Mechanisms of Bioactivities of Fucoidan from the Brown Seaweed Fucus vesiculosus L. of the Barents Sea

被引:140
作者
Pozharitskaya, Olga N. [1 ]
Obluchinskaya, Ekaterina D. [1 ]
Shikov, Alexander N. [1 ,2 ]
机构
[1] RAS, MMBI, Vladimirskaya 17, Murmansk 183010, Russia
[2] St Petersburg State Chem Pharmaceut Univ, Prof Popov 14, St Petersburg 197376, Russia
关键词
fucoidan; cyclooxygenase; dipeptidyl peptidase IV; anti-inflammatory; anti-hyperglycemic; anti-coagulant; COVID19; CONTAINING SULFATED POLYSACCHARIDES; IN-VITRO; ANTIOXIDANT ACTIVITY; ANTICOAGULANT ACTIVITY; ANTIINFLAMMATORY ACTIVITY; KINASE PATHWAY; EXTRACTION; FRACTIONS; INHIBITION; HEPARIN;
D O I
10.3390/md18050275
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The aim of this study was to elucidate some mechanisms of radical scavenging and the anti-inflammatory, anti-hyperglycemic, and anti-coagulant bioactivities of high molecular weight fucoidan from Fucus vesiculosus in several in vitro models. Fucoidan has displayed potent 1, 1-diphenyl-2-picryl hydrazil radical scavenging and reduction power activities. It significantly inhibits the cyclooxygenase-2 (COX-2) enzyme (IC50 4.3 mu g mL(-1)) with a greater selectivity index (lg(IC80 COX-2/IC80COX-1), -1.55) than the synthetic non-steroidal anti-inflammatory drug indomethacin (lg(IC80 COX-2/IC80COX-1), -0.09). A concentration-dependent inhibition of hyaluronidase enzyme with an IC50 of 2.9 mu g mL(-1) was observed. Fucoidan attenuated the lipopolysaccharide-induced expression of mitogen-activated protein kinase p38. Our findings suggest that the inhibition of dipeptidyl peptidase-IV (DPP-IV) (IC50 1.11 mu g mL(-1)) is one of the possible mechanisms involved in the anti-hyperglycemic activity of fucoidan. At a concentration of 3.2 mu g mL(-1), fucoidan prolongs the activated partial thromboplastin time and thrombin time by 1.5-fold and 2.5-fold compared with a control, respectively. A significant increase of prothrombin time was observed after the concentration of fucoidan was increased above 80 mu g mL(-1). This evidenced that fucoidan may have an effect on intrinsic/common pathways and little effect on the extrinsic mechanism. This study sheds light on the multiple pathways of the bioactivities of fucoidan. As far as we know, the inhibition of hyaluronidase and DPP-IV by high molecular fucoidan was studied for the first time in this work. Our results and literature data suggest that molecular weight, sulfate content, fucose content, and polyphenols may contribute to these activities. It seems that high molecular weight fucoidan has promising therapeutic applications in different pharmacological settings. Anti-oxidant, anti-inflammatory and anti-coagulant drugs have been used for the management of complications of COVID19. Taken as a whole, fucoidan could be considered as a prospective candidate for the treatment of patients with COVID19; however, additional research in this field is required.
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页数:17
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共 81 条
[1]   Metabolite profiling and mechanisms of bioactivity of snake autolysate - A traditional Uzbek medicine [J].
Akbarov, Umidbek S. ;
Pozharitskaya, Olga N. ;
Laakso, Into ;
Seppanen-Laakso, Tuulikki ;
Urakova, Irina N. ;
Vuorela, Heikki ;
Makarov, Valery G. ;
Shikov, Alexander N. .
JOURNAL OF ETHNOPHARMACOLOGY, 2020, 250
[2]   Fucoidans from brown seaweeds: an update on structures, extraction techniques and use of enzymes as tools for structural elucidation [J].
Ale, Marcel Tutor ;
Meyer, Anne S. .
RSC ADVANCES, 2013, 3 (22) :8131-8141
[3]   Important Determinants for Fucoidan Bioactivity: A Critical Review of Structure-Function Relations and Extraction Methods for Fucose-Containing Sulfated Polysaccharides from Brown Seaweeds [J].
Ale, Marcel Tutor ;
Mikkelsen, Jorn D. ;
Meyer, Anne S. .
MARINE DRUGS, 2011, 9 (10) :2106-2130
[4]   Influence of molecular weight on the properties of Sargassum muticum fucoidan [J].
Alvarez-Vinas, Milena ;
Florez-Fernandez, Noelia ;
Jesus Gonzalez-Munoz, Maria ;
Dominguez, Herminia .
ALGAL RESEARCH-BIOMASS BIOFUELS AND BIOPRODUCTS, 2019, 38
[5]   ANTICOAGULANT PROPERTIES OF HEPARIN FRACTIONATED BY AFFINITY CHROMATOGRAPHY ON MATRIX-BOUND ANTITHROMBIN-3 AND BY GEL-FILTRATION [J].
ANDERSSON, LO ;
BARROWCLIFFE, TW ;
HOLMER, E ;
JOHNSON, EA ;
SIMS, GEC .
THROMBOSIS RESEARCH, 1976, 9 (06) :575-583
[6]   Characterization of substituted aryl meroterpenoids from red seaweed Hypnea musciformis as potential antioxidants [J].
Chakraborty, Kajal ;
Joseph, Deepu ;
Joy, Minju ;
Raola, Vamshi Krishna .
FOOD CHEMISTRY, 2016, 212 :778-788
[7]   Sulfated Polysaccharides Isolated from Cloned Grateloupia filicina and Their Anticoagulant Activity [J].
Chen, Xiaolin ;
Yang, Shengfeng ;
Wang, Jinxia ;
Song, Lin ;
Xing, Ronge ;
Liu, Song ;
Yu, Huahua ;
Li, Pengcheng .
BIOMED RESEARCH INTERNATIONAL, 2015, 2015
[8]   MEASUREMENT OF HEPARIN - METHOD BASED ON POTENTIATION OF ANTIFACTOR XA [J].
DENSON, KWE ;
BONNAR, J .
THROMBOSIS ET DIATHESIS HAEMORRHAGICA, 1973, 30 (03) :471-479
[9]  
Dewi Lestari, 2016, Med Arch, V70, P172, DOI 10.5455/medarh.2016.70.172-176
[10]   Anticoagulant fucoidan fractions from Fucus vesiculosus induce platelet activation in vitro [J].
Durig, J ;
Bruhn, T ;
Zurborn, KH ;
Gutensohn, K ;
Bruhn, HD ;
Beress, L .
THROMBOSIS RESEARCH, 1997, 85 (06) :479-491