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Marine Drugs
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Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities
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Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities

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

Deadline for manuscript submissions: 31 July 2025 | Viewed by 9840

Special Issue Editors

Dr. Hugo Pliego-Cortés

E-Mail Website
Guest Editor
Laboratoire de Biotechnologie et Chimie Marines, Université Bretagne Sud, Vannes, France
Interests: macroalgae; polysaccharides; bio-activity; analytical chemistry; fractionation; integrated multi-trophic aquaculture
Prof. Dr. Nathalie Bourgougnon

E-Mail Website
Guest Editor
Laboratoire de Biotechnologie et Chimie Marines, Université Bretagne Sud, Vannes, France
Interests: phycology; marine molecules; extraction eco-friendly processes; antiviral agents; SAR studies
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The marine environment holds a huge and diverse group of organisms with extraordinary capacities to thrive within challenging conditions. Their unique physiological and metabolic pathways allow them to produce a great diversity of molecules. Marine polysaccharides represent a broad spectrum of macromolecules with diverse and unusual structures; they play multiple roles and have extensive bioactive processes. At present, the most widespread uses are in the colloid industry for foods, feeds, pharmaceuticals, and cosmetics. However, its potential applications are numerous, with the potential to contribute to the marine circular economy and generate improvements in human welfare. Without a doubt, there are polysaccharides that are currently unknown, and our understanding of these is far from being concluded.

This Special Issue welcomes original research and comprehensive reviews in the field of marine polysaccharides, olisaccharides, and their derivatives with potential biological activities, such as antiviral, anticancer, anti-inflammatory, antioxidant, etc. Biochemical and structural characterization is encouraged due to its structural complexity and diversity. Marine polysaccharides and aligosaccharides sourcing is included, but is not exclusive to aquaculture, biotechnology, or synthetic biology. We hope that this Special Issue will provide the state of the art in marine polysaccharide research.

Dr. Hugo Pliego-Cortés
Prof. Dr. Nathalie Bourgougnon
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 polysaccharide
  • oligosaccharides
  • extraction
  • isolation
  • structural analysis
  • biological activity
  • bioprocessing
  • biorefinery
  • marine organism
  • aquaculture

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Published Papers (7 papers)

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Research

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18 pages, 3560 KiB  
Article
Exploring the In Vivo Fate of β-1, 3/1, 6-Glucan Using Quantitative Tandem Mass Spectrometry Based on a Structure-Specific Fragment
by Shuying Xu, Jiale Hao, Chunyan Ye, Xintong Li, Pengcheng Gao, Ni Song, Chanjuan Liu, Youjing Lv, Guangli Yu and Guoyun Li
Mar. Drugs 2025, 23(4), 177; https://doi.org/10.3390/md23040177 - 20 Apr 2025
Viewed by 113
Abstract
β-glucan, a promising drug candidate for immuno-antitumor therapy, holds tremendous potential for clinical applications. However, the absence of highly sensitive quantitative methods for polysaccharides, attributed to their complicated chemical structures and susceptibility to endogenous interference, has posed significant challenges for their clinical development. [...] Read more.
β-glucan, a promising drug candidate for immuno-antitumor therapy, holds tremendous potential for clinical applications. However, the absence of highly sensitive quantitative methods for polysaccharides, attributed to their complicated chemical structures and susceptibility to endogenous interference, has posed significant challenges for their clinical development. Here, we report a highly sensitive and reliable analytical strategy for quantifying β-1, 3/1, 6-glucan derived from Durvillaea antarctica (BG136) in various biological matrices. This approach integrates targeted depolymerization and derivatization, followed by oligosaccharide isomer fingerprinting using ultra-high-performance liquid chromatography-triple quadrupole tandem mass spectrometry (UHPLC-MS/MS). The absolute quantification of BG136 relied on the abundance of the structure-specific trisaccharide (Glc-β1, 6-Glc-β1, 3-Glc) generated. This methodology not only facilitates prototype-based BG136 administration but also exhibits remarkable sensitivity. Following method optimization and validation, we successfully explored the in vivo fate of BG136 across multiple models, including cellular uptake and release kinetics, as well as preclinical and clinical pharmacokinetics. These achievements provide insight into the “black box” of BG136 from administration to elimination in vivo. This work marks the first practical application of this strategy in complex biological matrices, offering methodological support for the successful execution of the BG136 Phase I clinical trial. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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14 pages, 2462 KiB  
Article
Fucosylated Glycosaminoglycan Oligosaccharide HS14, Derived from Sea Cucumbers, Is a Novel Inhibitor of Platelet Toll-like Receptor 2
by Huifang Sun, Guangyu Zhu, Sujuan Li, Pengfei Li, Jiali Zhang, Ronghua Yin, Lin Yuan, Na Gao and Jinhua Zhao
Mar. Drugs 2025, 23(3), 110; https://doi.org/10.3390/md23030110 - 4 Mar 2025
Viewed by 670
Abstract
(1) Background: Toll-like receptor 2 (TLR2) on platelets is increasingly recognized as a pivotal mediator in infection-induced platelet activation and aggregation, contributing to both inflammatory and thrombotic diseases. Targeting TLR2 on platelets offers a promising therapeutic strategy for inflammatory and thrombotic-related disorders. However, [...] Read more.
(1) Background: Toll-like receptor 2 (TLR2) on platelets is increasingly recognized as a pivotal mediator in infection-induced platelet activation and aggregation, contributing to both inflammatory and thrombotic diseases. Targeting TLR2 on platelets offers a promising therapeutic strategy for inflammatory and thrombotic-related disorders. However, inhibitors targeting platelet TLR2 have not yet been reported. (2) Methods: Platelet aggregation was assessed using a light transmission aggregometer. Platelet activation was evaluated by measuring the release of P-selectin and von Willebrand factor (vWF) via ELISA. Intracellular Ca2+ mobilization was quantified using Fluo 3-AM fluorescence, recorded by flow cytometry. Static platelet adhesion was visualized under a microscope, and the formation of platelet–granulocyte aggregates in human whole blood was analyzed by flow cytometry. (3) Results: Fucosylated glycosaminoglycan (FG) tetradecasaccharide HS14 inhibited the activation and aggregation of human platelets induced by the synthetic bacterial lipopeptide Pam3CSK4 in a concentration-dependent manner. This inhibitory effect gives rise to significant anti-inflammatory and anti-thrombotic activities, as evidenced by reduced platelet adhesion and decreased platelet–granulocyte aggregates formation in human whole blood. (4) Conclusions: This study is the first to identify FG oligosaccharide HS14 as a promising inhibitor of platelet TLR2/TLR1, demonstrating significant therapeutic potential for inflammatory and thrombotic-related diseases. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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13 pages, 7126 KiB  
Article
Selenium–Chondroitin Sulfate Nanoparticles Inhibit Angiogenesis by Regulating the VEGFR2-Mediated PI3K/Akt Pathway
by Xia Zheng, Xiaofei Liu, Zhuo Wang, Rui Li, Qiaoli Zhao, Bingbing Song, Kit-Leong Cheong, Jianping Chen and Saiyi Zhong
Mar. Drugs 2025, 23(1), 22; https://doi.org/10.3390/md23010022 - 2 Jan 2025
Viewed by 1235
Abstract
Chondroitin sulfate (CS), a class of glycosaminoglycans covalently attached to proteins to form proteoglycans, is widely distributed in the extracellular matrix and cell surface of animal tissues. In our previous study, CS was used as a template for the synthesis of seleno-chondroitin sulfate [...] Read more.
Chondroitin sulfate (CS), a class of glycosaminoglycans covalently attached to proteins to form proteoglycans, is widely distributed in the extracellular matrix and cell surface of animal tissues. In our previous study, CS was used as a template for the synthesis of seleno-chondroitin sulfate (SeCS) through the redox reaction of ascorbic acid (Vc) and sodium selenite (Na2SeO3) and we found that SeCS could inhibit tumor cell proliferation and invasion. However, its effect on angiogenesis and its underlying mechanism are unknown. In this study, we analyzed the effect of SeCS on tube formation in vitro, based on the inhibition of tube formation and migration of human umbilical vein endothelial cells (HUVECs), and evaluated the in vivo angiogenic effect of SeCS using the chick embryo chorioallantoic membrane (CAM) assay. The results showed that SeCS significantly inhibited the angiogenesis of chicken embryo urothelium. Further mechanism analysis showed that SeCS had a strong inhibitory effect on VEGFR2 expression and its downstream PI3K/Akt signaling pathway, which contributed to its anti-angiogenic effects. In summary, SeCS showed good anti-angiogenic effects in an HUVEC cell model and a CAM model, suggesting that it may be a potential angiogenesis inhibitor. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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15 pages, 9352 KiB  
Article
Therapeutic Potential of Oligo-Fucoidan in Mitigating Peritoneal Dialysis-Associated Fibrosis
by Yu-Wei Chen, Mei-Yi Wu, Nai-Jen Huang, Mai-Szu Wu, Yung-Ho Hsu, Chia-Te Liao and Cheng-Hsien Chen
Mar. Drugs 2024, 22(12), 529; https://doi.org/10.3390/md22120529 - 25 Nov 2024
Viewed by 1330
Abstract
Peritoneal dialysis (PD) serves as a home-based kidney replacement therapy with increasing utilization across the globe. However, long-term use of high-glucose-based PD solution incites repeated peritoneal injury and inevitable peritoneal fibrosis, thus compromising treatment efficacy and resulting in ultrafiltration failure eventually. In the [...] Read more.
Peritoneal dialysis (PD) serves as a home-based kidney replacement therapy with increasing utilization across the globe. However, long-term use of high-glucose-based PD solution incites repeated peritoneal injury and inevitable peritoneal fibrosis, thus compromising treatment efficacy and resulting in ultrafiltration failure eventually. In the present study, we utilized human mesothelial MeT-5A cells for the in vitro experiments and a PD mouse model for in vivo validation to study the pathophysiological mechanisms underneath PD-associated peritoneal fibrosis. High-glucose PD solution (Dianeal 4.25%, Baxter) increased protein expression of mesothelial–mesenchymal transition (MMT) markers, such as N-cadherin and α-SMA in MeT-5A cells, whereas it decreased catalase expression and stimulated the production of reactive oxygen species (ROS). Furthermore, macrophage influx and increased serum pro-inflammatory cytokines, such as IL-1β, MCP-1, and TNF-α, were observed in the PD mouse model. Interestingly, we discovered that oligo-fucoidan, an oligosaccharide extract from brown seaweed, successfully prevented PD-associated peritoneal thickening and fibrosis through antioxidant effect, downregulation of MMT markers, and attenuation of peritoneal and systemic inflammation. Hence, oligo-fucoidan has the potential to be developed into a novel preventive strategy for PD-associated peritoneal fibrosis. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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20 pages, 7887 KiB  
Article
Degradation of Natural Undaria pinnatifida into Unsaturated Guluronic Acid Oligosaccharides by a Single Alginate Lyase
by Hui Wang, Jiaqi Wen, Nuraliya Ablimit, Kun Deng, Wenzhuo Wang and Wei Jiang
Mar. Drugs 2024, 22(10), 453; https://doi.org/10.3390/md22100453 - 2 Oct 2024
Cited by 1 | Viewed by 1695
Abstract
Here, we report on a bifunctional alginate lyase (Vnalg7) expressed in Pichia pastoris, which can degrade natural Undaria pinnatifida into unsaturated guluronic acid di- and trisaccharide without pretreatment. The enzyme activity of Vnalg7 (3620.00 U/mL-culture) was 15.81-fold higher than that of the [...] Read more.
Here, we report on a bifunctional alginate lyase (Vnalg7) expressed in Pichia pastoris, which can degrade natural Undaria pinnatifida into unsaturated guluronic acid di- and trisaccharide without pretreatment. The enzyme activity of Vnalg7 (3620.00 U/mL-culture) was 15.81-fold higher than that of the original alg (228.90 U/mL-culture), following engineering modification. The degradation rate reached 52.75%, and reducing sugar reached 30.30 mg/mL after combining Vnalg7 (200.00 U/mL-culture) and 14% (w/v) U. pinnatifida for 6 h. Analysis of the action mode indicated that Vnalg7 could degrade many substrates to produce a variety of unsaturated alginate oligosaccharides (AOSs), and the minimal substrate was tetrasaccharide. Site-directed mutagenesis showed that Glu238, Glu241, Glu312, Arg236, His307, Lys414, and Tyr418 are essential catalytic sites, while Glu334, Glu344, and Asp311 play auxiliary roles. Mechanism analysis revealed the enzymatic degradation pattern of Vnalg7, which mainly recognizes and attacks the third glycosidic linkage from the reducing end of oligosaccharide substrate. Our findings provide a novel alginate lyase tool and a sustainable and commercial production strategy for value-added biomolecules using seaweeds. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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Review

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33 pages, 2638 KiB  
Review
Marine Algae Polysaccharides: An Overview of Characterization Techniques for Structural and Molecular Elucidation
by Kaitlin C. Lesco, S. Kim R. Williams and Lieve M. L. Laurens
Mar. Drugs 2025, 23(3), 105; https://doi.org/10.3390/md23030105 - 27 Feb 2025
Cited by 2 | Viewed by 1305
Abstract
Polysaccharides make up a large portion of the organic material from and in marine organisms. However, their structural characterization is often overlooked due to their complexity. With many high-value applications and unique bioactivities resulting from the polysaccharides’ complex and heterogeneous structures, dedicated analytical [...] Read more.
Polysaccharides make up a large portion of the organic material from and in marine organisms. However, their structural characterization is often overlooked due to their complexity. With many high-value applications and unique bioactivities resulting from the polysaccharides’ complex and heterogeneous structures, dedicated analytical efforts become important to achieve structural elucidation. Because algae represent the largest marine resource of polysaccharides, the majority of the discussion is focused on well-known algae-based hydrocolloid polymers. The native environment of marine polysaccharides presents challenges to many conventional analytical techniques necessitating novel methodologies. We aim to deliver a review of the current state of the art in polysaccharide characterization, focused on capabilities as well as limitations in the context of marine environments. This review covers the extraction and isolation of marine polysaccharides, in addition to characterizations from monosaccharides to secondary and tertiary structures, highlighting a suite of analytical techniques. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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36 pages, 4076 KiB  
Review
A Comparative Review of Alternative Fucoidan Extraction Techniques from Seaweed
by Matthew Chadwick, Loïc G. Carvalho, Carlos Vanegas and Simone Dimartino
Mar. Drugs 2025, 23(1), 27; https://doi.org/10.3390/md23010027 - 7 Jan 2025
Cited by 1 | Viewed by 3080
Abstract
Fucoidan is a sulfated polysaccharide found in brown seaweed. Due to its reported biological activities, including antiviral, antibacterial and anti-inflammatory activities, it has garnered significant attention for potential biomedical applications. However, the direct relationship between fucoidan extracts’ chemical structures and bioactivities is unclear, [...] Read more.
Fucoidan is a sulfated polysaccharide found in brown seaweed. Due to its reported biological activities, including antiviral, antibacterial and anti-inflammatory activities, it has garnered significant attention for potential biomedical applications. However, the direct relationship between fucoidan extracts’ chemical structures and bioactivities is unclear, making it extremely challenging to predict whether an extract will possess a given bioactivity. This relationship is further complicated by a lack of uniformity in the recent literature in terms of the assessment and reporting of extract properties, yield and chemical composition (e.g., sulfate, fucose, uronic acid and monosaccharide contents). These inconsistencies pose significant challenges when directly comparing extraction techniques across studies. This review collected data on extract contents and properties from a selection of available studies. Where information was unavailable directly, efforts were made to extrapolate data. This approach enabled a comprehensive examination of the correlation between extraction techniques and the characteristics of the resulting extracts. A holistic framework is presented for the selection of fucoidan extraction methods, outlining key heuristics to consider when capturing the broader context of a seaweed bioprocess. Future work should focus on developing knowledge within these heuristic categories, such as the creation of technoeconomic models of each extraction process. This framework should allow for a robust extraction selection process that integrates process scale, cost and constraints into decision making. Key quality attributes for biologically active fucoidan are proposed, and areas for future research are identified, such as studies for specific bioactivities aimed at elucidating fucoidan’s mechanism of action. This review also sets out future work required to standardize the reporting of fucoidan extract data. Standardization could positively enhance the quality and depth of data on fucoidan extracts, enabling the relationships between physical, chemical and bioactive properties to be identified. Recommendations on best practices for the production of high-quality fucoidan with desirable yield, characteristics and bioactivity are highlighted. Full article
(This article belongs to the Special Issue Marine Polysaccharides and Oligosaccharides: Extraction and Biological Activities)
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