine-derived antiparasitic agents. Among parasites, we are especially interested in protozoans and multicellular eukaryotics. Thus, papers accounting for safe and green chemistry, as well as targeted interventions linked to the therapeutic properties of marine agents from autochthonous species against parasites infecting humans and livestock, will be of outstanding interest for this Special Issue.

Dr. Saccoccia Fulvio
Dr. Carla Fernandes
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 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

  • antiparasitic
  • marine agents
  • safe extraction
  • green chemistry
  • parasites
  • helminths
  • protozoans

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Published Papers (5 papers)

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Research

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15 pages, 964 KiB  
Article
Synthesis and Evaluation of Marine-Inspired Compounds Result in Hybrids with Antitrypanosomal and Antileishmanial Activities
by Diogo Teixeira Carvalho, Melissa Teixeira, Sara Luelmo, Nuno Santarém, Eugénia Pinto, Anabela Cordeiro-da-Silva and Emília Sousa
Mar. Drugs 2023, 21(11), 551; https://doi.org/10.3390/md21110551 - 24 Oct 2023
Viewed by 1575
Abstract
Natural products are a very rich source for obtaining new compounds with therapeutic potential. In the search for new antiparasitic and antimicrobial agents, molecular hybrids were designed based on the structures of antimicrobial marine quinazolinones and eugenol, a natural phenolic compound. Following reports [...] Read more.
Natural products are a very rich source for obtaining new compounds with therapeutic potential. In the search for new antiparasitic and antimicrobial agents, molecular hybrids were designed based on the structures of antimicrobial marine quinazolinones and eugenol, a natural phenolic compound. Following reports of the therapeutic potential of quinazolinones and eugenol derivatives, it was expected that the union of these pharmacophores could generate biologically relevant substances. The designed compounds were obtained by classical synthetic procedures and were characterized by routine spectrometric techniques. Nine intermediates and final products were then evaluated in vitro against Trypanosoma brucei and Leishmania infantum. Antifungal and antibacterial activity were also evaluated. Six compounds (9b, 9c, 9d, 10b, 10c, and 14) showed mild activity against T. brucei with IC50 in the range of 11.17–31.68 μM. Additionally, intermediate 9c showed anti-Leishmania activity (IC50 7.54 μM) and was six times less cytotoxic against THP-1 cells. In conclusion, novel derivatives with a simple quinazolinone scaffold showing selectivity against parasites without antibacterial and antifungal activities were disclosed, paving the way for new antitrypanosomal agents. Full article
(This article belongs to the Special Issue Marine Antiparasitic Agents)
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14 pages, 1625 KiB  
Article
Laurequinone, a Lead Compound against Leishmania
by Sara García-Davis, Atteneri López-Arencibia, Carlos J. Bethencourt-Estrella, Desirée San Nicolás-Hernández, Ezequiel Viveros-Valdez, Ana R. Díaz-Marrero, José J. Fernández, Jacob Lorenzo-Morales and José E. Piñero
Mar. Drugs 2023, 21(6), 333; https://doi.org/10.3390/md21060333 - 30 May 2023
Cited by 4 | Viewed by 2100
Abstract
Among neglected tropical diseases, leishmaniasis is one of the leading causes, not only of deaths but also of disability-adjusted life years. This disease, caused by protozoan parasites of the genus Leishmania, triggers different clinical manifestations, with cutaneous, mucocutaneous, and visceral forms. As existing [...] Read more.
Among neglected tropical diseases, leishmaniasis is one of the leading causes, not only of deaths but also of disability-adjusted life years. This disease, caused by protozoan parasites of the genus Leishmania, triggers different clinical manifestations, with cutaneous, mucocutaneous, and visceral forms. As existing treatments for this parasitosis are not sufficiently effective or safe for the patient, in this work, different sesquiterpenes isolated from the red alga Laurencia johnstonii have been studied for this purpose. The different compounds were tested in vitro against the promastigote and amastigote forms of Leishmania amazonensis. Different assays were also performed, including the measurement of mitochondrial potential, determination of ROS accumulation, and chromatin condensation, among others, focused on the detection of the cell death process known in this type of organism as apoptosis-like. Five compounds were identified that displayed leishmanicidal activity: laurequinone, laurinterol, debromolaurinterol, isolaurinterol, and aplysin, showing IC50 values against promastigotes of 1.87, 34.45, 12.48, 10.09, and 54.13 µM, respectively. Laurequinone was the most potent compound tested and was shown to be more effective than the reference drug miltefosine against promastigotes. Different death mechanism studies carried out showed that laurequinone appears to induce programmed cell death or apoptosis in the parasite studied. The obtained results underline the potential of this sesquiterpene as a novel anti-kinetoplastid therapeutic agent. Full article
(This article belongs to the Special Issue Marine Antiparasitic Agents)
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11 pages, 1026 KiB  
Article
Synthesis and Antimalarial Evaluation of Halogenated Analogues of Thiaplakortone A
by Folake A. Egbewande, Brett D. Schwartz, Sandra Duffy, Vicky M. Avery and Rohan A. Davis
Mar. Drugs 2023, 21(5), 317; https://doi.org/10.3390/md21050317 - 22 May 2023
Viewed by 1892
Abstract
The incorporation of bromine, iodine or fluorine into the tricyclic core structure of thiaplakortone A (1), a potent antimalarial marine natural product, is reported. Although yields were low, it was possible to synthesise a small nine-membered library using the previously synthesised [...] Read more.
The incorporation of bromine, iodine or fluorine into the tricyclic core structure of thiaplakortone A (1), a potent antimalarial marine natural product, is reported. Although yields were low, it was possible to synthesise a small nine-membered library using the previously synthesised Boc-protected thiaplakortone A (2) as a scaffold for late-stage functionalisation. The new thiaplakortone A analogues (3–11) were generated using N-bromosuccinimide, N-iodosuccinimide or a Diversinate™ reagent. The chemical structures of all new analogues were fully characterised by 1D/2D NMR, UV, IR and MS data analyses. All compounds were evaluated for their antimalarial activity against Plasmodium falciparum 3D7 (drug-sensitive) and Dd2 (drug-resistant) strains. Incorporation of halogens at positions 2 and 7 of the thiaplakortone A scaffold was shown to reduce antimalarial activity compared to the natural product. Of the new compounds, the mono-brominated analogue (compound 5) displayed the best antimalarial activity with IC50 values of 0.559 and 0.058 μM against P. falciparum 3D7 and Dd2, respectively, with minimal toxicity against a human cell line (HEK293) observed at 80 μM. Of note, the majority of the halogenated compounds showed greater efficacy against the P. falciparum drug-resistant strain. Full article
(This article belongs to the Special Issue Marine Antiparasitic Agents)
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Review

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27 pages, 4278 KiB  
Review
Therapeutic Potential of Marine-Derived Cyclic Peptides as Antiparasitic Agents
by Ricardo Ribeiro, Lia Costa, Eugénia Pinto, Emília Sousa and Carla Fernandes
Mar. Drugs 2023, 21(12), 609; https://doi.org/10.3390/md21120609 - 25 Nov 2023
Cited by 4 | Viewed by 4720
Abstract
Parasitic diseases still compromise human health. Some of the currently available therapeutic drugs have limitations considering their adverse effects, questionable efficacy, and long treatment, which have encouraged drug resistance. There is an urgent need to find new, safe, effective, and affordable antiparasitic drugs. [...] Read more.
Parasitic diseases still compromise human health. Some of the currently available therapeutic drugs have limitations considering their adverse effects, questionable efficacy, and long treatment, which have encouraged drug resistance. There is an urgent need to find new, safe, effective, and affordable antiparasitic drugs. Marine-derived cyclic peptides have been increasingly screened as candidates for developing new drugs. Therefore, in this review, a systematic analysis of the scientific literature was performed and 25 marine-derived cyclic peptides with antiparasitic activity (1–25) were found. Antimalarial activity is the most reported (51%), followed by antileishmanial (27%) and antitrypanosomal (20%) activities. Some compounds showed promising antiparasitic activity at the nM scale, being active against various parasites. The mechanisms of action and targets for some of the compounds have been investigated, revealing different strategies against parasites. Full article
(This article belongs to the Special Issue Marine Antiparasitic Agents)
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30 pages, 2013 KiB  
Review
Promising Antiparasitic Natural and Synthetic Products from Marine Invertebrates and Microorganisms
by Mingyue Zhang, Qinrong Zhang, Qunde Zhang, Xinyuan Cui and Lifeng Zhu
Mar. Drugs 2023, 21(2), 84; https://doi.org/10.3390/md21020084 - 25 Jan 2023
Cited by 4 | Viewed by 3431
Abstract
Parasitic diseases still threaten human health. At present, a number of parasites have developed drug resistance, and it is urgent to find new and effective antiparasitic drugs. As a rich source of biological compounds, marine natural products have been increasingly screened as candidates [...] Read more.
Parasitic diseases still threaten human health. At present, a number of parasites have developed drug resistance, and it is urgent to find new and effective antiparasitic drugs. As a rich source of biological compounds, marine natural products have been increasingly screened as candidates for developing new antiparasitic drugs. The literature related to the study of the antigenic animal activity of marine natural compounds from invertebrates and microorganisms was selected to summarize the research progress of marine compounds and the structure–activity relationship of these compounds in the past five years and to explore the possible sources of potential antiparasitic drugs for parasite treatment. Full article
(This article belongs to the Special Issue Marine Antiparasitic Agents)
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