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In Vitro and In Vivo Approaches to Study Potential Marine Drugs

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

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 15474

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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
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Dr. Ivan Cheng-Sanchez

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Department of Chemistry, University of Zurich, Zurich, Switzerland
Interests: total synthesis; natural products; medicinal chemistry
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 are still a challenging, growing problem for human health. For example, according to the World Health Organization (WHO), cancer is the second leading cause of death globally and is responsible for an estimated 9.6 million deaths in 2018. Globally, about 1 in 6 deaths is due to cancer. In this context, the vast marine world fits perfectly as a natural source for the discovery of new potential drugs. 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.

Prof. Dr. Francisco Sarabia
Dr. Ivan Cheng-Sanchez
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

Antitumoral
Marine natural products
Biological activity
Total synthesis
Synthetic approaches
Analogues
Anti-inflammatory
Antimicrobial
Antiviral

Published Papers (5 papers)

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Research

15 pages, 3166 KiB

Open AccessArticle

Glucuronomannan GM2 from Saccharina japonica Enhanced Mitochondrial Function and Autophagy in a Parkinson’s Model

by Yingjuan Liu, Weihua Jin, Zhenzhen Deng, Quanbin Zhang and Jing Wang

Mar. Drugs 2021, 19(2), 58; https://doi.org/10.3390/md19020058 - 25 Jan 2021

Cited by 4 | Viewed by 2191

Abstract

Parkinson’s disease (PD), one of the most common neurodegenerative disorders, is caused by dopamine depletion in the striatum and dopaminergic neuron degeneration in the substantia nigra. In our previous study, we hydrolyzed the fucoidan from Saccharina japonica, obtaining three glucuronomannan oligosaccharides (GMn; GM1, GM2, and GM3) and found that GMn ameliorated behavioral deficits in Parkinsonism mice and downregulated the apoptotic signaling pathway, especially with GM2 showing a more effective role in neuroprotection. However, the neuroprotective mechanism is unclear. Therefore, in this study, we aimed to assess the neuroprotective effects of GM2 in vivo and in vitro. We applied GM2 in 1-methyl-4-phenylpyridinium (MPP⁺)-treated PC12 cells, and the results showed that GM2 markedly improved the cell viability and mitochondrial membrane potential, inhibited MPP⁺-induced apoptosis, and enhanced autophagy. Furthermore, GM2 contributed to reducing the loss of dopaminergic neurons in 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mice through enhancing autophagy. These data indicate that a possible protection of mitochondria and upregulation of autophagy might underlie the observed neuroprotective effects, suggesting that GM2 has potential as a promising multifunctional lead disease-modifying therapy for PD. These findings might pave the way for additional treatment strategies utilizing carbohydrate drugs in PD. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs)

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15 pages, 3143 KiB

Open AccessArticle

Immunomodulatory Effects of a Low-Molecular Weight Polysaccharide from Enteromorpha prolifera on RAW 264.7 Macrophages and Cyclophosphamide- Induced Immunosuppression Mouse Models

by Yingjuan Liu, Xiaolin Wu, Weihua Jin and Yunliang Guo

Mar. Drugs 2020, 18(7), 340; https://doi.org/10.3390/md18070340 - 28 Jun 2020

Cited by 35 | Viewed by 3585

Abstract

The water-soluble polysaccharide EP2, from Enteromorpha prolifera, belongs to the group of polysaccharides known as glucuronoxylorhamnan, which mainly contains glucuronic acid (GlcA), xylose (Xyl), and rhamnose (Rha). The aim of this study was to detect the immunomodulatory effects of EP2 on RAW 264.7 macrophages and cyclophosphamide (CYP)-induced immunosuppression mouse models. The cells were treated with EP2 for different time periods (0, 0.5, 1, 3, and 6 h). The results showed that EP2 promoted nitric oxide production and up-regulated the expression of pro-inflammatory cytokines, such as IL-1β, IL-6, and TNF-α, in a time-dependent manner. Furthermore, we found that EP2-activated iNOS, COX2, and NLRP3 inflammasomes, and the TLR4/MAPK/NF-κB signaling pathway played an important role. Moreover, EP2 significantly increased the body weight, spleen index, thymus index, inflammatory cell counts, and the levels of IL-1β, IL-6, and TNF-α in CYP-induced immunosuppression mouse models. These results indicate that EP2 might be a potential immunomodulatory drug and provide the scientific basis for the comprehensive utilization and evaluation of E. prolifera in future applications. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs)

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15 pages, 2494 KiB

Open AccessArticle

Bengamide Analogues Show A Potent Antitumor Activity against Colon Cancer Cells: A Preliminary Study

by Beatriz García-Pinel, Cristina Porras-Alcalá, Laura Cabeza, Raul Ortiz, José Prados, Consolación Melguizo, Iván Cheng-Sánchez, Juan Manuel López-Romero and Francisco Sarabia

Mar. Drugs 2020, 18(5), 240; https://doi.org/10.3390/md18050240 - 02 May 2020

Cited by 6 | Viewed by 3117

Abstract

The limited success and side effects of the current chemotherapeutic strategies against colorectal cancer (CRC), the third most common cancer worldwide, demand an assay with new drugs. The prominent antitumor activities displayed by the bengamides (Ben), a family of natural products isolated from marine sponges of the Jaspidae family, were explored and investigated as a new option to improve CRC treatment. To this end, two potent bengamide analogues, Ben I (5) and Ben V (10), were selected for this study, for which they were synthesized according to a new synthetic strategy recently developed in our laboratories. Their antitumor effects were analyzed in human and mouse colon cell lines, using cell cycle analysis and antiproliferative assays. In addition, the toxicity of the selected analogues was tested in human blood cells. These biological studies revealed that Ben I and V produced a significant decrease in CRC cell proliferation and induced a significant cell cycle alteration with a greater antiproliferative effect on tumor cell lines than normal cells. Interestingly, no toxicity effects were detected in blood cells for both compounds. All these biological results render the bengamide analogues Ben I and Ben V as promising antitumoral agents for the treatment of CRC. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs)

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13 pages, 1033 KiB

Open AccessArticle

Aerosolizable Marine Phycotoxins and Human Health Effects: In Vitro Support for the Biogenics Hypothesis

by Emmanuel Van Acker, Maarten De Rijcke, Jana Asselman, Ilse M. Beck, Steve Huysman, Lynn Vanhaecke, Karel A.C. De Schamphelaere and Colin R. Janssen

Mar. Drugs 2020, 18(1), 46; https://doi.org/10.3390/md18010046 - 10 Jan 2020

Cited by 13 | Viewed by 3628

Abstract

Respiratory exposure to marine phycotoxins is of increasing concern. Inhalation of sea spray aerosols (SSAs), during harmful Karenia brevis and Ostreopsis ovata blooms induces respiratory distress among others. The biogenics hypothesis, however, suggests that regular airborne exposure to natural products is health promoting via a downregulation of the mechanistic target of rapamycin (mTOR) pathway. Until now, little scientific evidence supported this hypothesis. The current explorative in vitro study investigated both health-affecting and potential health-promoting mechanisms of airborne phycotoxin exposure, by analyzing cell viability effects via cytotoxicity assays and effects on the mTOR pathway via western blotting. To that end, A549 and BEAS-2B lung cells were exposed to increasing concentrations (ng·L⁻¹–mg·L⁻¹) of (1) pure phycotoxins and (2) an extract of experimental aerosolized homoyessotoxin (hYTX). The lowest cell viability effect concentrations were found for the examined yessotoxins (YTXs). Contradictory to the other phycotoxins, these YTXs only induced a partial cell viability decrease at the highest test concentrations. Growth inhibition and apoptosis, both linked to mTOR pathway activity, may explain these effects, as both YTXs were shown to downregulate this pathway. This proof-of-principle study supports the biogenics hypothesis, as specific aerosolizable marine products (e.g., YTXs) can downregulate the mTOR pathway. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs)

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13 pages, 2095 KiB

Open AccessArticle

Evaluation of Marine Diindolinonepyrane in Vitro and in Vivo: Permeability Characterization in Caco-2 Cells Monolayer and Pharmacokinetic Properties in Beagle Dogs

by Zibin Ma, Ruihua Guo, Jeevithan Elango, Bin Bao and Wenhui Wu

Mar. Drugs 2019, 17(12), 651; https://doi.org/10.3390/md17120651 - 20 Nov 2019

Cited by 5 | Viewed by 2398

Abstract

A marine fibrinolytic compound was studied for use in thrombolytic therapy. Firstly, the absorption and transportation characteristics of 2,5-BHPA (2,5-BHPA:2,5-Bis-[8-(4,8-dimethyl-nona-3,7-dienyl)-5,7-dihydroxy-8-methyl-3-keto-1,2,7,8-tertahydro-6H-pyran[a]isoindol-2-yl]-pentanoic acid, a novel pyran-isoindolone derivative with bioactivity isolated from a rare marine microorganism in our laboratory) in the human Caco-2 cells monolayer model were investigated. We collected 2,5-BHPA in the cells to calculate the total recovery, and its concentration was analyzed by LC/MS/MS (Liquid Chromatography/Mass Spectrum/Mass Spectrum). The results showed that 2,5-BHPA has low permeability and low total recoveries in the Caco-2 cells membrane. Pharmacokinetics and tissue distribution of 2,5-BHPA were investigated in beagle dogs using HPLC (High Performance Liquid Chromatography) after intravenous administration of three different doses (7.5, 5.0, 2.5 mg·kg⁻¹). Pharmacokinetic data indicated that 2,5-BHPA fitted well to a two-compartment model. Elimination half-lives (T_1/2) were 49 ± 2, 48 ± 2, and 49 ± 2 min, respectively; the peak concentrations (C_max) were 56.48 ± 6.23, 48.63 ± 5.53, and 13.64 ± 2.76 μg·mL⁻¹, respectively; clearance rates (CL) were 0.0062 ± 0.0004, 0.0071 ± 0.0008, and 0.0092 ±0.0006 L·min⁻¹·kg⁻¹, respectively; mean retention times (MRT) were 28.17 ± 1.16, 26.23 ± 0.35, and 28.66 ± 0.84 min, respectively. The low penetrability of 2,5-BHPA indicated that the intravenous route of administration is more appropriate than the oral route. Meanwhile, 2,5-BHPA showed a good pharmacokinetic profile in beagle dogs. The tissue distribution showed that 2,5-BHPA could quickly distribute into the heart, intestines, liver, stomach, spleen, lungs, testicles, urine, intestine, kidneys, brain, and feces. The concentration of 2,5-BHPA was higher in the liver and bile. Interestingly, 2,5-BHPA was detected in the brain. Taken together, the above results suggested that our work might be beneficial in the development of agents for thrombolytic treatment. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs)

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