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

Marine Drugs ◽  
2020 ◽  
Vol 18 (5) ◽  
pp. 275 ◽  
Author(s):  
Olga N. Pozharitskaya ◽  
Ekaterina D. Obluchinskaya ◽  
Alexander N. Shikov
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Radical Scavenging ◽  
Brown Seaweed ◽  
Fucus Vesiculosus ◽  
Thrombin Time ◽  
Dpp Iv ◽  
Management Of Complications ◽  
Cox 2 ◽  
Anti Inflammatory

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 μg 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 μg 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 μg mL−1) is one of the possible mechanisms involved in the anti-hyperglycemic activity of fucoidan. At a concentration of 3.2 μg 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 μg 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.

2,5-disubstituted-4-thiazolidinones: Synthesis, anti-inflammatory, free radical scavenging potentials and structural insights through molecular docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh
Keyword(s):  
Free Radicals ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Assay Method ◽  
Acidic Group ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory

: The present work reports synthesis and screening of fifteen 2,5-disubstituted-4-thiazolidinones with different substitutions of varied arylidene groups at imino. The structures of the compounds were confirmed by spectral characterization. The compounds were subjected to in vivo anti-inflammatory and in vitro antioxidant activities. The derivatives possessed remarkable activities quite close to standard drugs used. Unlike conventional non-selective NSAIDs, the synthesized compounds did not contain any acidic group, thereby ensuring a complete cure from ulcers. To further substantiate the claim for safer derivatives, the active compounds were docked against the cyclooxygenase (COX)-2 enzyme. It was found that 4-fluorophenylimino substituent at 2- position and 3-nitro moiety on a 5-benzylidene nucleus of the 4-thiazolidinone derivative fitted in the COX-2 binding pocket. The compounds exhibited remarkable activity in scavenging free radicals, as depicted by the DPPH assay method. The structure-activity relationship was also established in the present work with respect to the nature and position of the substituents. The active compounds were evaluated for drug-like nature under Lipinski’s rule of five, and the toxicity behaviour of active compounds was predicted using ADMETlab software. The compounds have the potential to target degenerative disorders associated with inflammation and the generation of free radicals.

scholarly journals SYNTHESIS, BIOLOGICAL EVALUATION, AND DOCKING STUDY OF NOVEL 2-PHENYL-1- BENZOPYRAN-4-ONE DERIVATIVES - AS A POTENT CYCLOOXYGENASE-2 INHIBITOR

2019 ◽  
pp. 304-310
Author(s):  
NATARAJAN KIRUTHIGA ◽  
THANGAVELU PRABHA ◽  
CHELLAPPA SELVINTHANUJA ◽  
KULANDAIVEL SRINIVASAN ◽  
THANGAVEL SIVAKUMAR
Keyword(s):  
Chronic Diseases ◽  
Radical Scavenging ◽  
Data Bank ◽  
Docking Study ◽  
Biological Evaluation ◽  
Cyclooxygenase 2 ◽  
Spectroscopic Techniques ◽  
Cox 2 ◽  
Anti Inflammatory

Objective: The inflammation and oxidative stress were related together in the generation of reactive oxygen species, which is responsible for the enhancement of inflammation associated with various chronic diseases. Methods: The aim of this study is to synthezise and characterizes the flavones (2-phenyl-1-benzopyran-4-one) derivatives and analyzed by their docking hypothetical data as an effective anti-inflammatory mediator against cyclooxygenase-2 (COX-2) enzyme. Further, the evaluation of various in vitro antioxidant and anti-inflammatory studies was carried out. Results: The 10 compounds were synthesized and characterized by ultraviolet, infrared, nuclear magnetic resonance, and mass spectroscopic techniques. The docking data results of these 10 flavones derivatives against COX-2 enzymes (Protein Data Bank ID: 3LN1) showed the binding energy ranging between −5.53 kcal/mol and −7.02 kcal/mol when compared with that of the standard diclofenac (−6.34 kcal/mol). The in vitro studies suggest that the lipophilic character of the side chain donor, along with the hydroxyl substituted flavones found to have significant half maximal inhibitory concentration values. Conclusion: Based on these in silico and in vitro evaluation results, these synthesized compounds could act as a promising inhibitor to target the COX- 2 enzyme. Hence, those compounds were effective in the management of chronic diseases by exhibits free radical scavenging and anti-inflammatory property.

scholarly journals Demonstration of kallikrein-like protease activity in nonactivated plasma of patients with Cooley's anemia

Blood ◽  
1983 ◽  
Vol 61 (2) ◽  
pp. 232-237
Author(s):  
M Andrew ◽  
M Manno ◽  
M Karpatkin
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Trypsin Inhibitor ◽  
Gel Filtration ◽  
Lima Bean ◽  
Thrombin Time ◽  
Diisopropyl Fluorophosphate ◽  
Bean Trypsin Inhibitor ◽  
Cooley's Anemia

Routine evaluation of 12 children with Cooley's anemia revealed that each one had a prolonged partial thromboplastin time. However, prothrombin time and thrombin time were within the normal range. Specific assays demonstrated low levels of the four contact factors: factors XI, XII, prekallikrein, and high molecular weight kininogen. Further investigation revealed activity against para-nitroanilide peptide substrates in unactivated plasma from all 12 patients. Following gel filtration on Sephadex G200, the activity emerged in one peak in the void volume, indicating a molecular weight of greater the 500,000. Activity was greatest against H-D-Pro-Phe-Arg-pNA, the substrate for plasma kallikrein, and was inhibited by diisopropyl fluorophosphate and trasolyl. It was unaffected by hirudin, soy bean trypsin inhibitor, and lima bean trypsin inhibitor. It was destroyed by heating at 56 degrees C. Specific antisera against human prekallikrein and human alpha-macroglobulin did not reduce the activity. It is concluded that a high molecular weight kallikrein-like protease, is present in the plasma of these patients. It is postulated that it is released into the circulation from tissue as a result of damage due to iron overload. It is further postulated that this protease brings about in vivo activation of the contrast factors, resulting in a fall in their circulating levels.

scholarly journals Low-molecular-weight fucoidan and high-stability fucoxanthin from brown seaweed exert prebiotics and anti-inflammatory activities in Caco-2 cells

2016 ◽  
Vol 60 (1) ◽  
pp. 32033 ◽  
Author(s):  
Pai-An Hwang ◽  
Nam Nhut Phan ◽  
Wen-Jung Lu ◽  
Bui Thi Ngoc Hieu ◽  
Yen-Chang Lin
Keyword(s):  
Molecular Weight ◽  
High Stability ◽  
Brown Seaweed ◽  
Low Molecular Weight ◽  
Anti Inflammatory
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