• Korean Journal of Plant Resources
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• v.36 no.1
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• pp.15-25
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• 2023

Myriophyllum spicatum L. has been used as an ornamental in ponds and aquariums, and as a folk remedy for inflammation and pus. Nevertheless, the biological activity and underlying mechanisms of anti-inflammatory effects are unclear. This study is aimed at investigating the antioxidative and anti-inflammatory activities of ethanol extract of Myriophyllum spicatum L. (EMS) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Antioxidant activity of EMS was assessed by radical-scavenging effects on ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals. As inflammatory response parameters produced by LPS-stimulated RAW 264.7 cells were quantified to assess the anti-inflammatory activity of EMS. Our results showed that EMS increased FRAP and DPPH radical-scavenging activity. In EMS-treated RAW 264.7 cells, the production of NO, PGE₂, TNF-α and IL-1β was significantly inhibited at the non-cytotoxic concentration. In addition, EMS significantly attenuated LPS-stimulated the toll-like receptor (TLR) 4/myeloid differentiation protein (MyD) 88 signaling pathway, and inhibited nuclear translocation of nuclear factor-kappa B(NF-κB). Positive correlations were noted between anti-inflammatory activity and antioxidant activity. In conclusion, it was indicated that EMS suppresses the transcription of inflammatory factors by inhibiting the TLR4/MyD88/NF-κB signaling pathway, thereby suppressing LPS-stimulated inflammation in RAW 264.7 cells. This study highlights the potential role of EMS against inflammation and associated diseases.

• Journal of Applied Biological Chemistry
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• v.57 no.3
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• pp.227-234
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• 2014

The anti-inflammatory effect of Sargassum micracanthum water extract (SMWE) was investigated using lipopolysaccharide (LPS)-induced inflammatory response in this study. The murine macrophage cell line RAW 264.7 cells were used and MTT assay was performed to measure the cell proliferation ability. The secretion of nitric oxide (NO), tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-6 (IL-6), and IL-$1{\beta}$ was measured in LPS-induced RAW 264.7 cells by ELISA. The expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and nuclear transcription factor-kappa B p65 protein was studied by immunoblotting. The Balb/c mice were used for an acute toxicity test, and imprinting control region mice were purchased to evaluate a croton oil-induced ear edema. As a result, there was no cytotoxicity in the macrophage proliferation treated with SMWE compared to the control. NO levels decreased with increasing concentration of SMWE and were inhibited over 50%. Moreover, the secretion of IL-6, TNF-${\alpha}$, and IL-$1{\beta}$ was suppressed in a dose-dependent manner, especially, IL-$1{\beta}$ inhibition activity was over 50% at 50 ${mu}g$/mL. The formation of ear edema of mice was reduced at the highest dose tested compared to that in the control. Moreover, in acute toxicity test, no moralities occurred in mice administered 5,000 mg/kg body weight of SMWE over 2 weeks observation period. These results suggested that SMWE may have significant effects on inflammatory factors and be potential anti-inflammatory therapeutic materials.

• Food Science and Preservation
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• v.22 no.5
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• pp.735-743
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• 2015

This study investigated the anti-inflammatory activity of barley leaf extract in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and hairless mice. Pre-treatment with barley leaf extract significantly inhibited the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-II (COX-II) in a dose-dependent manner in LPS-stimulated RAW264.7 cells. Barley leaf extract also significantly inhibited the secretion of inflammatory cytokines, such as tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$), and interleukin-6 (IL-6). Moreover, phosphorylation of mitogen-activated protein kinases (MAPKs) and nuclear translocation of nuclear factor-kappa B (NF-${\kappa}B$) were strongly suppressed by barley leaf extract in LPS-stimulated cells. In hairless mice, barley extract significantly decreased the pathological phenotypes of contact dermatitis, such as erythema, edema, and scabs. These results indicate that barley leaf extract has an anti-inflammatory effect and therefore a possible role in the treatment of inflammatory diseases or in functional cosmetics.

• YAKHAK HOEJI
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• v.59 no.6
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• pp.251-258
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• 2015

Aim of the present study was to investigate whether methanol extract from the leaves of Staphylea bumalda could be used to suppress lipopolysaccharide (LPS)-induced inflammatory responses in murine macrophage cell lines, Raw 264.7 cells. The extract reduced nitric oxide (NO), cyclooxigenase-2 (COX-2) and pro-inflammatory cytokines production from LPS-stimulated Raw 264.7 cells. These inhibitory effects were associated with decreases in the phosphorylation of MAP kinases and the activity of $NF{\kappa}B$ signal pathways. Our results indicate that Staphylea bumalda significantly inhibits the inflammatory activity of activated macrophages, suggesting that Staphylea bumalda could be a potential candidate for the treatment of inflammatory disease.

• Korean Journal of Food Science and Technology
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• v.44 no.3
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• pp.331-336
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• 2012

In this study, we selected Gardeniae fructus (GF) as an anti-inflammatory functional material and improved the biological activity of GF through the treatment of ${\beta}$-glucosidase. For the simple evaluation of anti-inflammatory activity, the inhibitory activity of GF extract (GFE) on the production of NO by RAW264.7 cells in the presence of LPS was examined. ${\beta}$-glucosidase originating from Aspergillus niger or Aspergillus fumigatus has effectively improved the anti-inflammatory activity of GFE. The enzyme treatment raised the activity of GFE by more than 10 times. The optimum conditions for the enzyme reaction were at pH 4.6, $45^{\circ}C$, and 20 U/mL for 24 h with agitation. In addition, in vitro production of cytokines (IL-$1{\beta}$, IL-6, TNF-${\alpha}$), COX-2, and the NF-${\kappa}B$ activation of RAW264.7 cells decreased more in the presence of GFE treated with ${\beta}$-glucosidase originating from Aspergillus niger (GFAN) than in the presence of GFE. These results suggest that enzyme-treated GFE might be a potential candidate for natural anti-inflammatory food materials.

• Tuberculosis and Respiratory Diseases
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• v.61 no.4
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• pp.374-383
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• 2006

Background: Ethyl pyruvate (EP) is a derivative of pyruvate that has recently been identified by both various in vitro and in vivo studies to have antioxidant and anti-inflammatory effects. The aim of this study was to determine the effect of EP on lipopolysaccharide (LPS)-induced acute lung injury (ALI). Methods: 5 weeks old, male BALB/c mice were used. ALI was induced by an intratracheal instillation of LPS 0.5mg/Kg/$50{\mu}L$ of saline. The mice were divided into the control, LPS, EP+LPS, and LPS+EP groups. In the control group, balanced salt solution was injected intraperitoneally 30 minutes before or 9 hours after the intratracheal instillation of saline. In the LPS group, a balanced salt solution was also injected intraperitoneally 30 minutes before or 9 hours after instillation the LPS. In the EP+LPS group, 40mg/Kg of EP was injected 30 minutes before LPS instillation. In the LPS+EP group, 40mg/Kg of EP was injected 9 hours after LPS instillation. The TNF-$\alpha$ and IL-6 concentrations in the bronchoalveolar lavage fluid (BALF), and that of NF-$\kappa$B in the lung tissue were measured in the control, LPS and EP+LPS groups at 6 hours after instillation of saline or LPS, and the ALI score and myeloperoxidase (MPO) activity were measured in all four groups 24 and 48 hours after LPS instillation, respectively. Results: The TNF-$\alpha$ and IL-6 concentrations were significantly lower in the EP+LPS group than in the LPS group (p<0.05). The changes in the concentration of these inflammatory cytokines were strongly correlated with that of NF-$\kappa$B (p<0.01). The ALI scores were significantly lower in the EP+LPS and LPS+EP groups compared with the LPS group (p<0.05). In the EP+LPS group, the MPO activity was significantly lower than the LPS group (p=0.019). Conclusion: EP, either administered before or after LPS instillation, has protective effects against the pathogenesis of LPS-induced ALI. EP has potential theurapeutic effects on LPS-induced ALI.

• Proceedings of the Korean Society of Life Science Conference
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• 2008.10a
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• pp.98.2-98.2
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• 2008

• Molecules and Cells
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• v.41 no.3
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• pp.244-255
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• 2018

Low-grade pro-inflammatory state and leptin resistance are important underlying mechanisms that contribute to obesity-associated hypertension. We tested the hypothesis that Astragaloside IV (As IV), known to counteract obesity and hypertension, could prevent obesity-associated hypertension by inhibiting pro-inflammatory reaction and leptin resistance. High-fat diet (HFD) induced obese rats were randomly assigned to three groups: the HFD control group (HF con group), As IV group, and the As IV + ${\alpha}$-bungaratoxin (${\alpha}-BGT$) group (As IV+${\alpha}-BGT$ group). As IV ($20mg{\cdot}Kg^{-1}{\cdot}d^{-1}$) was administrated to rats for 6 weeks via daily oral gavage. Body weight and blood pressure were continuously measured, and NE levels in the plasma and renal cortex was evaluated to reflect the sympathetic activity. The expressions of leptin receptor (LepRb) mRNA, phosphorylated signal transducer and activator of transcription-3 (p-STAT3), phosphorylated phosphatidylinositol 3-kinase (p-PI3K), suppressor of cytokine signaling 3 (SOCS3) mRNA, and protein-tyrosine phosphatase 1B (PTP1B) mRNA, pro-opiomelanocortin (POMC) mRNA and neuropeptide Y (NPY) mRNA were measured by Western blot or qRT-PCR to evaluate the hypothalamic leptin sensitivity. Additionally, we measured the protein or mRNA levels of ${\alpha}7nAChR$, inhibitor of nuclear factor ${\kappa}B$ kinase subunit ${\beta}/nuclear$ factor ${\kappa}B$ ($IKK{\beta}/NF-KB$) and pro-inflammatory cytokines ($IL-1{\beta}$ and $TNF-{\alpha}$) in hypothalamus and adipose tissue to reflect the anti-inflammatory effects of As IV through upregulating expression of ${\alpha}7nAChR$. We found that As IV prevented body weight gain and adipose accumulation, and also improved metabolic disorders in HFD rats. Furthermore, As IV decreased BP and HR, as well as NE levels in blood and renal tissue. In the hypothalamus, As IV alleviated leptin resistance as evidenced by the increased p-STAT3, LepRb mRNA and POMC mRNA, and decreased p-PI3K, SOCS3 mRNA, and PTP1B mRNA. The effects of As IV on leptin sensitivity were related in part to the up-regulated ${\alpha}7nAchR$ and suppressed $IKK{\beta}/NF-KB$ signaling and pro-inflammatory cytokines in the hypothalamus and adipose tissue, since co-administration of ${\alpha}7nAChR$ selective antagonist ${\alpha}-BGT$ could weaken the improved effect of As IV on central leptin resistance. Our study suggested that As IV could efficiently prevent obesityassociated hypertension through inhibiting inflammatory reaction and improving leptin resistance; furthermore, these effects of As IV was partly related to the increased ${\alpha}7nAchR$ expression.

• Journal of Applied Biological Chemistry
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• v.65 no.3
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• pp.203-213
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• 2022

Abeliophyllum distichum (A. distichum, Korean endemic plant) is one genus and one species in the Oleaceae family. According to the color variation of petals and calyx, A. distichum is classified as A. distichum (white flower), A. distichum for. lilacinum (pink flowers), A. distichum for. eburneum (ivory flowers), and Okhwang 1 (golden flowers). In previous studies, bioactivities (antioxidant, anti-inflammatory, and anti-cancer) of A. distichum have been reported. We conducted a comparison of the differences in bioactive compounds and the anti-inflammatory effects on macrophages among four flowers of A. distichum (FAD). The identification and quantification of glycosides were analyzed by HPLC/PDA and LCMS. These results were shown FAD has rutin, hirsutrin, and acteoside. Antioxidant activity of FAD significantly decreased reactive oxygen species. In addition, FAD reduced the expression of pro-inflammatory mediators (nitric oxide, iNOS, and COX-2) in lipopolysaccharide-induced RAW 264.7 cells. For further study, we investigated the regulation of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways. In conclusion, FAD may exert anti-inflammatory effects by suppressing inflammatory mediators via regulations of NF-κB and MAPK signaling pathways. Therefore, these findings suggest that FAD is a potential resource as a preventative or therapeutic agent for inflammation.

• Biomolecules & Therapeutics
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• v.30 no.1
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• pp.48-54
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• 2022

GPR43 (also known as FFAR2), a metabolite-sensing G-protein-coupled receptor stimulated by short-chain fatty acid (SCFA) ligands is involved in innate immunity and metabolism. GPR43 couples with Gα_i/o and Gα_q/11 heterotrimeric proteins and is capable of decreasing cyclic AMP and inducing Ca²⁺ flux. The GPR43 receptor has additionally been shown to bind β-arrestin 2 and inhibit inflammatory pathways, such as NF-κB. However, GPR43 shares the same ligands as GPR41, including acetate, propionate, and butyrate, and determination of its precise functions in association with endogenous ligands, such as SCFAs alone, therefore remains a considerable challenge. In this study, we generated novel synthetic agonists that display allosteric modulatory effects on GPR43 and downregulate NF-κB activity. In particular, the potency of compound 187 was significantly superior to that of pre-existing compounds in vitro. However, in the colitis model in vivo, compound 110 induced more potent attenuation of inflammation. These novel allosteric agonists of GPR43 clearly display anti-inflammatory potential, supporting their clinical utility as therapeutic drugs.