scholarly journals Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE2 and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2556 ◽  
Author(s):  
Mohammed S. Abdel-Maksoud ◽  
Mohammed I. El-Gamal ◽  
Mahmoud M. Gamal El-Din ◽  
Yunji Choi ◽  
Jungseung Choi ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Pyrazole Ring ◽  
Inhibitory Effect ◽  
No Production ◽  
Raw 264.7 ◽  
Design Synthesis ◽  
Raw 264.7 Macrophages ◽  
New Compounds ◽  
Oxide Synthase

This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. The IC50 for nitric oxide inhibition, PGE2 inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity.

scholarly journals Elucidation of Danzhixiaoyao Wan and Its Constituent Herbs on Antioxidant Activity and Inhibition of Nitric Oxide Production

2007 ◽  
Vol 4 (4) ◽  
pp. 425-430 ◽  
Author(s):  
Hui Liao ◽  
Linda K. Banbury ◽  
David N. Leach
Keyword(s):  
Nitric Oxide ◽  
Antioxidant Activity ◽  
Inhibitory Effect ◽  
No Production ◽  
Raw 264.7 ◽  
Gardenia Jasminoides ◽  
The Individual ◽  
Clinical Conditions ◽  
Heat Property

Danzhixiaoyao Wan (DW) is a common 10 herbs formulation in China for regulating several clinical conditions affecting women. This research tried to explain one of DW's functions, purging heat, usingin vitropharmacological analyses. The whole formulation and each single herb of DW were compared based on antioxidant activity with the oxygen radical absorbance capacity (ORAC) assay, and for their inhibitory effect (IE) on nitric oxide (NO) production by lipopolysaccharide (LPS)-activated RAW 264.7 macrophages with the Griess assay. The results showed that DW as a whole formulation had both antioxidant activity and an IE on NO production, while the individual herb component of DW varied in their ORAC values and inhibition of NO production. The ORAC value of the whole DW was 450 μmol TE g−1. The order of antioxidant (ORAC) activity of the single herbs was:Mentha haplocalyx(1352 μmol TE g−1) >Glycyrrhiza uralensis(1184 μmol TE g−1) >Gardenia jasminoides(1129 μmol TE g−1) >Paeonia suffruticosa(465 μmol TE g−1), with the contributions being additive rather than synergistic. The production of nitrite by stimulated RAW 264.7 murine macrophages (unstimulated: 0.5 ± 0.1 μM versus LPS: 38.9 ± 2.3 μM) was significantly inhibited (P< 0.05) byM. haplocalyx,G. jasminoides,Bupleurum chinenseandPaeonia lactiflora. DW as a whole had an IE on NO production, but this was not significant. The single herbM. haplocalyxhad the highest ORAC value and the highest IE on NO production, followed byG. jasminoides. Both of these herbs have the ‘purging heat’ property in the theory of traditional Chinese medicine and this property of the samples may be correlated with the antioxidant activity and IE on NO production.

scholarly journals Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE2 Productions and Nitric Oxide in Murine RAW 264.7 Macrophages

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6489
Author(s):  
Mahmoud M. Gamal El-Din ◽  
Mohammed I. El-Gamal ◽  
Young-Do Kwon ◽  
Su-Yeon Kim ◽  
Hee-Soo Han ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Effect ◽  
No Production ◽  
Raw 264.7 ◽  
Inhibitory Effects ◽  
Western Blots ◽  
Raw 264.7 Macrophages ◽  
Inos Protein Expression ◽  
Ic50 Values ◽  
Cox 2

A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E2 (PGE2) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds 1a–m have first been assessed for cytotoxicity against RAW 264.7 macrophages to determine their non-cytotoxic concentration(s) for anti-inflammatory testing to make sure that the inhibition of PGE2 and NO production would not be caused by cytotoxicity. It was found that compounds 1f and 1m were the most potent PGE2 inhibitors with IC50 values of 7.1 and 1.1 μM, respectively. In addition, these compounds also showed inhibitory effects of 11.6% and 37.19% on LPS-induced NO production, respectively. The western blots analysis of COX-2 and iNOS showed that the PGE2 and NO inhibitory effect of compound 1m are attributed to inhibition of COX-2 and iNOS protein expression through inactivation of p38.

scholarly journals Diterpenoids Isolated from Podocarpus macrophyllus Inhibited the Inflammatory Mediators in LPS-Induced HT-29 and RAW 264.7 Cells

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4326
Author(s):  
ChoEen Kim ◽  
DucDat Le ◽  
Mina Lee
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Effect ◽  
Raw 264.7 Cells ◽  
No Production ◽  
Raw 264.7 ◽  
Sexually Transmitted ◽  
Anti Inflammatory ◽  
Extracellular Regulated Kinase ◽  
Oxide Synthase ◽  
Ht 29

Species of Podocarpus are used traditionally in their native areas for the treatment of fevers, asthma, coughs, cholera, chest pain, arthritis, rheumatism, and sexually transmitted diseases. To identify natural products having efficacy against inflammatory bowel disease (IBD), we identified a new, 16-hydroxy-4β-carboxy-O-β-D-glucopyranosyl-19-nor-totarol (4) together with three known diterpenoids from P. macrophyllus. Furthermore, all the extracts, fractions, and isolates 1-4 were investigated for their anti-inflammatory effects by assessing the expression on nitric oxide (NO) production and proinflammatory cytokines in lipopolysaccharide (LPS)-stimulated RAW 264.7 and HT-29 cells. Among them, nagilactone B (2) exhibited a potent anti-inflammatory effect against NO production on RAW 264.7 cells; therefore, nagilactone B was further assessed for anti-inflammatory activity. Western blot analysis revealed that nagilactone B significantly decreased the expression of LPS-stimulated protein, inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, and phosphorylated extracellular regulated kinase (pERK)1/2. In addition, nagilactone B downregulated tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-8 levels in LPS-induced macrophages and colonic epithelial cells. To our best knowledge, this is the first report on the inhibitory effect of nagilactone B (pure state) and rakanmakilactone G against NO production in LPS-stimulated RAW 264.7 cells. Thus, diterpenoids isolated from P. macrophyllus could be employed as potential therapeutic phytochemicals for IBD.

scholarly journals Actinofuranones D-I from a Lichen-Associated Actinomycetes, Streptomyces gramineus, and Their Anti-Inflammatory Effects

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2393 ◽  
Author(s):  
Jian Ma ◽  
Bixuan Cao ◽  
Chengbin Liu ◽  
Peipei Guan ◽  
Yu Mu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Fermentation Broth ◽  
Raw 264.7 Cells ◽  
No Production ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophage Cells ◽  
Anti Inflammatory ◽  
Factor Α ◽  
New Compounds ◽  
Oxide Synthase

Six new metabolites, actinofuranones D-I (compounds 1–6), were isolated together with three known compounds—JBIR-108 (7), E-975 (8), and E-492 (9)—from a fermentation broth of Streptomyces gramineus derived from the lichen Leptogium trichophorum. The structures of the new compounds 1–6 were established using comprehensive NMR spectroscopic data analysis, as well as UV, IR, and MS data. The anti-inflammatory activity of these isolated compounds were evaluated by examining their ability to inhibit nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophage cells. Compounds 4, 5, 8, and 9 attenuated the production of NO due to the suppression of the expression of nitric oxide synthase (iNOS) in LPS-induced RAW 264.7 cells. Moreover, 4, 5, 8, and 9 also inhibited LPS-induced release of proinflammatory cytokines interleukin-6 (IL-6) and tumor necrosis factor α (TNF-α).

scholarly journals In Vitro and In Vivo Anti-Inflammatory Effects of Sulfated Polysaccharides Isolated from the Edible Brown Seaweed, Sargassum fulvellum

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 277
Author(s):  
Lei Wang ◽  
Hye-Won Yang ◽  
Ginnae Ahn ◽  
Xiaoting Fu ◽  
Jiachao Xu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Brown Seaweed ◽  
Sulfated Polysaccharides ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophages ◽  
Sargassum Fulvellum ◽  
Pharmaceutical Industries ◽  
Anti Inflammatory

In the present study, the in vitro and in vivo anti-inflammatory effects of the sulfated polysaccharides isolated from Sargassum fulvellum (SFPS) were evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and zebrafish. The results indicated that SFPS improved the viability of LPS-stimulated RAW 264.7 macrophages from 80.02 to 86.80, 90.09, and 94.62% at the concentration of 25, 50, and 100 µg/mL, respectively. Also, SFPS remarkably and concentration-dependently decreased the production levels of inflammatory molecules including nitric oxide (NO), tumor necrosis factor-alpha, prostaglandin E2, interleukin-1 beta, and interleukin-6 in LPS-treated RAW 264.7 macrophages. In addition, SFPS significantly inhibited the expression levels of cyclooxygenase-2 and inducible nitric oxide synthase in LPS-treated RAW 264.7 macrophages. Furthermore, the in vivo test results indicated that SFPS improved the survival rate of LPS-treated zebrafish from 53.33 to 56.67, 60.00, and 70.00% at the concentration of 25, 50, and 100 µg/mL, respectively. In addition, SFPS effectively reduced cell death, reactive oxygen species, and NO levels in LPS-stimulated zebrafish. Taken together, these results suggested that SFPS possesses strong in vitro and in vivo anti-inflammatory activities, and could be used as an ingredient to develop anti-inflammatory agents in the functional food and pharmaceutical industries.

scholarly journals Effects of chitosan on nitric oxide production and inducible nitric oxide synthase activity and mRNA expression in weaned piglets

2018 ◽  
Vol 60 (No. 8) ◽  
pp. 359-366
Author(s):  
J. Li ◽  
B. Shi ◽  
S. Yan ◽  
L. Jin ◽  
Y. Guo ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Mrna Expression ◽  
Inducible Nitric Oxide Synthase ◽  
No Production ◽  
Weaned Piglets ◽  
Inos Activity ◽  
Oxide Synthase ◽  
Inducible Nitric Oxide

The effects of chitosan on nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) activity and gene expression in vivo or vitro were investigated in weaned piglets. In vivo, 180 weaned piglets were assigned to five dietary treatments with six replicates. The piglets were fed on a basal diet supplemented with 0 (control), 100, 500, 1000, and 2000 mg chitosan/kg feed, respectively. In vitro, the peripheral blood mononuclear cells (PBMCs) from a weaned piglet were cultured respectively with 0 (control), 40, 80, 160, and 320 &micro;g chitosan/ml medium. Results showed that serum NO concentrations on days 14 and 28 and iNOS activity on day 28 were quadratically improved with increasing chitosan dose (P &lt; 0.05). The iNOS mRNA expressions were linearly or quadratically enhanced in the duodenum on day 28, and were improved quadratically in the jejunum on days 14 and 28 and in the ileum on day 28 (P &lt; 0.01). In vitro, the NO concentrations, iNOS activity, and mRNA expression in unstimulated PBMCs were quadratically enhanced by chitosan, but the improvement of NO concentrations and iNOS activity by chitosan were markedly inhibited by N-(3-[aminomethyl] benzyl) acetamidine (1400w) (P&nbsp;&lt; 0.05). Moreover, the increase of NO concentrations, iNOS activity, and mRNA expression in PBMCs induced by lipopolysaccharide (LPS) were suppressed significantly by chitosan (P &lt; 0.05). The results indicated that the NO concentrations, iNOS activity, and mRNA expression in piglets were increased by feeding chitosan in a dose-dependent manner. In addition, chitosan improved the NO production in unstimulated PBMCs but inhibited its production in LPS-induced cells, which exerted bidirectional regulatory effects on the NO production via modulated iNOS activity and mRNA expression.

Inhibitory Effect of Trimidox on Lipopolysaccharide-Induced Nitric Oxide Production in RAW 264.7 Macrophages

2007 ◽  
Vol 104 (3) ◽  
pp. 278-281 ◽  
Author(s):  
Syu-ichi Kanno ◽  
Mai Kakuta ◽  
Yasue Kitajima ◽  
Yuu Osanai ◽  
Kaori Kurauchi ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Effect ◽  
Raw 264.7 ◽  
Nitric Oxide Production ◽  
Raw 264.7 Macrophages ◽  
Oxide Production
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