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Marine Drugs
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Fucoidans: Structures-Based Bioactivities
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Fucoidans: Structures-Based Bioactivities

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Structural Studies on Marine Natural Products".

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 20664

Special Issue Editors

Prof. Dr. You-Jin Jeon

E-Mail Website
Guest Editor
1. Department of Marine Life Sciences, Jeju National University, Jeju 63243, Republic of Korea
2. Marine Science Institute, Jeju National University, Jeju 63333, Republic of Korea
Interests: polysaccharides, fucoidans, carrageenans, ulvans, agars, alginic acids, chitins and chitosans, chondroitin sulfates, glucosaminoglycans, marine organism; prevention or improvement of disorders; functionalities, bioactivities, bioavailabilities
Special Issues, Collections and Topics in MDPI journals
Dr. Xiaoting Fu

E-Mail Website
Guest Editor
College of Food Science and Engineering, Ocean University of China, Qingdao 266000, China
Interests: polysaccharides from marine algae; nutritional analysis of marine algae

Special Issue Information

Dear Colleagues,

Fucoidans are a group of fucose-containing sulfated polysaccharides found in many species of brown seaweed. Fucoidans are highly bioactive seaweed substances with different structures. It is well known that the bioactivities of fucoidans largely depend on the contents of fucose and sulfate on the polysaccharide backbone structure. In addition, the molecular weight and mono-sugar composition are also important in the expression of fucoidans’ bioactivities. In industrial applications, yield and extraction efficiency are also essential. Currently, however, further studies on the relationship between structure and bioactivity are critical to understand the functions and activities of fucoidans.

This Special Issue is focused on the different bioactivities expressed by structures, including not only the basic composition but also the linkages of sugars and sulfate groups bound on the backbone, and their applications in functional and healthy foods, medicine, and cosmeceuticals.

As the Guest Editors, we invite authors to contribute their latest research focused on structure-based bioactivities, in in vitro, ex vivo and in vivo experiments.

Prof. Dr. You-Jin Jeon
Dr. Xiaoting Fu
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

  • fucoidan
  • seaweeds
  • bioactivities
  • fucose
  • sulfate
  • structures
  • linkage

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Published Papers (7 papers)

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Research

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17 pages, 2593 KiB  
Article
Anti-Inflammatory Activity of Fucan from Spatoglossum schröederi in a Murine Model of Generalized Inflammation Induced by Zymosan
by Ana Katarina Andrade Silva, Cássio Ricardo de Medeiros Souza, Hylarina Montenegro Diniz Silva, Jéssica Teixeira Jales, Lucas Alves de Souza Gomez, Ericka Janine Dantas da Silveira, Hugo Alexandre Oliveira Rocha and Janeusa Trindade Souto
Mar. Drugs 2023, 21(11), 557; https://doi.org/10.3390/md21110557 - 26 Oct 2023
Cited by 2 | Viewed by 1702
Abstract
Fucans from marine algae have been the object of many studies that demonstrated a broad spectrum of biological activities, including anti-inflammatory effects. The aim of this study was to verify the protective effects of a fucan extracted from the brown algae Spatoglossum schröederi [...] Read more.
Fucans from marine algae have been the object of many studies that demonstrated a broad spectrum of biological activities, including anti-inflammatory effects. The aim of this study was to verify the protective effects of a fucan extracted from the brown algae Spatoglossum schröederi in animals submitted to a generalized inflammation model induced by zymosan (ZIGI). BALB/c mice were first submitted to zymosan-induced peritonitis to evaluate the treatment dose capable of inhibiting the induced cellular migration in a simple model of inflammation. Mice were treated by the intravenous route with three doses (20, 10, and 5 mg/kg) of our fucan and, 1 h later, were inoculated with an intraperitoneal dose of zymosan (40 mg/kg). Peritoneal exudate was collected 24 h later for the evaluation of leukocyte migration. Doses of the fucan of Spatoglossum schröederi at 20 and 10 mg/kg reduced peritoneal cellular migration and were selected to perform ZIGI experiments. In the ZIGI model, treatment was administered 1 h before and 6 h after the zymosan inoculation (500 mg/kg). Treatments and challenges were administered via intravenous and intraperitoneal routes, respectively. Systemic toxicity was assessed 6 h after inoculation, based on three clinical signs (bristly hair, prostration, and diarrhea). The peritoneal exudate was collected to assess cellular migration and IL-6 levels, while blood samples were collected to determine IL-6, ALT, and AST levels. Liver tissue was collected for histopathological analysis. In another experimental series, weight loss was evaluated for 15 days after zymosan inoculation and fucan treatment. The fucan treatment did not present any effect on ZIGI systemic toxicity; however, a fucan dose of 20 mg/kg was capable of reducing the weight loss in treated mice. The treatment with both doses also reduced the cellular migration and reduced IL-6 levels in peritoneal exudate and serum in doses of 20 and 10 mg/kg, respectively. They also presented a protective effect in the liver, with a reduction in hepatic transaminase levels in both doses of treatment and attenuated histological damage in the liver at a dose of 10 mg/kg. Fucan from S. schröederi presented a promising pharmacological activity upon the murine model of ZIGI, with potential anti-inflammatory and hepatic protective effects, and should be the target of profound and elucidative studies. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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16 pages, 2876 KiB  
Article
The Anti-Inflammatory Effect of Low Molecular Weight Fucoidan from Sargassum siliquastrum in Lipopolysaccharide-Stimulated RAW 264.7 Macrophages via Inhibiting NF-κB/MAPK Signaling Pathways
by Arachchige Maheshika Kumari Jayasinghe, Kirinde Gedara Isuru Sandanuwan Kirindage, Ilekuttige Priyan Shanura Fernando, Kil-Nam Kim, Jae-Young Oh and Ginnae Ahn
Mar. Drugs 2023, 21(6), 347; https://doi.org/10.3390/md21060347 - 4 Jun 2023
Cited by 13 | Viewed by 2460
Abstract
Brown seaweed is a rich source of fucoidan, which exhibits a variety of biological activities. The present study discloses the protective effect of low molecular weight fucoidan (FSSQ) isolated from an edible brown alga, Sargassum siliquastrum, on lipopolysaccharide (LPS)-stimulated inflammatory responses in RAW [...] Read more.
Brown seaweed is a rich source of fucoidan, which exhibits a variety of biological activities. The present study discloses the protective effect of low molecular weight fucoidan (FSSQ) isolated from an edible brown alga, Sargassum siliquastrum, on lipopolysaccharide (LPS)-stimulated inflammatory responses in RAW 264.7 macrophages. The findings of the study revealed that FSSQ increases cell viability while decreasing intracellular reactive oxygen species production in LPS-stimulated RAW 264.7 macrophages dose-dependently. FSSQ reduced the iNOS and COX-2 expression, inhibiting the NO and prostaglandin E2 production. Furthermore, mRNA expression of IL-1β, IL-6, and TNF-α was downregulated by FSSQ via modulating MAPK and NF-κB signaling. The NLRP3 inflammasome protein complex, including NLRP3, ASC, and caspase-1, as well as the subsequent release of pro-inflammatory cytokines, such as IL-1β and IL-18, release in LPS-stimulated RAW 264.7 macrophages was inhibited by FSSQ. The cytoprotective effect of FSSQ is indicated via Nrf2/HO-1 signaling activation, which is considerably reduced upon suppression of HO-1 activity by ZnPP. Collectively, the study revealed the therapeutic potential of FSSQ against inflammatory responses in LPS-stimulated RAW 264.7 macrophages. Moreover, the study suggests further investigations on commercially viable methods for fucoidan isolation. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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18 pages, 7490 KiB  
Article
Fine-Dust-Induced Skin Inflammation: Low-Molecular-Weight Fucoidan Protects Keratinocytes and Underlying Fibroblasts in an Integrated Culture Model
by Kirinde Gedara Isuru Sandanuwan Kirindage, Arachchige Maheshika Kumari Jayasinghe, Namki Cho, Seok Ho Cho, Hee Min Yoo, Ilekuttige Priyan Shanura Fernando and Ginnae Ahn
Mar. Drugs 2023, 21(1), 12; https://doi.org/10.3390/md21010012 - 23 Dec 2022
Cited by 10 | Viewed by 2486
Abstract
Prolonged exposure to fine dust (FD) increases the risk of skin inflammation. Stimulated epidermal cells release growth factors into their extracellular environment, which can induce inflammation in dermal cells. Algae are considered rich sources of bioactive materials. The present study emphasized the effect [...] Read more.
Prolonged exposure to fine dust (FD) increases the risk of skin inflammation. Stimulated epidermal cells release growth factors into their extracellular environment, which can induce inflammation in dermal cells. Algae are considered rich sources of bioactive materials. The present study emphasized the effect of low-molecular-weight fucoidan isolated from Sargassum confusum (LMF) against FD-induced inflammation in HaCaT keratinocytes and underneath fibroblasts (HDFs) in an integrated culture model. HDFs were treated with media from FD-stimulated HaCaT with LMF treatments (preconditioned media). The results suggested that FD increased the oxidative stress in HaCaT, thereby increasing the sub-G1 phase of the cell cycle up to 587%, as revealed via flow cytometric analysis. With preconditioned media, HDFs also displayed oxidative stress; however, the increase in the sub-G1 phase was insignificant compared with HaCaT. LMF dose-dependently regulated the NF-κB/MAPK signaling in HaCaT. Furthermore, significant downregulation in NF-κB/MAPK signaling, as well as inflammatory cytokines, tissue inhibitors of metalloproteinases, matrix metalloproteinases, and reduction in relative elastase and collagenase activities related to the extracellular matrix degeneration were observed in HDFs with a preconditioned media treatment. Therefore, we concluded that HDFs were protected from inflammation by preconditioned media. Continued research on tissue culture and in vivo studies may reveal the therapeutic potential of LMF. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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20 pages, 3644 KiB  
Article
Structural Characterization and In Vivo Anti-Inflammatory Activity of Fucoidan from Cystoseira crinita (Desf.) Borry
by Elisaveta Apostolova, Paolina Lukova, Alexandra Baldzhieva, Cédric Delattre, Roland Molinié, Emmanuel Petit, Redouan Elboutachfaiti, Mariana Nikolova, Ilia Iliev, Marianna Murdjeva and Vesela Kokova
Mar. Drugs 2022, 20(11), 714; https://doi.org/10.3390/md20110714 - 15 Nov 2022
Cited by 21 | Viewed by 2754
Abstract
The aim of this study was to evaluate the effects of fucoidan isolated from C. crinita on histamine-induced paw inflammation in rats, and on the serum levels of TNF-α, IL-1β, IL-6, and IL-10 in rats during systemic inflammation response. The levels of TNF-α [...] Read more.
The aim of this study was to evaluate the effects of fucoidan isolated from C. crinita on histamine-induced paw inflammation in rats, and on the serum levels of TNF-α, IL-1β, IL-6, and IL-10 in rats during systemic inflammation response. The levels of TNF-α in a model of acute peritonitis in rats were also investigated. The isolated crude fucoidan was identified as a sulfated xylogalactofucan with high, medium, and low molecular weight fractions and a content of fucose of 39.74%, xylose of 20.75%, and galactose of 15.51%. Fucoidan from C. crinita showed better anti-inflammatory effects in the rat paw edema model, and this effect was present during all stages of the experiment. When compared to controls, a commercial fucoidan from F. vesiculosus, the results also displayed anti-inflammatory activity on the 60th, 90th, and 120th minute of the experiment. A significant decrease in serum levels of IL-1β in rats treated with both doses of C. crinita fucoidan was observed in comparison to controls, whereas TNF-α concentrations were reduced only in the group treated with fucoidan from C. crinita at the dose of 25 mg/kg bw. In the model of carrageenan-induced peritonitis, we observed a tendency of decrease in the levels of the pro-inflammatory cytokine TNF-α in peritoneal fluid after a single dose of C. crinita fucoidan, but this did not reach the statistical significance margin. Single doses of C. crinita fucoidan did not alter serum levels of the anti-inflammatory cytokine IL-10 in animals with lipopolysaccharide-induced systemic inflammation. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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22 pages, 4202 KiB  
Article
Fucoidan-Incorporated Composite Scaffold Stimulates Osteogenic Differentiation of Mesenchymal Stem Cells for Bone Tissue Engineering
by Yashaswini Devi G.V., Apoorva H Nagendra, Sudheer Shenoy P., Kaushik Chatterjee and Jayachandran Venkatesan
Mar. Drugs 2022, 20(10), 589; https://doi.org/10.3390/md20100589 - 21 Sep 2022
Cited by 11 | Viewed by 2965
Abstract
Globally, millions of bone graft procedures are being performed by clinicians annually to treat the rising prevalence of bone defects. Here, the study designed a fucoidan from Sargassum ilicifolium incorporated in an osteo-inductive scaffold comprising calcium crosslinked sodium alginate-nano hydroxyapatite-nano graphene oxide (Alg-HA-GO-F), [...] Read more.
Globally, millions of bone graft procedures are being performed by clinicians annually to treat the rising prevalence of bone defects. Here, the study designed a fucoidan from Sargassum ilicifolium incorporated in an osteo-inductive scaffold comprising calcium crosslinked sodium alginate-nano hydroxyapatite-nano graphene oxide (Alg-HA-GO-F), which tends to serve as a bone graft substitute. The physiochemical characterization that includes FT-IR, XRD, and TGA confirms the structural integration between the materials. The SEM and AFM reveal highly suitable surface properties, such as porosity and nanoscale roughness. The incorporation of GO enhanced the mechanical strength of the Alg-HA-GO-F. The findings demonstrate the slower degradation and improved protein adsorption in the fucoidan-loaded scaffolds. The slow and sustained release of fucoidan in PBS for 120 h provides the developed system with an added advantage. The apatite formation ability of Alg-HA-GO-F in the SBF solution predicts the scaffold’s osteointegration and bone-bonding capability. In vitro studies using C3H10T1/2 revealed a 1.5X times greater cell proliferation in the fucoidan-loaded scaffold than in the control. Further, the results determined the augmented alkaline phosphatase and mineralization activity. The physical, structural, and enriching osteogenic potential results of Alg-HA-GO-F indicate that it can be a potential bone graft substitute for orthopedic applications. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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18 pages, 3029 KiB  
Article
High Molecular Weight Fucoidan Restores Intestinal Integrity by Regulating Inflammation and Tight Junction Loss Induced by Methylglyoxal-Derived Hydroimidazolone-1
by Jae-Min Lim, Hee Joon Yoo and Kwang-Won Lee
Mar. Drugs 2022, 20(9), 580; https://doi.org/10.3390/md20090580 - 17 Sep 2022
Cited by 9 | Viewed by 2675
Abstract
Fucoidan from brown seaweeds has several biological effects, including preserving intestinal integrity. To investigate the intestinal protective properties of high molecular weight fucoidan (HMWF) from Undaria pinnatifida on intestinal integrity dysfunction caused by methylglyoxal-derived hydroimidazolone-1 (MG-H1), one of the dietary advanced-glycation end products [...] Read more.
Fucoidan from brown seaweeds has several biological effects, including preserving intestinal integrity. To investigate the intestinal protective properties of high molecular weight fucoidan (HMWF) from Undaria pinnatifida on intestinal integrity dysfunction caused by methylglyoxal-derived hydroimidazolone-1 (MG-H1), one of the dietary advanced-glycation end products (dAGEs) in the human-colon carcinoma-cell line (Caco-2) cells and ICR mice. According to research, dAGEs may damage the intestinal barrier by increasing gut permeability. The findings of the study showed that HMWF + MG-H1 treatment reduced by 16.8% the amount of reactive oxygen species generated by MG-H1 treatment alone. Furthermore, HMWF + MGH-1 treatment reduced MG-H1-induced monolayer integrity disruption, as measured by alterations in transepithelial electrical resistance (135% vs. 75.5%) and fluorescein isothiocyanate incorporation (1.40 × 10−6 cm/s vs. 3.80 cm/s). HMWF treatment prevented the MG-H1-induced expression of tight junction markers, including zonula occludens-1, occludin, and claudin-1 in Caco-2 cells and mouse colon tissues at the mRNA and protein level. Also, in Caco-2 and MG-H1-treated mice, HMWF plays an important role in preventing receptor for AGEs (RAGE)-mediated intestinal damage. In addition, HMWF inhibited the nuclear factor kappa B activation and its target genes leading to intestinal inflammation. These findings suggest that HMWF with price competitiveness could play an important role in preventing AGEs-induced intestinal barrier dysfunction. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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Review

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19 pages, 836 KiB  
Review
A Review on Fucoidan Structure, Extraction Techniques, and Its Role as an Immunomodulatory Agent
by Thilina U. Jayawardena, D. P. Nagahawatta, I. P. S. Fernando, Yong-Tae Kim, Jin-Soo Kim, Won-Suk Kim, Jung Suck Lee and You-Jin Jeon
Mar. Drugs 2022, 20(12), 755; https://doi.org/10.3390/md20120755 - 30 Nov 2022
Cited by 43 | Viewed by 4770
Abstract
Functional ingredients for human health have recently become the focus of research. One such potentially versatile therapeutic component is fucose-containing sulfated polysaccharides (FCSPs), referred to as fucoidans. The exploitation of marine brown algae provides a rich source of FCSPs because of their role [...] Read more.
Functional ingredients for human health have recently become the focus of research. One such potentially versatile therapeutic component is fucose-containing sulfated polysaccharides (FCSPs), referred to as fucoidans. The exploitation of marine brown algae provides a rich source of FCSPs because of their role as a structural component of the cell wall. Fucoidans are characterized by a sulfated fucose backbone. However, the structural characterization of FCSPs is impeded by their structural diversity, molecular weight, and complexity. The extraction and purification conditions significantly influence the yield and structural alterations. Inflammation is the preliminary response to potentially injurious inducements, and it is of the utmost importance for modulation in the proper direction. Improper manipulation and/or continuous stimuli could have detrimental effects in the long run. The web of immune responses mediated through multiple modulatory/cell signaling components can be addressed through functional ingredients, benefiting patients with no side effects. In this review, we attempted to address the involvement of FCSPs in the stimulation/downregulation of immune response cell signaling. The structural complexity and its foremost influential factor, extraction techniques, have also attracted attention, with concise details on the structural implications of bioactivity. Full article
(This article belongs to the Special Issue Fucoidans: Structures-Based Bioactivities)
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