• Biomolecules & Therapeutics
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• v.25 no.6
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• pp.641-647
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• 2017

Galangin (3,5,7-trihydroxyflavone) is a polyphenolic compound abundant in honey and medicinal herbs, such as Alpinia officinarum. In this study, we investigated the anti-inflammatory effects of galangin under in vitro and in vivo neuroinflammatory conditions caused by polyinosinic-polycytidylic acid (poly(I:C)), a viral mimic dsRNA analog. Galangin suppressed the production of nitric oxide, reactive oxygen species, and pro-inflammatory cytokines in poly(I:C)-stimulated BV2 microglia. On the other hand, galangin enhanced anti-inflammatory interleukin (IL)-10 production. Galangin also suppressed the expression of pro-inflammatory markers in poly(I:C)-injected mouse brains. Further mechanistic studies showed that galangin inhibited poly(I:C)-induced nuclear factor (NF)-${\kappa}B$ activity and phosphorylation of Akt without affecting MAP kinases. Interestingly, galangin increased the expression and transcriptional activity of peroxisome proliferator-activated receptor (PPAR)-${\gamma}$, known to play an anti-inflammatory role. To investigate whether PPAR-${\gamma}$ is involved in the anti-inflammatory function of galangin, BV2 cells were pre-treated with PPAR-${\gamma}$ antagonist before treatment of galangin. We found that PPAR-${\gamma}$ antagonist significantly blocked galangin-mediated upregulation of IL-10 and attenuated the inhibition of tumor necrosis factor (TNF)-${\alpha}$ and IL-6 in poly(I:C)-stimulated microglia. In conclusion, our data suggest that PI3K/Akt, NF-${\kappa}B$, and PPAR-${\gamma}$ play a pivotal role in mediating the anti-inflammatory effects of galangin in poly(I:C)-stimulated microglia.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.54 no.2
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• pp.152-161
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• 2021

Eisenia bicyclis is known to have secondary metabolites exhibiting various biological activities. In a preliminary study, the n-hexane fraction obtained from the ethanolic extract of E. bicyclis showed higher anti-inflammatory activity than the ethyl acetate and butyl alcohol fractions based on the inhibition of lipopolysaccharide (LPS)-stimulated nitric oxide (NO) production in RAW 264.7 cells. Using this fraction (E. bicyclis hexane fraction, EHF), we investigated the molecular mechanisms underlying its anti-inflammatory effect in LPS-stimulated RAW 264.7 cells. Pretreatment of the cells with up to 50 ㎍/mL EHF significantly inhibited NO and prostaglandin E₂ production as well as their responsible enzyme proteins and mRNAs, in a dose-dependent manner (P<0.05). Similarly, EHF markedly reduced the production of pro-inflammatory cytokines, such as interleukin (IL)-1β, IL-6 and tumor necrosis factor (TNF)-α as well as their mRNA levels. Nuclear translocation of nuclear factor-kappa B (NF-κB) was strongly suppressed by EHF treatment. EHF significantly reduced the phosphorylation of mitogen-activated protein kinases and phosphatidylinositol 3-kinase/Akt in LPS-stimulated cells. Moreover, EHF reduced ear edema in phorbol myristate acetate (PMA)-induced mice. These results indicate that EHF contains potent anti-inflammatory compounds, which may be used as a dietary supplement for the prevention of inflammatory diseases.

• Herbal Formula Science
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• v.27 no.1
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• pp.17-29
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• 2019

Inflammatory and oxidative stimuli play a critical role not only in the process of transforming normal cells into cancer cells, but also in the proliferation process of cancer cells. Sipyukmiryukieum (SYMRKU), a traditional Korean herb-combined remedy, is composed of 16 kinds of herbal medicines, which were recorded for "Ongjeo" treatment in "Dongeuibogam". In this study, we investigated the inhibitory effect of SYMRKU against inflammatory and oxidative responses in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Our results showed that SYMRKU significantly inhibited LPS-induced secretion of pro-inflammatory mediators including nitric oxide (NO) and prostaglandin $E_2$ without showing any significant cytotoxicity. Consistent with these results, SYMRKU down-regulated LPS-induced expression of their regulatory enzymes such as inducible NO synthase and cyclooxygenase-2. SYMRKU also inhibited LPS-induced production and expression of pro-inflammatory cytokines such as tumor necrosis factor-${\alpha}$, interleukin (IL)-$1{\beta}$ and IL-6. In addition, SYMRKU significantly reduced the production of reactive oxygen species by LPS and showed a strong, which was associated with induction of nuclear factor erythroid 2-related factor 2 and heme oxygenase-1 expression. Although further studies are needed to fully understand the anti-inflammatory effects associated with the antioxidant capacity of SYMRKU, the findings of the current study suggest that SYMRKU may have potential benefits by inhibiting the onset and/or treatment of inflammatory and/or oxidative diseases.

• International Journal of Oral Biology
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• v.45 no.2
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• pp.33-41
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• 2020

Neuroinflammation is known as the main mechanism implicated in the advancement of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. The main feature of neuroinflammation is associated with the activation of microglia. The activated microglia increase proinflammatory cytokine production and induce progressive neuronal cell death. Citrus flavonoids show neuroprotective effects that are associated with the anti-inflammatory action of flavonoids in neurodegenerative diseases. Among these citrus flavonoids, kaempferol, naringin, and nobiletin show inhibitory effects on nuclear factor-κB and mitogen-activated protein kinase signaling pathways that can modulate inflammatory conditions in microglial cells. In the present review, we present the anti-inflammatory activities of citrus flavonoids and therapeutic potential of flavonoids as neuroprotective agents.

• YAKHAK HOEJI
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• v.43 no.1
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• pp.117-123
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• 1999

Because of the potent effects of lipid mediators such as prostaglandins (PGs), leukotriens (LTs) and platelet activating factor (PAF) on a variety of cells and tissues, they are considered as major contributors to the process leading to inflammation and allergy. To pursue the mechanism of anti-inflammatory activity of Lonicera japonica, we tested inhibitory effects of 7 flavonoids from Lonicera japonica on arachidonic acid cascade related enzymes, such as inflammatory phospholipase $A_2$, cyclooxygenase-1 and 2, 5-lipoxygenase, in bone marrow derived mast cell (BMMC), and lyso PAF-acetyltransferase in rat spleen microsomes. Anti-inflammatory activities of lonicera japonica are thought to be attributed at least in part to the inhibition of arachidonic acid cascade releated enzymes by flavonoids such as apigenin, luteolin quercetin.

• Journal of Life Science
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• v.31 no.8
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• pp.736-744
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• 2021

Artemisia princeps Pampanini is an herbal medicine widely used to immune function-related diseases, such as anti-oxidative, anti-inflammatory, and antibacterial agents. In this study, we investigated the anti-inflammatory effects of AP extract and underlying mechanisms were evaluated in RAW 264.7 cells. The effects of AP extract were also studied in a complete Freund's adjuvant (CFA)-induced arthritis and lipopolysaccharide (LPS)-induced inflammation mouse model. In RAW 264.7 cells, AP extracts significantly inhibited the LPS-induced nitric oxide (NO) production and inducible NO synthase and cyclooxygenase-2 protein expression. The LPS-induced phosphorylation of mitogen-activated protein kinases and nuclear factor-κB was also significantly blocked by AP extract in RAW 264.7 cells. Oral administration of AP extract suppressed the increase in mouse paw edema and spleen index compared to CFA-treated mice group. Histologically, the infiltration of inflammatory cells was increased in cartilage and synovium in the CFA-treated mouse group, whereas it was suppressed in the AP extract-administered group. Furthermore, AP extract treatment significantly reduced the inflammatory cytokine, tumor necrosis factor-α, levels in CFA and LPS-treated mouse. In conclusion, the anti-inflammatory and anti-arthritis effect of AP extract was confirmed in both in vitro and in vivo models, suggesting that Artemisia princeps Pampanini may be a candidate material for arthritis treatment.

• The Korea Journal of Herbology
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• v.28 no.2
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• pp.67-73
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• 2013

Objective : Lithospermum Erythrorhizon (LE) has been used as an anti-bacterial and anti-inflammatory agent. However, it is unclear that LE aqueous extract could show the anti-inflammatory effects in RAW 264.7cells. The purpose of this study was to investigate the anti-inflammatory effect of aqueous extract from LE on lipopolysaccharide (LPS) - induced inflammatory response. Methods : To measure out the cytotoxicity of LE, we performed the MTT assay. To evaluate the anti-inflammatory effects of LE, we examined the inflammatory mediators such as nitric oxide (NO), prostaglandin E2 ($PGE_2$) and pro-inflammatory cytokines (tumor necrosis factor (TNF)-${\alpha}$, interleukin, (IL)-$1{\beta}$ and (IL)-6) on RAW 264.7 cells. We also examined molecular mechanisms such as mitogen-activated protein kinases (MAPKs) and nuclear factor-B (NF-${\kappa}B$) activation by western blot. Results : Aqueous Extract from LE itself did not have any cytotoxic effect in RAW 264.7 cells. Aqueous extract from LE inhibited LPS-induced productions of inflammatory mediators such as NO, $PGE_2$, and pro-inflammatory cytokines including TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 in RAW 264.7cells. In addition, LE inhibited the phosphorylation of p38 kinases (p38), c-Jun $NH_2$-terminal kinase (JNK), and NF-${\kappa}B$ activation in RAW 264.7 cells. Conclusion : LE down-regulated LPS-induced production of inflammatory mediators through the inhibition of p38, JNK and NF-${\kappa}B$ activation. Taken together, these results could provide the evidence for the anti-inflammatory effects of LE. Therefore, LE may be a novel target in the management of inflammation and help to support a potential strategy for prevention and therapy of inflammatory diseases.

• Journal of Applied Biological Chemistry
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• v.56 no.4
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• pp.249-255
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• 2013

Recently, algae has been considered as a potential anti-inflammatory source due to its distinctive habitat environment exposing to light and high oxygen concentration. In present study, anti-inflammatory effect of brown alga, Sargassum fullvellum ethanol extract (SFEE), was examined. SFEE inhibited not only the production of nitric oxide and pro-inflammatory cytokines (IL-6, IL-$1{\beta}$, TNF-${\alpha}$) but also the expression of inducible nitric oxide synthase and cyclooxygenase 2 in LPS-induced RAW 264.7 cells without affecting cell viability. SFEE also suppressed the expression of nuclear factor kappa B (NF-${\kappa}B$), suggesting that SFEE could affect the expression of inflammation related cytokines and proteins through the regulation of NF-${\kappa}B$. Furthermore, formation of edema of the ear was 40% lower in mice treated with the highest dose (250 mg/kg) of SFEE than in the control mice. Thus, our study showed that SFEE may be a potential therapeutic anti-inflammatory drug.

• Natural Product Sciences
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• v.23 no.1
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• pp.1-4
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• 2017

Sinensetin, a pentamethoxyflavone, is known to exert various pharmacological activities including anti-angiogenesis, anti-diabetic and anti-inflammatory activities. However, its effects on the human mast cell - 1 (HMC-1) mediated inflammatory mechanism remain unknown. To explore the mediator and cellular inflammatory response of sinensetin, we examined its influence on phorbol 12-myristate 13-acetate (PMA) plus A23187 induced inflammatory mediator production in a human mast cell line. In this study, interleukin (IL)-6 production was measured using the enzyme-linked immunosorbent assay and reverse transcription polymerase chain reaction. Sinensetin inhibited PMA plus A23187 induced IL-6 production in a dose-dependent manner as well as IL-4, IL-5 and IL-8 mRNA expression. Furthermore, sinensetin inhibited signal transducer and activator of transcription 3 (STAT3) phosphorylation, suggesting that sinensetin inhibits the production of inflammatory mediators by blocking STAT3 phosphorylation. Moreover, sinensetin was found to inhibit nuclear factor kappa B activation. These findings suggest that sinensetin may be involved in the regulation of mast cell-mediated inflammatory responses.

• Natural Product Sciences
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• v.27 no.2
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• pp.115-121
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• 2021

Lentinus edodes contains functional metabolites such as polysaccharopeptides, lectins, and secondary metabolites. Fermented soybean paste is representative fermented materials in Korea, and is gradually increasing due to various biological activities. In the present study, ethanol extracts of fermented products with/without L. edodes were designated as SPL and SP, and prepared to develop safer and therapeutic functional foods with antioxidant and anti-inflammatory activities for treatment of inflammatory disorders. SP and SPL extracts exhibited antioxidant effects via inhibiting radical activities. Inflammatory mediators, nitric oxide (NO), prostaglandin E₂ (PGE₂), interleukin (IL)-1β, IL-6, IL-8, tumor necrosis factor (TNF)-α, and inducible nitric oxide synthase (iNOS) production and nuclear factor-kappa B (NF-κB) activation were down-regulated by two extracts. SPL extract more strongly enhanced the antioxidant and anti-inflammatory activities than SP extract. Its' activities shown more longer fermentation period and more strong inhibitory effects. Taken together, our results suggested that fermented product with medicinal plant has synergic effect and SPL can be a potential candidate for treatment of inflammatory bowel diseases.