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Marine Drugs
Special Issues
Perspectives for the Development of New Multitarget Marine Drugs
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Perspectives for the Development of New Multitarget Marine Drugs

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Synthesis and Medicinal Chemistry of Marine Natural Products".

Deadline for manuscript submissions: closed (30 September 2024) | Viewed by 9492

Special Issue Editors

Prof. Dr. Concetta Imperatore

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Guest Editor
Department of Pharmacy, University of Naples Federico II, Naples, Italy
Interests: marine natural products; isolation and stereostructural elucidation of bioactive secondary metabolites; design and synthesis of analogues of marine natural products; NMR spectroscopy; marine invertebrates
Special Issues, Collections and Topics in MDPI journals
Dr. Marcello Casertano

E-Mail Website
Guest Editor
Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, Napoli, Italy
Interests: marine bioactive products; organic chemistry; NMR spectroscopy; stereostructural elucidation; quinone reactivity; antiinfective; antimicrobial; multitarget agents parasitic infections
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, there has been growing interest in marine natural products (MNPs) since they are endowed with unusual scaffolds and have a high potential to facilitate the discovery of new leads with particular mechanisms of action. MNPs are ideal chemical probes for determining the biochemical pathways underlying a given disease and discovering novel drug targets. The main limitation of MNPs is that they are usually isolated in low amounts that are sufficient for elucidation of their structure but inadequate for extensive drug screening. In this context, organic synthesis proves to be a powerful tool to enhance the potential of MNPs: the synthesis of MNPs or of their analogues is one of the feasible strategies for enriching screening libraries with an adequate number of MNPs and MNP-inspired molecules.

The incidence of chronic multifactorial diseases has been increasing dramatically in the last few years, placing a high economic burden on public health systems. The combination of various drugs is usually the best option for the treatment of multifactorial diseases, but can lead to undesired drug–drug interactions and reduced patient adherence. The lack of efficiency of traditional drug therapies has stimulated pharmacological research in the search for a multi-target-directed ligand approach; in this approach, MNPs are able to simultaneously modulate several relevant therapeutic targets of a certain disease.

For the Special Issue, “Perspectives for the Development of New Multitarget Marine Drugs”, we invite academic and industry scientists from a large number of fields to submit original and conceptual research articles. Reviews that present up-to-date knowledge on multitarget MNPs and MNP-derived synthetic compounds useful for a specific therapeutic area (e.g., antidiabetic, antitumor, anti-inflammatory, antimicrobial, etc.) are also welcome.

Prof. Dr. Concetta Imperatore
Dr. Marcello Casertano
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

  • marine natural products
  • drug combination
  • multitarget drugs
  • designed multiple ligands
  • drug repurposing
  • organic synthesis
  • marine inspired products
  • multifactorial diseases
  • marine-guided bioassays

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Published Papers (4 papers)

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Research

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18 pages, 7511 KiB  
Article
Surf Redfish-Based ZnO-NPs and Their Biological Activity with Reference to Their Non-Target Toxicity
by Ahmed I. Hasaballah, Hussein A. El-Naggar, Ibrahim E. Abd-El Rahman, Fatimah Al-Otibi, Reham M. Alahmadi, Othman F. Abdelzaher, Mohamed H. Kalaba, Basma H. Amin, Mohamed M. Mabrouk, Ahmed G. A. Gewida, Marwa F. Abd El-Kader and Mostafa A. Elbahnasawy
Mar. Drugs 2023, 21(8), 437; https://doi.org/10.3390/md21080437 - 2 Aug 2023
Cited by 3 | Viewed by 1840
Abstract
The marine environment is a rich source of bioactive compounds. Therefore, the sea cucumber was isolated from the Red Sea at the Al-Ain Al-Sokhna coast and it was identified as surf redfish (Actinopyga mauritiana). The aqueous extract of the surf redfish [...] Read more.
The marine environment is a rich source of bioactive compounds. Therefore, the sea cucumber was isolated from the Red Sea at the Al-Ain Al-Sokhna coast and it was identified as surf redfish (Actinopyga mauritiana). The aqueous extract of the surf redfish was utilized as an ecofriendly, novel and sustainable approach to fabricate zinc oxide nanoparticles (ZnO-NPs). The biosynthesized ZnO-NPs were physico-chemically characterized and evaluated for their possible antibacterial and insecticidal activities. Additionally, their safety in the non-target organism model (Nile tilapia fish) was also investigated. ZnO-NPs were spherical with an average size of 24.69 ± 11.61 nm and had a peak at 350 nm as shown by TEM and UV-Vis, respectively. XRD analysis indicated a crystalline phase of ZnO-NPs with an average size of 21.7 nm. The FTIR pattern showed biological residues from the surf redfish extract, highlighting their potential role in the biosynthesis process. DLS indicated a negative zeta potential (−19.2 mV) of the ZnO-NPs which is a good preliminary indicator for their stability. ZnO-NPs showed larvicidal activity against mosquito Culex pipiens (LC50 = 15.412 ppm and LC90 = 52.745 ppm) and a potent adulticidal effect to the housefly Musca domestica (LD50 = 21.132 ppm and LD90 = 84.930 ppm). Tested concentrations of ZnO-NPs showed strong activity against the 3rd larval instar. Topical assays revealed dose-dependent adulticidal activity against M. domestica after 24 h of treatment with ZnO-NPs. ZnO-NPs presented a wide antibacterial activity against two fish-pathogen bacteria, Pseudomonas aeruginosa and Aeromonas hydrophila. Histopathological and hematological investigations of the non-target organism, Nile tilapia fish exposed to 75–600 ppm ZnO-NPs provide dose-dependent impacts. Overall, data highlighted the potential applications of surf redfish-mediated ZnO-NPs as an effective and safe way to control mosquitoes, houseflies and fish pathogenic bacteria. Full article
(This article belongs to the Special Issue Perspectives for the Development of New Multitarget Marine Drugs)
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Review

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22 pages, 1629 KiB  
Review
Seaweeds as Nutraceutical Elements and Drugs for Diabetes Mellitus: Future Perspectives
by João Cotas, Silvia Lomartire, Leonel Pereira, Ana Valado, João Carlos Marques and Ana M. M. Gonçalves
Mar. Drugs 2024, 22(4), 168; https://doi.org/10.3390/md22040168 - 10 Apr 2024
Cited by 4 | Viewed by 3437
Abstract
Diabetes mellitus is a chronic metabolic condition marked by high blood glucose levels caused by inadequate insulin synthesis or poor insulin use. This condition affects millions of individuals worldwide and is linked to a variety of consequences, including cardiovascular disease, neuropathy, nephropathy, and [...] Read more.
Diabetes mellitus is a chronic metabolic condition marked by high blood glucose levels caused by inadequate insulin synthesis or poor insulin use. This condition affects millions of individuals worldwide and is linked to a variety of consequences, including cardiovascular disease, neuropathy, nephropathy, and retinopathy. Diabetes therapy now focuses on controlling blood glucose levels through lifestyle changes, oral medicines, and insulin injections. However, these therapies have limits and may not successfully prevent or treat diabetic problems. Several marine-derived chemicals have previously demonstrated promising findings as possible antidiabetic medicines in preclinical investigations. Peptides, polyphenols, and polysaccharides extracted from seaweeds, sponges, and other marine species are among them. As a result, marine natural products have the potential to be a rich source of innovative multitargeted medications for diabetes prevention and treatment, as well as associated complications. Future research should focus on the chemical variety of marine creatures as well as the mechanisms of action of marine-derived chemicals in order to find new antidiabetic medicines and maximize their therapeutic potential. Based on preclinical investigations, this review focuses on the next step for seaweed applications as potential multitargeted medicines for diabetes, highlighting the bioactivities of seaweeds in the prevention and treatment of this illness. Full article
(This article belongs to the Special Issue Perspectives for the Development of New Multitarget Marine Drugs)
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17 pages, 2067 KiB  
Review
The Rare Marine Bioactive Compounds in Neurological Disorders and Diseases: Is the Blood-Brain Barrier an Obstacle or a Target?
by Xiaozhen Diao, Hui Han, Bailin Li, Zhen Guo, Jun Fu and Wenhui Wu
Mar. Drugs 2023, 21(7), 406; https://doi.org/10.3390/md21070406 - 18 Jul 2023
Cited by 5 | Viewed by 2680
Abstract
The blood-brain barrier (BBB) is a dynamic barrier separating neurocytes and brain tissues from blood that is extremely sealed and strictly regulated by transporters such as aquaporin-4 (AQP-4), glucose transporter (GLUT), and specialized tight junctional complexes (TJCs) including tight junctions (TJs), adherens junctions [...] Read more.
The blood-brain barrier (BBB) is a dynamic barrier separating neurocytes and brain tissues from blood that is extremely sealed and strictly regulated by transporters such as aquaporin-4 (AQP-4), glucose transporter (GLUT), and specialized tight junctional complexes (TJCs) including tight junctions (TJs), adherens junctions (AJs), and Zonulae occludens (ZOs). With specifically selective transcellular and paracellular permeability, the BBB maintains a homeostatic microenvironment to protect the central nervous system (CNS). In recent years, increasing attention has been paied to the importance of BBB disruption and dysfunction in the pathology of neurological disorders and diseases, such as Alzheimer’s diseases (AD), Parkinson diseases (PD), stroke and cerebral edema. However, the further research on how the integral structure and function of BBB are altered under the physiological or pathological conditions is still needed. Focusing on the ultrastructural features of the BBB and combining the latest research on associated proteins and transporters, physiological regulation and pathological change of the BBB were elucidated. By summarizing the protective effects of known bioactive compounds derived from marine life on the BBB, this review aims to highlight the BBB as a key to the treatment of several major neurological diseases instead of a normally described obstacle to drug absorption and transport. Overall, the BBB’s morphological characteristics and physiological function and their regulation provide the theoretical basis for the study on the BBB and inspire the diagnosis of and therapy for neurological diseases. Full article
(This article belongs to the Special Issue Perspectives for the Development of New Multitarget Marine Drugs)
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Other

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12 pages, 2262 KiB  
Perspective
Synthesis of Marine (-)-Pelorol and Future Perspectives
by Antonio Rosales Martínez and Ignacio Rodríguez-García
Mar. Drugs 2024, 22(9), 425; https://doi.org/10.3390/md22090425 - 19 Sep 2024
Viewed by 813
Abstract
Meroterpenoid-type marine natural compounds have attracted an increasing amount of attention due to their peculiar chemical structures and their potential for the development of therapeutically important probes. Within this group of substances pelorol stands out; it is a natural compound isolated from marine [...] Read more.
Meroterpenoid-type marine natural compounds have attracted an increasing amount of attention due to their peculiar chemical structures and their potential for the development of therapeutically important probes. Within this group of substances pelorol stands out; it is a natural compound isolated from marine organisms with a unique structure and an interesting biological profile. In this article, we summarize and highlight the most interesting aspects of the synthetic procedures towards this compound, which have two common key steps. The first is the coupling of a drimanyl derivative with a compound derived from an arene. The second is a Friedel–Crafts cyclization which forms the C ring of the natural product. Despite the synthetic advances achieved so far, we consider that a more efficient synthetic procedures could be carried out, since their synthetic routes are difficult to scale up due to numerous reaction steps and the limitations imposed by the use of some reagents. In this article, we present a new and versatile retrosynthetic analysis of (-)-pelorol and analogs, which is highly desirable for their easy preparation and subsequent broad study of their biological activities. This is a retrosynthetic route that could improve those reported in the literature in terms of cost-effectiveness. Full article
(This article belongs to the Special Issue Perspectives for the Development of New Multitarget Marine Drugs)
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