scholarly journals PLA-PEG Nanoparticles Improve the Anti-Inflammatory Effect of Rosiglitazone on Macrophages by Enhancing Drug Uptake Compared to Free Rosiglitazone

Materials ◽  
2018 ◽  
Vol 11 (10) ◽  
pp. 1845 ◽  
Author(s):  
Giovanna Giacalone ◽  
Nicolas Tsapis ◽  
Ludivine Mousnier ◽  
Hélène Chacun ◽  
Elias Fattal
Keyword(s):  
Polymeric Nanoparticles ◽  
Heart Diseases ◽  
The United States ◽  
Drug Uptake ◽  
Dependent Manner ◽  
Raw264.7 Macrophages ◽  
Efficient Delivery ◽  
Anti Inflammatory ◽  
Atherosclerosis Treatment ◽  
Inflammatory Effect

Among cardiovascular diseases, atherosclerosis remains the first cause of death in the United States of America and Europe, as it leads to myocardial infarction or stroke. The high prevalence of heart diseases is due to the difficulty in diagnosing atherosclerosis, since it can develop for decades before symptoms occur, and to the complexity of the treatment since targets are also important components of the host defenses. The antidiabetics thiazolidinediones, among which is rosiglitazone (RSG), have demonstrated anti-atherosclerotic effect in animal models, and are therefore promising candidates for the improvement of atherosclerosis management. Nevertheless, their administration is hindered by the insurgence of severe side effects. To overcome this limitation, rosiglitazone has been encapsulated into polymeric nanoparticles, which permit efficient delivery to its nuclear target, and selective delivery to the site of action, allowing the reduction of unwanted effects. In the present work, we describe nanoparticle formulation using polylactic acid (PLA) coupled to polyethylene glycol (PEG), their characterization, and their behavior on RAW264.7 macrophages, an important target in atherosclerosis treatment. RSG nanocarriers showed no toxicity on cells at all concentrations tested, an anti-inflammatory effect in a dose-dependent manner, up to 5 times more efficient than the free molecule, and an increased RSG uptake which is consistent with the effect shown. These biodegradable nanoparticles represent a valid tool to be further investigated for the treatment of atherosclerosis.

scholarly journals Benzoylaconine Modulates LPS-Induced Responses through Inhibition of Toll-Like Receptor-Mediated NF-κB and MAPK Signaling in RAW264.7 Cells

2021 ◽  
Author(s):  
Changkai Zhou ◽  
Jing Gao ◽  
Hongyan Ji ◽  
Wenjing Li ◽  
Xiaomin Xing ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Nuclear Translocation ◽  
Mapk Signaling ◽  
Dependent Manner ◽  
Toll Like Receptor ◽  
Protein Levels ◽  
Raw264.7 Macrophages ◽  
Elevated Protein ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Abstract Previous studies have shown that benzoylaconine (BAC), a representative monoester alkaloid, has a potential anti-inflammatory effect. This study investigated the underlying molecular mechanisms using the mode of LPS-activated RAW264.7 macrophage cells. Our findings showed that BAC significantly suppressed the release of pro-inflammatory cytokines and mediators, including IL-6, TNF-α, IL-1β, ROS, NO, and PGE2. BAC treatment also effectively downregulated the elevated protein levels of iNOS and COX-2 induced by LPS in a dose-dependent manner. In this study, we found that BAC inhibited LPS-induced NF-κB activation by reducing the phosphorylation and degradation of IκBα by Western blotting and blocking the nuclear translocation of p65 using an immunofluorescence assay. The elevated protein levels of JNK, p38, and ERK phosphorylation after LPS stimulation were restored effectively by BAC treatment. Moreover, LPS-induced phosphorylation of TAK1, which is a crucial upstream regulatory factor of Toll-like receptor-induced MAPK and NF-κB signaling, was inhibited by BAC in activated RAW264.7 macrophages. These findings demonstrated that BAC exhibited an anti-inflammatory effect by inhibition of Toll-like receptor-induced MAPK and NF-κB pathways, indicating that it could potentially be used for treating inflammatory diseases.

scholarly journals Inhibition of Inflammatory Response by Artepillin C in Activated RAW264.7 Macrophages

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Ewelina Szliszka ◽  
Anna Mertas ◽  
Zenon P. Czuba ◽  
Wojciech Król
Keyword(s):  
Cell Viability ◽  
Radical Scavenging ◽  
Gm Csf ◽  
Raw264.7 Macrophages ◽  
Griess Reaction ◽  
Artepillin C ◽  
Anti Inflammatory ◽  
Radical Scavenging Ability ◽  
Brazilian Green Propolis ◽  
Inflammatory Effect

Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is the main bioactive component of Brazilian green propolis. The aim of this study was to investigate the anti-inflammatory effect of artepillin C on LPS + IFN-γ- or PMA-stimulated RAW264.7 macrophages. The cell viability was evaluated by MTT and LDH assays. The radical scavenging ability was determined using DPPH•and ABTS•+. ROS and RNS generation was analyzed by chemiluminescence. NO concentration was detected by the Griess reaction. The release of various cytokines by activated RAW264.7 cells was measured in the culture supernatants using a multiplex bead array system based on xMAP technology. NF-κB activity was confirmed by the ELISA-based TransAM NF-κB kit. At the tested concentrations, the compound did not decrease the cell viability and did not cause the cytotoxicity. Artepillin C exerted strong antioxidant activity, significantly inhibited the production of ROS, RNS, NO, and cytokine IL-1β, IL-3, IL-4, IL-5, IL-9, IL-12p40, IL-13, IL-17, TNF-α, G-CSF, GM-CSF, MCP-1, MIP-1α, MIP-1β, RANTES, and KC, and markedly blocked NF-κB expression in stimulated RAW264.7 macrophages. Our findings provide new insights for understanding the mechanism involved in the anti-inflammatory effect of artepillin C and support the application of Brazilian green propolis in complementary and alternative medicine.

Heme oxygenase-1 mediates the anti-inflammatory effect of mushroom Phellinus linteus in LPS-stimulated RAW264.7 macrophages

2006 ◽  
Vol 106 (3) ◽  
pp. 364-371 ◽  
Author(s):  
Byung-Chul Kim ◽  
Joung-Woo Choi ◽  
Hye-Young Hong ◽  
Sin-Ae Lee ◽  
Suntaek Hong ◽  
...  
Keyword(s):  
Heme Oxygenase ◽  
Heme Oxygenase 1 ◽  
Phellinus Linteus ◽  
Raw264.7 Macrophages ◽  
Anti Inflammatory ◽  
Inflammatory Effect

scholarly journals Effects of esculentoside A on turnour necrosis factor production by mice peritoneal macrophages

1992 ◽  
Vol 1 (6) ◽  
pp. 375-377 ◽  
Author(s):  
Fang Jun ◽  
Zheng Qin Yue ◽  
Wang Hong Bin ◽  
Ju Dian Wen ◽  
Yi Yang Hua
Keyword(s):  
Tumour Necrosis Factor ◽  
Tumour Necrosis ◽  
Inflammatory Mediator ◽  
Platelet Activating Factor ◽  
Peritoneal Macrophages ◽  
Dependent Manner ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Necrosis Factor ◽  
Inflammatory Effect

Esculentoside A (EsA) is a saponin isolated from the roots of Phytolacca esculenta. Previous experiments showed that it had strong anti-inflammatory effects. Tumour necrosis factor (TNF) is an important inflammatory mediator. In order to study the mechanism of the anti-inflammatory effect of EsA, it was determined whether TNF production from macrophages was altered by EsA under lipopolysaccharide (LPS) stimulated conditions. EsA was found to decrease both extracellular and cell associated TNF production in a dose dependent manner at concentrations higher than 1 μmol/l EsA. Previous studies have showed that EsA reduced the releasing of platelet activating factor (PAF) from rat macrophages. The reducing effects of EsA on the release of TNF and PAF may explain its anti-inflammatory effect.

The beclomethasone anti-inflammatory effect occurs in cell/mediator-dependent manner and is additively enhanced by formoterol: NFkB, p38, PKA analysis

Life Sciences ◽  
2018 ◽  
Vol 203 ◽  
pp. 27-38 ◽  
Author(s):  
Silvana Cianchetti ◽  
Cristina Cardini ◽  
Alessandro Corti ◽  
Marta Menegazzi ◽  
Elena Darra ◽  
...  
Keyword(s):  
Dependent Manner ◽  
Anti Inflammatory ◽  
Inflammatory Effect

In vitro antihemolytic effect, in vivo anti inflammatory and In vitro antioxidant activity of Anchusa azurea Mill

2021 ◽  
Vol 20 ◽  
Author(s):  
Boussoualim Naouel ◽  
Trabsa Hayat ◽  
Krache Imane ◽  
Ouhida Soraya ◽  
Arrar Lekhmissi ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Folk Medicine ◽  
Oxidative Degradation ◽  
Negative Control ◽  
Dependent Manner ◽  
Anti Inflammatory ◽  
Β Carotene ◽  
Inflammatory Effect

Background: Anchusa azurea Mill. (AA) is a medicinal plant largely used traditionally in folk medicine in Algeria, it is locally named: hamham. It is effective in the treatment of various diseases. Objectives: The aim of the present study is to determine the antioxidant, anti-inflammatory and anti-hemolytic effects of phenolic fractions from Anchusa azurea Mill. Methods: In this study, various extracts from Anchusa azurea Mill. (AA) using solvents with increasing polarity were prepared. The quantification of polyphenols and flavonoids was determined. The anti-radical activity of the different extracts was evaluated using DPPH and by measuring the inhibition of the oxidative degradation of β-carotene. The In vitro antihemolytic effect of the plant extracts is determined (CrE, ChE, AcE and AqE). For each extract, four concentrations were tested: 10.59, 21.18, 42.37, 84.74 µg/ml. Vitamin C is used as a standard. Free-radical attack was measured by measuring the HT50 (Half-Hemolysis Time). The anti-inflammatory effect using PMA on mice of the methanolic extract (CrE) was evaluated. Results: The quantification of polyphenols and flavonoids showed that ethyl acetate extract (AcE) contains a higher amount of polyphenols. However, chloroform extract (ChE) presents a higher amount of flavonoids. AcE showed an important scavenging activity using the DPPH radical (IC50= 68.35 µg/ml). The results showed that AcE also exhibited very great inhibition on the oxidation of β-carotene/linoleic acid (84.33%). All extracts increased the HT50 values (Half-Hemolysis Time) in a dose-dependent manner. The three highest concentrations (21.18, 42.37 and 84.74 µg / ml) of ChE caused a very significant delay (p ≤ 0.001) of hemolysis compared to the negative control and the positive control "VIT C". The anti-inflammatory effect using PMA on mice showed that the methanolic extract (CrE) of AA reduced the weight of the ear edema. Conclusions: This plant has a strong pharmacological power, which supports its traditional medicinal use.

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