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A biocompatible, heterogeneous, fucose-rich, sulfated polysaccharide (fucoidan) is biosynthesized in brown seaweed. In this study, fucoidan was isolated from Padina arborescens (PAC) using celluclast-assisted extraction, purified, and evaluated for its anti-inflammatory potential in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Structural analyses were performed using Fourier transform infrared (FTIR) and scanning electron microscopy. Among the purified fucoidans, fucoidan fraction 5 (F5) exhibited strong inhibitory activity against LPS-induced nitric oxide (NO) production and pro-inflammatory cytokine generation through the regulation of iNOS/COX-2, MAPK, and NF-κB signaling in LPS-induced RAW 264.7 cells. Determination of the structural characteristics indicated that purified F5 exhibited characteristics similar to those of commercial fucoidan. In addition, further analyses suggested that F5 inhibits LPS-induced toxicity, cell death, and NO generation in zebrafish models. Taken together, these findings imply that P. arborescens fucoidans have exceptional anti-inflammatory action, both in vitro and in vivo, and that they may have prospective uses in the functional food sector.
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Lipopolisacáridos , Phaeophyceae , Animales , Pez Cebra , Polisacáridos , Inflamación , Óxido NítricoRESUMEN
Muscle atrophy is a detrimental and injurious condition that leads to reduced skeletal muscle mass and disruption of protein metabolism. Oyster (Crassostrea nippona) is a famous and commonly consumed shellfish in East Asia and has become a popular dietary choice worldwide. The current investigation evaluated the efficacy of C. nippona against muscle atrophy, which has become a severe health issue. Mammalian skeletal muscles are primarily responsible for efficient metabolism, energy consumption, and body movements. The proteins that regulate muscle hypertrophy and atrophy are involved in muscle growth. C. nippona extracts were enzymatically hydrolyzed using alcalase (AOH), flavourzyme (FOH), and protamex (POH) to evaluate their efficacy in mitigating dexamethasone-induced muscle damage in C2C12 cells in vitro. AOH exhibited notable cell proliferative abilities, promoting dose-dependent myotube formation. These results were further solidified by protein expression analysis. Western blot and gene expression analysis via RT-qPCR demonstrated that AOH downregulated MuRF-1, Atrogin, Smad 2/3, and Foxo-3a, while upregulating myogenin, MyoD, myosin heavy chain expression, and mTOR, key components of the ubiquitin-proteasome and mTOR signaling pathways. Finally, this study suggests that AOH holds promise for alleviating dexamethasone-induced muscle atrophy in C2C12 cells in vitro, offering insights for developing functional foods targeting conditions akin to sarcopenia.
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Crassostrea , Animales , Atrofia Muscular , Suplementos Dietéticos , Serina-Treonina Quinasas TOR , Dexametasona , MamíferosRESUMEN
Cardiovascular diseases (CVDs) are responsible for significant mortality rates globally that have been raised due to the limitation of the available treatments and prevalence of CVDs. The innovative research and identification of potential preventives for CVDs are essential to alleviate global deaths and complications. The marine environment is a rich source of bioactive substances and provides a unique chemical arsenal against numerous ailments due to its unrivaled biodiversity. Marine polyphenolic compounds (MPCs) are unique because of their structural variety and biologically significant activity. Further, MPCs are well-reported for their valuable biological activities, such as anti-inflammatory, cardioprotective, and antioxidant, demonstrating encouraging results in preventing and treating CVDs. Therefore, investigation of the structure-activity relationship (SAR) between MPCs and CVDs provides insights that reveal how the structural components of these compounds affect their effectiveness. Further, comprehending this correlation is essential for advancing medications and nutraceuticals sourced from marine sources, which could transform the strategy for treating and preventing cardiovascular diseases. Therefore, this study provides a comprehensive analysis of existing research by emphasizing the role of MPCs in CVD treatments and evaluating the SAR between MPCs and CVDs with challenges and future directions.
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Organismos Acuáticos , Enfermedades Cardiovasculares , Polifenoles , Polifenoles/química , Polifenoles/uso terapéutico , Polifenoles/farmacología , Humanos , Relación Estructura-Actividad , Enfermedades Cardiovasculares/tratamiento farmacológico , Organismos Acuáticos/química , Animales , Antioxidantes/química , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Cardiotónicos/farmacología , Cardiotónicos/uso terapéutico , Cardiotónicos/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/uso terapéuticoRESUMEN
Fish head byproducts derived from surimi processing contribute about 15% of the total body weight, which are beneficial to health because they contain essential nutrients. In this study, olive flounder (OF) was the target species in order to maximize the byproduct utilization. In RAW 264.7 macrophages, the seven hydrolysates from OF head byproducts were examined for their inhibitory potential against inflammation and the oxidative stress induced by lipopolysaccharides (LPS). The pepsin hydrolysate (OFH-PH) demonstrated strong anti-inflammatory activity via the down-regulation of NO production, with an IC50 value of 299.82 ± 4.18 µg/mL. We evaluated the inhibitory potential of pro-inflammatory cytokines and PGE2 to confirm these findings. Additionally, iNOS and COX-2 protein expressions were confirmed using western blotting. Furthermore, the results from the in vivo zebrafish model demonstrated that OFH-PH decreased the LPS-elevated heart rate, NO production, cell death, and intracellular ROS level, while increasing the survival percentage. Hence, the obtained results of this study serve as a platform for future research and provide insight into the mediation of inflammatory disorders. These results suggest that OFH-PH has the potential to be utilized as a nutraceutical and functional food ingredient.
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Lenguado , Perciformes , Animales , Pez Cebra , Lipopolisacáridos/toxicidad , Pepsina A , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Estrés Oxidativo , MacrófagosRESUMEN
The limited availability of treatments for many infectious diseases highlights the need for new treatments, particularly for viral infections. Natural compounds from seaweed are attracting increasing attention for the treatment of various viral diseases, and thousands of novel compounds have been isolated for the development of pharmaceutical products. Seaweed is a rich source of natural bioactive compounds, including polysaccharides. The discovery of algal polysaccharides with antiviral activity has significantly increased in the past few decades. Furthermore, unique polysaccharides isolated from seaweeds, such as carrageenan, alginates, fucoidans, galactans, laminarians, and ulvans, have been shown to act against viral infections. The antiviral mechanisms of these agents are based on their inhibition of DNA or RNA synthesis, viral entry, and viral replication. In this article, we review and provide an inclusive description of the antiviral activities of algal polysaccharides. Additionally, we discuss the challenges and opportunities for developing polysaccharide-based antiviral therapies, including issues related to drug delivery and formulation. Finally, this review highlights the need for further research for fully understanding the potential of seaweed polysaccharides as a source of antiviral agents and for developing effective treatments for viral diseases.
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Fucoidans are sulfate-rich polysaccharides with a wide variety of beneficial biological activities. The present study aimed to highlight the anti-inflammatory activity of fucoidan from the brown seaweed Sargassum autumnale (SA) against lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells. Among the isolated fucoidan fractions, the third fraction (SAF3) showed a superior protective effect on LPS-stimulated RAW 264.7 cells. SAF3 inhibits nitric oxide (NO) production and expression of prostaglandin E-2 (PGE2) via downregulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX2) expression in LPS-induced RAW 26.7 cells. SAF3 treatment decreased pro-inflammatory cytokines IL-1ß, TNF-α, and IL-6 expression in LPS-induced cells. LPS stimulation activated NF-κB and MAPK signaling cascades in RAW 264.7 cells, while treatment with SAF3 suppressed them in a concentration-dependent manner. Existing outcomes confirm that SAF3 from S. autumnale possesses potent anti-inflammatory activity and exhibits good potential for application as a functional food ingredient or for the treatment of inflammation-related disorders.
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FN-kappa B , Sargassum , Animales , Ratones , FN-kappa B/metabolismo , Lipopolisacáridos/farmacología , Lipopolisacáridos/metabolismo , Sargassum/metabolismo , Polisacáridos/farmacología , Polisacáridos/metabolismo , Macrófagos , Antiinflamatorios/farmacología , Antiinflamatorios/metabolismo , Células RAW 264.7 , Óxido Nítrico Sintasa de Tipo II/metabolismo , Óxido Nítrico/metabolismo , Ciclooxigenasa 2/metabolismoRESUMEN
The skin is the outermost anatomical barrier, which plays a vital role in the maintenance of internal homeostasis and protection against physical, chemical, and biological detractors. Direct contact with various stimuli leads to several physiological changes that are ultimately important for the growth of the cosmetic industry. Due to the consequences of using synthetic compounds in skincare and cosmeceutical-related industries, the pharmaceutical and scientific communities have recently shifted their focus to natural ingredients. The nutrient-rich value of algae, which are some of the most interesting organisms in marine ecosystems, has attracted attention. Secondary metabolites isolated from seaweeds are potential candidates for a wide range of economic applications, including food, pharmaceuticals, and cosmetics. An increasing number of studies have focused on polyphenol compounds owing to their promising biological activities against oxidation, inflammation, allergies, cancers, melanogenesis, aging, and wrinkles. This review summarizes the potential evidence of the beneficial properties and future perspectives of using marine macroalgae-derived polyphenolic compounds for advancing the cosmetic industry.
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Cosméticos , Algas Marinas , Polifenoles/farmacología , Ecosistema , Cosméticos/farmacología , Cosméticos/química , Algas Marinas/química , Sustancias ProtectorasRESUMEN
Brown seaweeds contain fucoidan, which has numerous biological activities. Here, the anti-fine-dust activity of fucoidan extracted from Ecklonia maxima, an abundant brown seaweed from South Africa, was explored. Fourier transmittance infrared spectroscopy, high-performance anion-exchange chromatography with pulsed amperometric detection analysis of the monosaccharide content, and nuclear magnetic resonance were used for the structural characterization of the polysaccharides. The toll-like receptor (TLR)-mediated nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways were evaluated. The results revealed that E. maxima purified leaf fucoidan fraction 7 (EMLF7), which contained the highest sulfate content, showed the best anti-inflammatory activity by attenuating the TLR-mediated NF-κB/MAPK protein expressions in the particulate matter-stimulated cells. This was solidified by the successful reduction of Prostaglandin E2, NO, and pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1ß. The current findings confirm the anti-inflammatory activity of EMLF7, as well as the potential use of E. maxima as a low-cost fucoidan source due to its abundance. This suggests its further application as a functional ingredient in consumer products.
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FN-kappa B , Phaeophyceae , Antiinflamatorios/química , Polvo , Lipopolisacáridos/farmacología , Macrófagos , FN-kappa B/metabolismo , Phaeophyceae/metabolismo , Polisacáridos/química , Transducción de Señal , Receptores Toll-Like/metabolismoRESUMEN
Airborne particulate matter (PM) originating from industrial processes is a major threat to the environment and health in East Asia. PM can cause asthma, collateral lung tissue damage, oxidative stress, allergic reactions, and inflammation. The present study was conducted to evaluate the protective effect of eckmaxol, a phlorotannin isolated from Ecklonia maxima, against PM-induced inflammation in MH-S macrophage cells. It was found that PM induced inflammation in MH-S lung macrophages, which was inhibited by eckmaxol treatment in a dose-dependent manner (21.0−84.12 µM). Eckmaxol attenuated the expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) in PM-induced lung macrophages. Subsequently, nitric oxide (NO), prostaglandin E-2 (PGE-2), and pro-inflammatory cytokines (IL-1ß, IL-6, and TNF-α) were downregulated. PM stimulated inflammation in MH-S lung macrophages by activating Toll-like receptors (TLRs), nuclear factor-kappa B (NF-κB), and mitogen-activated protein kinase (MAPK) pathways. Eckmaxol exhibited anti-inflammatory properties by suppressing the activation of TLRs, downstream signaling of NF-κB (p50 and p65), and MAPK pathways, including c-Jun N-terminal kinase (JNK) and p38. These findings suggest that eckmaxol may offer substantial therapeutic potential in the treatment of inflammatory diseases.
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Inflamación , Pulmón , Macrófagos , Material Particulado , Phaeophyceae , Neumonía , Polifenoles , Humanos , Ciclooxigenasa 2/metabolismo , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Pulmón/efectos de los fármacos , Pulmón/patología , Macrófagos/efectos de los fármacos , Proteínas Quinasas Activadas por Mitógenos/metabolismo , FN-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Material Particulado/toxicidad , Phaeophyceae/química , Receptores Toll-Like/metabolismo , Polifenoles/química , Polifenoles/farmacología , Polifenoles/uso terapéutico , Neumonía/inducido químicamente , Neumonía/tratamiento farmacológicoRESUMEN
A global health concern has emerged as a response to the recent SARS-CoV-2 pandemic. The identification and inhibition of drug targets of SARS-CoV-2 is a decisive obligation of scientists. In addition to the cell entry mechanism, SARS-CoV-2 expresses a complicated replication mechanism that provides excellent drug targets. Papain-like protease (PLpro) and 3-chymotrypsin-like protease (3CLpro) play a vital role in polyprotein processing, producing functional non-structural proteins essential for viral replication and survival in the host cell. Moreover, PLpro is employed by SARS-CoV-2 for reversing host immune responses. Therefore, if some particular compound has the potential to interfere with the proteolytic activities of 3CLpro and PLpro of SARS-CoV-2, it may be effective as a treatment or prophylaxis for COVID-19, reducing viral load, and reinstating innate immune responses. Thus, the present study aims to inhibit SARS-CoV-2 through 3CLpro and PLpro using marine natural products isolated from marine algae that contain numerous beneficial biological activities. Molecular docking analysis was utilized in the present study for the initial screening of selected natural products depending on their 3CLpro and PLpro structures. Based on this approach, Ishophloroglucin A (IPA), Dieckol, Eckmaxol, and Diphlorethohydroxycarmalol (DPHC) were isolated and used to perform in vitro evaluations. IPA presented remarkable inhibitory activity against interesting drug targets. Moreover, Dieckol, Eckmaxol, and DPHC also expressed significant potential as inhibitors. Finally, the results of the present study confirm the potential of IPA, Dieckol, Eckmaxol, and DPHC as inhibitors of SARS-CoV-2. To the best of our knowledge, this is the first study that assesses the use of marine natural products as a multifactorial approach against 3CLpro and PLpro of SARS-CoV-2.
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Antivirales , COVID-19 , Polifenoles , SARS-CoV-2 , Replicación Viral , Humanos , Antivirales/química , Antivirales/aislamiento & purificación , Antivirales/farmacología , COVID-19/prevención & control , Simulación del Acoplamiento Molecular , SARS-CoV-2/efectos de los fármacos , SARS-CoV-2/fisiología , Replicación Viral/efectos de los fármacos , Polifenoles/química , Polifenoles/aislamiento & purificación , Polifenoles/farmacologíaRESUMEN
A novel coronavirus, known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has surfaced and caused global concern owing to its ferocity. SARS-CoV-2 is the causative agent of coronavirus disease 2019; however, it was only discovered at the end of the year and was considered a pandemic by the World Health Organization. Therefore, the development of novel potent inhibitors against SARS-CoV-2 and future outbreaks is urgently required. Numerous naturally occurring bioactive substances have been studied in the clinical setting for diverse disorders. The intricate infection and replication mechanism of SARS-CoV-2 offers diverse therapeutic drug targets for developing antiviral medicines by employing natural products that are safer than synthetic compounds. Marine natural products (MNPs) have received increased attention in the development of novel drugs owing to their high diversity and availability. Therefore, this review article investigates the infection and replication mechanisms, including the function of the SARS-CoV-2 genome and structure. Furthermore, we highlighted anti-SARS-CoV-2 therapeutic intervention efforts utilizing MNPs and predicted SARS-CoV-2 inhibitor design. Supplementary Information: The online version contains supplementary material available at 10.1007/s42995-023-00215-9.
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Inflammatory bowel disease (IBD) is a prominent global public health issue. Anti-inflammatory medications, immunosuppressants, and biological therapies are currently used as treatments. However, they are often unsuccessful and have negative consequences on human health. Thus, there is a tremendous demand for using natural substances, such as seaweed polysaccharides, to treat IBD's main pathologic treatment targets. The cell walls of marine algae are rich in sulfated polysaccharides, including carrageenan in red algae, ulvan in green algae, and fucoidan in brown algae. These are effective candidates for drug development and functional nutrition products. Algal polysaccharides treat IBD through therapeutic targets, including inflammatory cytokines, adhesion molecules, intestinal epithelial cells, and intestinal microflora. This study aimed to systematically review the potential therapeutic effects of algal polysaccharides on IBD while providing the theoretical basis for a nutritional preventive mechanism for IBD and the restoration of intestinal health. The results suggest that algal polysaccharides have significant potential in complementary IBD therapy and further research is needed for fully understanding their mechanisms of action and potential clinical applications.
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In this study, seahorse peptide (SHP) was isolated from an alcalase-treated hydrolysate from Hippocampus abdominalis and assessed for its antioxidant potential against AAPH-induced oxidative stress damage. AAPH stimulation significantly decreased cell viability and increased intracellular reactive oxygen species (ROS) production in Vero cells. SHP treatment increased cell viability and remarkably lowered ROS production under AAPH-induced oxidative stress. Furthermore, it protected against AAPH-induced apoptotic DNA damage. Western blot analysis demonstrated that SHP treatment remarkably increased the protein expression levels of catalase and SOD in AAPH-induced Vero cells. A zebrafish study revealed that SHP-treated zebrafish embryos resulted in lower cell death, ROS generation, and lipid peroxidation than the AAPH-treated group. These results suggest that SHP is a potent functional antioxidant that could be developed as a natural antioxidant in the food and functional food industries.
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Antioxidantes , Smegmamorpha , Animales , Chlorocebus aethiops , Antioxidantes/farmacología , Antioxidantes/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Pez Cebra/genética , Pez Cebra/metabolismo , Células Vero , Smegmamorpha/genética , Smegmamorpha/metabolismo , Estrés Oxidativo , Péptidos/farmacología , Péptidos/metabolismoRESUMEN
Inflammation is a complex host-protective response against harmful stimuli involving macrophage activation that results in secretion of inflammatory mediators, like nitric oxide (NO), pro-inflammatory cytokines, and prostaglandin E2 (PGE2). In this study, we evaluated fucoidan isolated using Viscozyme-assisted enzymatic extraction of Sargassum coreanum extract against lipopolysaccharide (LPS)-stimulated inflammation in RAW 264.7 macrophages and zebrafish model. Among the fucoidan fractions isolated using ion exchange chromatography, SCVF5 showed the highest sulfate and fucose contents based on chemical composition and monosaccharide analysis. Fourier-transform infrared (FT-IR) spectroscopy confirmed the presence of sulfate esters by the stretching vibrations of the SO peak at 1240 cm-1. SCVF5 showed anti-inflammatory effects by inhibiting NO and PGE2 generation in LPS-stimulated RAW 264.7 macrophages by downregulating inducible NO synthase and cyclooxygenase-2 expression. Treatment with SCVF5 suppressed pro-inflammatory cytokine production, such as TNF-α, (IL)-1ß, and IL-6 by modulating the nuclear factor-kappa B signaling cascade in LPS-induced RAW 264.7 cells. Furthermore, in vivo results showed that SCVF5 can potentially downregulate LPS-induced toxicity, cell death, and NO production in LPS-induced zebrafish model. Collectively, these results suggest that S. coreanum fucoidan has remarkable anti-inflammatory activity in vitro and in vivo and may have potential applications in the functional food, cosmetic, and pharmaceutical industries.
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FN-kappa B , Sargassum , Ratones , Animales , FN-kappa B/metabolismo , Lipopolisacáridos/farmacología , Pez Cebra/metabolismo , Sargassum/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Células RAW 264.7 , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Dinoprostona/metabolismo , Óxido Nítrico/metabolismo , Sulfatos/uso terapéuticoRESUMEN
In this study, we investigated the potential antioxidant abilities of low-molecular weight fucoidans from enzyme-assisted hydrolysates of Sargassum autumnale, based on molecular weight changes, in vitro and in vivo. The yield and free radical-scavenging activities of enzyme-assisted hydrolysates of S. autumnale were screened. The protamex-assisted hydrolysate of S. autumnale (SAP) presented the highest yield and 2,2-diphenyl-1-picrylhydrazyl (DPPH)-scavenging activity; therefore, it was chosen for fucoidan purification. Three fucoidan fractions were observed in SAP, and their antioxidant activity was assessed. Fucoidan fraction 3 of protamex-assisted hydrolysate of S. autumnale (SAPF3) offered significant protection against H2O2-induced oxidative stress, and was structurally and physically similar to commercial fucoidan. Fucose and low-molecular weight fucoidans were highly concentrated in SAPF3. The results of our study show that SAPF3, a low-molecular weight fucoidan from S. autumnale, possesses strong antioxidant properties and may be an effective alternative to antioxidant agents in the functional food industry.
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Sargassum , Animales , Antioxidantes/química , Peróxido de Hidrógeno/farmacología , Peso Molecular , Estrés Oxidativo , Polisacáridos/química , Sargassum/química , Pez CebraRESUMEN
The increasing airborne particulate matter (PM) consisting of environmental contaminants such as dust, aerosols, and fibers has become a global concern by causing oxidative stress that leads to apoptosis and skin damage. The current study evaluated the protective effect of Caulerpa racemosa (CR) against PM-induced skin damage using human keratinocytes and a zebrafish model. The clionasterol-rich hexane fraction (CRHF2) of CR exhibited superior protective activity through downregulating intracellular reactive oxygen species levels and mitochondrial ROS levels, as well as the PM-induced increase in apoptotic body formation and upregulation of apoptotic signaling pathway proteins, along with sub-G1 cell accumulation dose-dependently. Furthermore, in vivo results showed that CRHF2 potentially downregulates PM-induced cell death, ROS, and NO production in the zebrafish model. Hence, the results evidenced that the protective effect of CRHF2 is caused by inhibiting oxidative stress and mitochondrial-mediated apoptosis in cells. Therefore, C. racemosa has the potential to be used in the development of pharmaceuticals to attenuate PM-induced skin diseases.
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Sargassum horneri (SH), a marine brown alga, is known to contain a variety of bioactive ingredients and previous studies reported sulfated polysaccharides in SH as a potential candidate for a functional ingredient. However, immune-enhancing activity combined with Lactobacillus plantarum (LAB) is not yet studied. In the present study, we attempted to characterize sulfated polysaccharides (SHCPs) in SH by MALDI-TOF/TOF mass spectrometry and evaluate their immune-enhancing effect on macrophage cells. The main residue of SHCPs in SH is 2-sulfated 1,4-linked L-fucose and this epitope combined with LAB shows immune enhancement properties through cytokine production at the cellular level and increases the population of lymphocytes and myelomonocytes in the adult zebrafish kidney. These results indicate that SHCPs, along with LAB, have potent immune-enhancing activity and may be utilized as a potential immunomodulatory ingredient.