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Marine Drugs
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In Vitro and In Vivo Approaches to Study Potential Marine...
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In Vitro and In Vivo Approaches to Study Potential Marine Drugs II

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

Deadline for manuscript submissions: closed (31 May 2022) | Viewed by 20140

Special Issue Editors

Dr. Ivan Cheng-Sanchez

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Guest Editor
Department of Chemistry, University of Zurich, Zurich, Switzerland
Interests: total synthesis; natural products; medicinal chemistry
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Francisco Sarabia

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Guest Editor
Department of Organic Chemistry, Faculty of Science, University of Málaga, 29071 Málaga, Spain
Interests: natural products; bioactive compounds; total synthesis; antitumor; antibiotics; cyclodepsipeptides; cyclopeptides
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The marine world represents a uniquely rich source of new bioactive metabolites, with unprecedented structures, fascinating biological profiles, and valuable therapeutic potential. Natural products of marine origin display a wide range of biological activities, such as antitumor, anti-inflammatory, and antimicrobial, among others. These compounds are attractive targets because they could represent the solution to a high number of diseases that still constitute a challenging, growing problem for human health. A current example is the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which has resulted in the coronavirus disease 2019 (COVID-19) pandemic, which has infected over 90 million people worldwide as of mid-January 2021. In this context, the lack of approved drugs to treat COVID-19 makes the vast marine world fit perfectly as a natural source for the discovery of new potential candidates, but also for other important human diseases that are still present and seriously affect human health, such as cancer, which is the second leading cause of death globally. The unexplored marine environment is a wide source of unprecedented compounds with new mechanisms of biological action and intriguing molecular structures that could represent the basis of new scaffolds of interest for the pharmaceuticals and could be the solution to overcome these devastating diseases.

This Special Issue will cover the entire scope of marine natural products that display in vitro and/or in vivo biological activities, also including their isolation, biology, and chemistry, as well as synthetic approaches towards them and related analogues. 

Dr. Ivan Cheng-Sanchez
Prof. Dr. Francisco Sarabia
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
  • Biological activity
  • Antitumoral
  • Cancer
  • Total synthesis
  • Synthetic approaches
  • Analogues

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Published Papers (4 papers)

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Research

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23 pages, 1547 KiB  
Article
In Vivo Nutritional Assessment of the Microalga Nannochloropsis gaditana and Evaluation of the Antioxidant and Antiproliferative Capacity of Its Functional Extracts
by Rosario Martínez, Alejandro García-Beltrán, Garyfallia Kapravelou, Cristina Mesas, Laura Cabeza, Gloria Perazzoli, Palmira Guarnizo, Alberto Rodríguez-López, Roberto Andrés Vallejo, Milagros Galisteo, Pilar Aranda, Jose Prados, María López-Jurado, Consolación Melguizo and Jesus M. Porres
Mar. Drugs 2022, 20(5), 318; https://doi.org/10.3390/md20050318 - 11 May 2022
Cited by 10 | Viewed by 3567
Abstract
Nannochloropsis gaditana is a microalga with interesting nutritional and functional value due to its high content of protein, polyunsaturated fatty acids, and bioactive compounds. However, the hardness of its cell wall prevents accessibility to these components. This work aimed to study the effect [...] Read more.
Nannochloropsis gaditana is a microalga with interesting nutritional and functional value due to its high content of protein, polyunsaturated fatty acids, and bioactive compounds. However, the hardness of its cell wall prevents accessibility to these components. This work aimed to study the effect of a treatment to increase the fragility of the cell wall on the bioavailability of its nutrients and functional compounds. The antioxidant and antiproliferative capacity of functional extracts from treated and untreated N. gaditana was assessed, and the profile of bioactive compounds was characterized. Furthermore, to study the effect of treatment on its nutrient availability and functional capacity, an in vivo experiment was carried out using a rat experimental model and a 20% dietary inclusion level of microalgae. Functional extracts from treated N. gaditana exhibited higher antioxidant activity than the untreated control. Furthermore, the treated microalga induced hypoglycemic action, higher nitrogen digestibility, and increased hepatic antioxidant activity. In conclusion, N. gaditana has interesting hepatoprotective, antioxidant, and anti-inflammatory potential, thus proving itself an ideal functional food candidate, especially if the microalga is treated to increase the fragility of its cell wall before consumption. Full article
(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs II)
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20 pages, 15265 KiB  
Article
Ecklonia cava Attenuates PM2.5-Induced Cognitive Decline through Mitochondrial Activation and Anti-Inflammatory Effect
by Seon Kyeong Park, Jin Yong Kang, Jong Min Kim, Hyun-Jin Kim and Ho Jin Heo
Mar. Drugs 2021, 19(3), 131; https://doi.org/10.3390/md19030131 - 27 Feb 2021
Cited by 16 | Viewed by 3758
Abstract
To evaluate the effects of Ecklonia cava (E. cava) on ambient-pollution-induced neurotoxicity, we used a mouse model exposed to particulate matter smaller than 2.5 µm in aerodynamic diameter (PM2.5). The intake of water extract from E. cava (WEE) effectively [...] Read more.
To evaluate the effects of Ecklonia cava (E. cava) on ambient-pollution-induced neurotoxicity, we used a mouse model exposed to particulate matter smaller than 2.5 µm in aerodynamic diameter (PM2.5). The intake of water extract from E. cava (WEE) effectively prevented the learning and memory decline. After a behavioral test, the toll-like receptor (TLR)-4-initiated inflammatory response was confirmed by PM2.5 exposure in the lung and brain tissues, and the WEE was regulated through the inhibition of nuclear factor-kappa B (NF-κB)/inflammasome formation signaling pathway and pro-inflammatory cytokines (IL-6 and IFN-γ). The WEE also effectively improved the PM2.5-induced oxidative damage of the lungs and brain through the inhibition of malondialdehyde (MDA) production and the activation of mitochondrial activity (mitochondrial ROS content, mitochondria membrane potential (MMP), adenosine triphosphate (ATP) content, and mitochondria-mediated apoptotic molecules). In particular, the WEE regulated the cognition-related proteins (a decreased amyloid precursor protein (APP) and p-Tau, and an increased brain-derived neurotrophic factor (BDNF)) associated with PM2.5-induced cognitive dysfunction. Additionally, the WEE prevented the inactivation of acetylcholine (ACh) synthesis and release as a neurotransmitter by regulating the acetylcholinesterase (AChE) activity, choline acetyltransferase (ChAT), and ACh receptor (AChR)-α3 in the brain tissue. The bioactive compounds of the WEE were detected as the polysaccharide (average Mw; 160.13 kDa) and phenolic compounds including 2′-phloroeckol. Full article
(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs II)
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Review

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37 pages, 9386 KiB  
Review
Antibody-Drug Conjugates Containing Payloads from Marine Origin
by Iván Cheng-Sánchez, Federico Moya-Utrera, Cristina Porras-Alcalá, Juan M. López-Romero and Francisco Sarabia
Mar. Drugs 2022, 20(8), 494; https://doi.org/10.3390/md20080494 - 30 Jul 2022
Cited by 13 | Viewed by 8039
Abstract
Antibody-drug conjugates (ADCs) are an important class of therapeutics for the treatment of cancer. Structurally, an ADC comprises an antibody, which serves as the delivery system, a payload drug that is a potent cytotoxin that kills cancer cells, and a chemical linker that [...] Read more.
Antibody-drug conjugates (ADCs) are an important class of therapeutics for the treatment of cancer. Structurally, an ADC comprises an antibody, which serves as the delivery system, a payload drug that is a potent cytotoxin that kills cancer cells, and a chemical linker that connects the payload with the antibody. Unlike conventional chemotherapy methods, an ADC couples the selective targeting and pharmacokinetic characteristics related to the antibody with the potent cytotoxicity of the payload. This results in high specificity and potency by reducing off-target toxicities in patients by limiting the exposure of healthy tissues to the cytotoxic drug. As a consequence of these outstanding features, significant research efforts have been devoted to the design, synthesis, and development of ADCs, and several ADCs have been approved for clinical use. The ADC field not only relies upon biology and biochemistry (antibody) but also upon organic chemistry (linker and payload). In the latter, total synthesis of natural and designed cytotoxic compounds, together with the development of novel synthetic strategies, have been key aspects of the consecution of clinical ADCs. In the case of payloads from marine origin, impressive structural architectures and biological properties are observed, thus making them prime targets for chemical synthesis and the development of ADCs. In this review, we explore the molecular and biological diversity of ADCs, with particular emphasis on those containing marine cytotoxic drugs as the payload. Full article
(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs II)
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27 pages, 3247 KiB  
Review
Natural Marine Products: Anti-Colorectal Cancer In Vitro and In Vivo
by Ningning Han, Jianjiang Li and Xia Li
Mar. Drugs 2022, 20(6), 349; https://doi.org/10.3390/md20060349 - 25 May 2022
Cited by 14 | Viewed by 3985
Abstract
Colorectal cancer, a malignant tumor with high mortality, has a poor prognosis due to drug resistance and toxicity in clinical surgery and chemotherapy. Thus, finding safer and more efficient drugs for clinical trials is vital and urgent. Natural marine compounds, with rich resources [...] Read more.
Colorectal cancer, a malignant tumor with high mortality, has a poor prognosis due to drug resistance and toxicity in clinical surgery and chemotherapy. Thus, finding safer and more efficient drugs for clinical trials is vital and urgent. Natural marine compounds, with rich resources and original chemical structures, are applied widely in anticancer treatments. We provide a systematic overview of recently reported marine compounds such as alkaloids, peptides, terpenoids, polysaccharides, and carotenoids from in vitro, in vivo, and clinical studies. The in vitro studies summarized the marine origins and pharmacological mechanisms, including anti-proliferation, anti-angiogenesis, anti-migration, anti-invasion, the acceleration of cycle arrest, and the promotion of tumor apoptosis, of various compounds. The in vivo studies outlined the antitumor effects of marine compounds on colorectal cancer model mice and evaluated their efficacy in terms of tumor inhibition, hepatotoxicity, and nephrotoxicity. The clinical studies summarized the major chemical classifications and targets of action of the clinical drugs that have entered clinical approval and completed approval for marine anticancer. In summary, we present the current situation regarding the application of natural anti-colorectal cancer marine compounds and prospects for their clinical application. Full article
(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs II)
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