Consorzio Interuniversitario Nazionale per la Bio-Oncologia, Italy. A comparative study of the anti-inflammatory, anticoagulant, antiangiogenic, and antiadhesive activities of nine different fucoidans from brown seaweeds

Department of Oncology and Neurosciences, University G. D'Annunzio Medical School & Foundation, 66013 Chieti, Italy, and Division of Immunogenetics, Hospital de Clínicas José de San Martín, Buenos Aires, Argentina.
Glycobiology (Impact Factor: 3.15). 06/2007; 17(5):541-52. DOI: 10.1093/glycob/cwm014
Source: PubMed


The anti-inflammatory, antiangiogenic, anticoagulant, and antiadhesive properties of fucoidans obtained from nine species of brown algae were studied in order to examine the influence of fucoidan origin and composition on their biological activities. All fucoidans inhibited leucocyte recruitment in an inflammation model in rats, and neither the content of fucose and sulfate nor other structural features of their polysaccharide backbones significantly affected the efficacy of fucoidans in this model. In vitro evaluation of P-selectin-mediated neutrophil adhesion to platelets under flow conditions revealed that only polysaccharides from Laminaria saccharina, L. digitata, Fucus evanescens, F. serratus, F. distichus, F. spiralis, and Ascophyllum nodosum could serve as P-selectin inhibitors. All fucoidans, except that from Cladosiphon okamuranus carrying substantial levels of 2-O-alpha-D-glucuronopyranosyl branches in the linear (1-->3)-linked poly-alpha-fucopyranoside chain, exhibited anticoagulant activity as measured by activated partial thromboplastin time whereas only fucoidans from L. saccharina, L. digitata, F. serratus, F. distichus, and F. evanescens displayed strong antithrombin activity in a platelet aggregation test. The last fucoidans potently inhibited human umbilical vein endothelial cell (HUVEC) tubulogenesis in vitro and this property correlated with decreased levels of plasminogen-activator inhibitor-1 in HUVEC supernatants, suggesting a possible mechanism of fucoidan-induced inhibition of tubulogenesis. Finally, fucoidans from L. saccharina, L. digitata, F. serratus, F. distichus, and F. vesiculosus strongly blocked MDA-MB-231 breast carcinoma cell adhesion to platelets, an effect which might have critical implications in tumor metastasis. The data presented herein provide a new rationale for the development of potential drugs for thrombosis, inflammation, and tumor progression.

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Available from: Nikolay E Nifantiev
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    • "It has been reported to have a wide range of physiological and biological activities, such as anti-inflammatory, anticoagulant, anti-tumor, anti-metastatic, and antiangiogenesis activities [18]–[20]. The biological activities and medicinal effect of fucoidan depend greatly on its structural properties, molecular weight, sulfate content, etc. Fucoidans from different algal species and extraction techniques differ from each other [21]–[24]. Fucoidan extracted from sporophylls of the brown seaweed Undaria pinnatifida (Ups-fucoidan) has a higher sulfate and L-fucose content and a wider range of physiological and biological activities than other fucoidans [24]. The anti-tumor activity of Ups-fucoidan has garnered much attention. "
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    ABSTRACT: Metastasis is one of the major causes of cancer-related death. It is a complex biological process involving multiple genes, steps, and phases. It is also closely connected to many biological activities of cancer cells, such as growth, invasion, adhesion, hematogenous metastasis, and lymphatic metastasis. Fucoidan derived from Undaria pinnatifida sporophylls (Ups-fucoidan) is a sulfated polysaccharide with more biological activities than other fucoidans. However, there is no information on the effects of Ups-fucoidan on tumor invasion and metastasis. We used the mouse hepatocarcinoma Hca-F cell line, which has high invasive and lymphatic metastasis potential in vitro and in vivo, to examine the effect of Ups-fucoidan on cancer cell invasion and metastasis. Ups-fucoidan exerted a concentration- and time-dependent inhibitory effect on tumor metastasis in vivo and inhibited Hca-F cell growth, migration, invasion, and adhesion capabilities in vitro. Ups-fucoidan inhibited growth and metastasis by downregulating vascular endothelial growth factor (VEGF) C/VEGF receptor 3, hepatocyte growth factor/c-MET, cyclin D1, cyclin-dependent kinase 4, phosphorylated (p) phosphoinositide 3-kinase, p-Akt, p-extracellular signal regulated kinase (ERK) 1/2, and nuclear transcription factor-κB (NF-κB), and suppressed adhesion and invasion by downregulating L-Selectin, and upregulating protein levels of tissue inhibitor of metalloproteinases (TIMPs). The results suggest that Ups-fucoidan suppresses Hca-F cell growth, adhesion, invasion, and metastasis capabilities and that these functions are mediated through the mechanism involving inactivation of the NF-κB pathway mediated by PI3K/Akt and ERK signaling pathways.
    Full-text · Article · Aug 2014 · PLoS ONE
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    • "In addition, these PLS have a number of biological activities, including anticoagulant, antiviral, gastroprotective, antinociceptive, and anti-inflammatory properties (Brito et al., 2013; Chaves et al., 2013; Cumashi et al., 2007; Silva et al., 2011). The Red Seaweed Digenea simplex (Wulfen) C. Agardh, a member of the Rhodomelaceae family, is used extensively in Japan as a parasiticide, and considered a good source of agar (El-Sayed, 1983; Tomoda, Nakatsuka, & Minami, 1972). "
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    ABSTRACT: Polysaccharides (PLS) have notably diverse pharmacological properties. In the present study, we investigated the previously unexplored anti-inflammatory and antinociceptive activities of the PLS fraction isolated from the marine red alga Digenea simplex. We found that the PLS fraction reduced carrageenan-induced edema in a dose-dependent manner, and inhibited inflammation induced by dextran, histamine, serotonin, and bradykinin. The fraction also inhibited neutrophil migration into both mouse paw and peritoneal cavity. This effect was accompanied by decreases in IL1-β and TNF-α levels in the peritoneal fluid. Pre-treatment of mice with PLS (60mg/kg) significantly reduced acetic acid-induced abdominal writhing. This same dose of PLS also reduced total licking time in both phases of a formalin test, and increased latency in a hot plate test. Therefore, we conclude that PLS extracted from D. simplex possess anti-inflammatory and antinociceptive activities and can be useful as therapeutic agents against inflammatory diseases.
    Full-text · Article · Aug 2014
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    • "Among them, marine seaweeds represent one of the richest sources of bioactive compounds which are widely used in pharmaceutical research [16–18]. Polyphenols and sulfated polysaccharides present in seaweeds have been proven for antiviral, antitumoral, anti-inflammatory, and anticoagulant activity [17–19]. Seaweeds contain prolific source of bioactive compounds which can be exploited for the treatment of major chronic diseases like diabetes through the inhibition of starch digesting enzymes and the regulation of glucose induced oxidative stress [20, 21]. "
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    ABSTRACT: One of the therapeutic approaches in treating diabetes is to reduce postprandial hyperglycemia by inhibiting major carbohydrate hydrolyzing enzymes. In the present study, crude extracts of marine seaweed, Turbinaria ornata, were tested for their antidiabetic potential using enzyme inhibitory assays (α-amylase, α-glucosidase, and dipeptidyl peptidase-IV). Among the tested extracts, methanol and acetone extracts showed significant inhibitory effects on α-amylase ( IC 50 250.9 μg/mL), α-glucosidase (535.6 μg/mL), and dipeptidyl peptidase-4 (55.2 μg/mL), respectively. Free radical scavenging activity of these extracts was analyzed using DPPH assay (65%). Extracts were tested for in vitro toxicity using DNA fragmentation assay, haemolytic assay, and MTT assay. None of the extracts showed toxicity in tested models. Furthermore, GC-MS analysis of lead extracts showed the presence of major compounds, hentriacontane, z, z-6, 28-heptatriactontadien-2-one, 8-heptadecene, and 1-heptacosanol. Our findings suggest that Turbinaria ornata can be used as a potential source for further in vivo studies in controlling hyperglycemia.
    Full-text · Article · Jun 2014 · BioMed Research International
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