Structural characteristics and anti-inflammatory activity of UV/H2O2-treated algal sulfated polysaccharide from Gracilaria lemaneiformis

2021 ◽  
pp. 112157
Author(s):  
Yufeng Gong ◽  
Yongxuan Ma ◽  
Peter Chi-Keung Cheung ◽  
Lijun You ◽  
Lan Liao ◽  
...  
Keyword(s):  
Structural Characteristics ◽  
Sulfated Polysaccharide ◽  
Inflammatory Activity ◽  
Gracilaria Lemaneiformis ◽  
Anti Inflammatory

scholarly journals Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

2021 ◽  
Vol 14 (7) ◽  
pp. 692
Author(s):  
Ryldene Marques Duarte da Cruz ◽  
Francisco Jaime Bezerra Mendonça-Junior ◽  
Natália Barbosa de Mélo ◽  
Luciana Scotti ◽  
Rodrigo Santos Aquino de Araújo ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Structural Characteristics ◽  
Tiaprofenic Acid ◽  
Inflammatory Activity ◽  
Drug Candidates ◽  
Biological Target ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Privileged Structures

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes.

Anti-inflammatory activity of a sulfated polysaccharide from the brown alga Sargassum cristaefolium

2016 ◽  
Vol 53 ◽  
pp. 16-23 ◽  
Author(s):  
Guan-James Wu ◽  
Shiau-Mei Shiu ◽  
Meng-Chen Hsieh ◽  
Guo-Jane Tsai
Keyword(s):  
Brown Alga ◽  
Sulfated Polysaccharide ◽  
Inflammatory Activity ◽  
Anti Inflammatory

Synthesis, crystal structures and anti-inflammatory activity of four 3,5-bis(arylidene)-N-benzenesulfonyl-4-piperidone derivatives

2018 ◽  
Vol 74 (10) ◽  
pp. 1171-1179 ◽  
Author(s):  
Ning Li ◽  
Xianyong Bai ◽  
Lianshuang Zhang ◽  
Yun Hou
Keyword(s):  
Hydrogen Bonds ◽  
High Resolution Mass Spectrometry ◽  
Structural Characteristics ◽  
Crystal Structure Analysis ◽  
Inflammatory Activity ◽  
Unsaturated Ketone ◽  
Activity Data ◽  
Strong Electron ◽  
Phenyl Rings ◽  
Anti Inflammatory

3,5-Bis(arylidene)-4-piperidone (BAP) derivatives display good antitumour and anti-inflammatory activities because of their double α,β-unsaturated ketone structural characteristics. If N-benzenesulfonyl substituents are introduced into BAPs, the configuration of the BAPs would change significantly and their anti-inflammatory activities should improve. Four N-benzenesulfonyl BAPs, namely (3E,5E)-1-(4-methylbenzenesulfonyl)-3,5-bis[4-(trifluoromethyl)benzylidene]piperidin-4-one dichloromethane monosolvate, C28H21F6NO3S·CH2Cl2, (4), (3E,5E)-1-(4-fluorobenzenesulfonyl)-3,5-bis[4-(trifluoromethyl)benzylidene]piperidin-4-one, C27H18F7NO3S, (5), (3E,5E)-1-(4-nitrobenzenesulfonyl)-3,5-bis[4-(trifluoromethyl)benzylidene]piperidin-4-one, C27H18F6N2O5S, (6), and (3E,5E)-1-(4-cyanobenzenesulfonyl)-3,5-bis[4-(trifluoromethyl)benzylidene]piperidin-4-one dichloromethane monosolvate, C28H18F6N2O3S·CH2Cl2, (7), were prepared by Claisen–Schmidt condensation and N-sulfonylation. They were characterized by NMR, FT–IR and HRMS (high resolution mass spectrometry). Single-crystal structure analysis reveals that the two 4-(trifluoromethyl)phenyl rings on both sides of the piperidone ring in (4)–(7) adopt an E stereochemistry of the olefinic double bonds. Molecules of both (4) and (6) are connected by hydrogen bonds into one-dimensional chains. In (5) and (7), pairs of adjacent molecules embrace through intermolecular hydrogen bonds to form a bimolecular combination, which are further extended into a two-dimensional sheet. The anti-inflammatory activity data reveal that (4)–(7) significantly inhibit LPS-induced interleukin (IL-6) and tumour necrosis factor (TNF-α) secretion. Most importantly, (6) and (7), with strong electron-withdrawing substituents, display more potential inhibitory effects than (4) and (5).

Gabapentin Antioxidant Derivatives with Anti-Inflammatory and Neuroprotective Potency

2021 ◽  
Vol 18 ◽  
Author(s):  
Georgios Papagiouvannis ◽  
Panagiotis Theodosis-Nobelos ◽  
Paraskevi Tziona ◽  
Antonios Gavalas ◽  
Panos N. Kourounakis ◽  
...  
Keyword(s):  
Structural Characteristics ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Protein Glycation ◽  
Inflammatory Activity ◽  
Biochemical Pathways ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Effective Drugs

Aims: The aim of this work is to investigate the antioxidant and anti-inflammatory potency of novel gabapentin derivatives, which could be proven useful as neuroprotective agents. Background: Alzheimer’s Disease (AD) is one of the most common neurodegenerative disorders worldwide. Due to its multi-factorial character, no effective treatment has been obtained yet. In this direction, the multi-targeting compounds approach could be useful for the development of novel, more effective drugs against AD. Oxidative stress and inflammation are highly involved in the progression of neurodegeneration, while gabapentin has been investigated for the treatment of behavioral symptoms in AD. Objective: In this work, derivatives of cinnamic acid, trolox and 3,5-di-tertbutyl-4-hydroxybenzoic acid amidated with gabapentin methyl ester, were designed and studied. Compounds with these structural characteristics are expected to act in various biochemical pathways, affecting neurodegenerative processes. Methods: The designed compounds were synthesized with classical amidation methods, purified by flash column chromatography, and identified spectrometrically (1H-NMR and 13C-NMR). Their purity was determined by CHN elemental analysis. They were tested in vitro for their antioxidant and anti-inflammatory properties, and for their inhibitory effect on acetylcholinesterase. Their in vivo anti-inflammatory activity was also tested. Results: Those molecules incorporating an antioxidant moiety possessed inhibitory activity against rat microsomal membrane lipid peroxidation and oxidative protein glycation, as well as radical scavenging activity. Moreover, most of them presented moderate inhibition towards lipoxygenase (up to 51% at 100μΜ) and acetylcholinesterase (AchE) (IC50 up to 274μΜ) activities. Finally, all synthesized compounds presented in vivo anti-inflammatory activity, decreasing carrageenan-induced rat paw edema up to 53% and some of them could inhibit cyclooxygenase significantly. Conclusion: These results indicate that the designed compounds could be proven useful as multi-targeting molecules against AD, since they affect various biochemical pathways associated with neurodegeneration. Thus, more effective drugs can be obtained, and possible adverse effects of drug combination can be limited.

Structural Characteristics of a Bioactive Polysaccharide from Sorghum arundinaceum

2003 ◽  
Vol 58 (5-6) ◽  
pp. 342-346 ◽  
Author(s):  
Bernadete P. da Silva ◽  
Graziela M. Silva ◽  
José P. Parente
Keyword(s):  
Molecular Weight ◽  
Capillary Permeability ◽  
Structural Characteristics ◽  
Apparent Molecular Weight ◽  
Spectroscopic Studies ◽  
Type Structure ◽  
Inflammatory Activity ◽  
Branching Points ◽  
Anti Inflammatory ◽  
Permeability Assay

AbstractA polysaccharide, an α-ᴅ -glucan with an apparent molecular weight of 6.85×104, called PSa glucan, was isolated from fresh seeds of Sorghum arundinaceum by fractionation on Sephacryl S-300 HR and Sephadex G-25. Chemical and spectroscopic studies indicated that it has a highly branched glucan type structure composed of α-(154) linked d-glucopyranose residues with (1→3), (1→6) branching points, and a significant amount of α-(1→6) branching to α-(1→3) linked ᴅ -glucopyranose residues. The anti-inflammatory activity of the polysaccharide was performed using the capillary permeability assay.

scholarly journals Anti-inflammatory activity of a sulfated polysaccharide isolated from an enzymatic digest of brown seaweedSargassum horneriin RAW 264.7 cells

2017 ◽  
Vol 11 (1) ◽  
pp. 3 ◽  
Author(s):  
Kalu Kapuge Asanka Sanjeewa ◽  
Ilekkuttige Priyan Shanura Fernando ◽  
Eun-A Kim ◽  
Ginnae Ahn ◽  
Youngheun Jee ◽  
...  
Keyword(s):  
Sulfated Polysaccharide ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Anti Inflammatory

scholarly journals Purification, Structural Characterization, and Anti-Inflammatory Effects of a Novel Polysaccharide Isolated from Orostachys fimbriata

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7116
Author(s):  
Datong Hu ◽  
Fan Su ◽  
Gan Yang ◽  
Jing Wang ◽  
Yingying Zhang
Keyword(s):  
Structural Characteristics ◽  
Deae Cellulose ◽  
Monosaccharide Composition ◽  
Inflammatory Activity ◽  
Inflammatory Factors ◽  
Composition Analysis ◽  
Sugar Chain ◽  
Chain Molecules ◽  
Anti Inflammatory ◽  
Branched Structure

The present study elucidated the structural characteristics and anti-inflammatory activity of a novel polysaccharide isolated from Orostachys fimbriata, which is a traditional Chinese medicinal plant. O. fimbriata polysaccharide (OFP) was extracted and subsequently purified by chromatography using a DEAE cellulose-52 and Sephadex G-75 column. The molecular weight was determined as 6.2 kDa. HPGPC and monosaccharide composition analysis revealed a homogeneous polysaccharide containing only Glc. Chromatography and spectral analysis showed that the possible chemical structure consisted of →4)-α-Glcp-(1→ and a small quantity of →4,6)-β-Glcp-(1→ in the main chain and →6)-β-Glcp-(1→, α-Glcp-(1→, and β-Glcp-(1→ in the side chain. Morphological analysis using scanning electron microscopy (SEM) and atomic force microscopy (AFM) indicated that OFP had a multi-branched structure, and the sugar chain molecules of polysaccharide appeared aggregated. OFP was found to exhibit anti-inflammatory activity by reducing the secretion of inflammatory factors in RAW264.7 cells and by decreasing the extent of xylene-induced ear swelling in mice.

Sulfated polysaccharide from pacific abalone attenuated DSS-induced acute and chronic ulcerative colitis in mice via regulating intestinal micro-ecology and NF-κB pathway

2021 ◽  
Author(s):  
Jinhui Jia ◽  
Panpan Zhang ◽  
Chenxi Zhang ◽  
Guoping Jiang ◽  
Weiyun Zheng ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Side Effects ◽  
Chronic Ulcerative Colitis ◽  
Sulfated Polysaccharide ◽  
Inflammatory Activity ◽  
Pacific Abalone ◽  
Anti Inflammatory

Due to potential side effects of current drugs in colitis treatment, polysaccharides with anti-inflammatory activity can be considered as an alternative molecule for colitis treatment. Sulfated polysaccharide from pacific abalone...

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