• Archives of Plastic Surgery
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• 제32권1호
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• pp.5-11
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• 2005

Prostaglandin $E_1$($PGE_1$) is known to have various physiological action such as vasodilatation, decrease of blood pressure, angiogenesis, inhibition of platelet aggregation and so forth. $PGE_1$ has been developed in many different formulations in order to overcome its chemical instability and deactivation in the lungs when administered parenterally. Lipo-AS013 is a potent drug with higher chemical stability and greater vascular wall targeting than others. The study was done on $3{\times}10cm$ model flap of dorsal skin of Sprague-Dawley rats and the flap perfusion survival were observed and documented. The flap treated with Lipo-AS013 beforehand was given intravenously Sodium fluorescein 10 minutes later, and then Percent Dye Fluorescence Index(% DFI) was calculated. The results were compared to a control group and the group administered locally epinephrine.. In the control group, the % DFI and flap survival rate increased from $54.1{\pm}6.7$ to $65.0{\pm}2.6$(p<0.01) while in Lipo-AS013 group from $55.3{\pm}2.2$ to $67.4{\pm}1.9$(p<0.01), respectively. In the epinephrine group, the % DFI(p<0.05) and flap survival rate(p<0.001) decreased. In the both epinephrine and Lipo-AS013 group Percent DFI and flap survival rate are comparable with the control group.The result indicates that the potent Lipo-AS013 enhances the blood flow and flap survival. This highly potent Lipo-AS013 may have targeting ability and accumulate $PGE_1$ onto the vascular walls. A quantitative analysis of fluorescence on the skin surface is a reliable tool to measure the blood perfusion into an ischemic flap and its viability. Further comparative study with conventional $PGE_1$ and Lipo-$PGE_1$ is needed in order to clarify the action and efficiency of Lipo-AS013.

• 생명과학회지
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• 제26권5호
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• pp.537-544
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• 2016

본 연구에서는 보리싹을 이용하여 항산화 활성 및 RAW 264.7 세포에서의 항염증 활성에 미치는 영향을 확인하였다. 보리싹 에탄올 추출물의 DPPH라디칼 소거활성은 1,000 μg/ml 농도에서 92.82±0.62%로 나타났으며, RC₅₀ 값은 442.34±5.54 μg/ml이었다. 보리싹 추출물의 총 폴리페놀과 플라보노이드 함량은 각각 17.55 μg/ml, 13.98 μg/ml로 나타났다. 또한 LPS로 염증을 유도한 RAW 264.7 세포에서 TNF-α와 PGE₂ 생성량은 LPS처리에 따라 증가하였으며, 보리싹 추출물 250, 500 μg/ml의 농도에서 유의적인 감소를 보였다. LPS에 의해 증가된 iNOS, COX-2 단백질 발현에 대해 보리싹 추출물 250 μg/ml의 농도에서 현저히 감소됨을 확인하였다. 이러한 결과들을 통해 보리싹은 항산화 및 항염증 효과를 가진 천연물 소재로 활용 가능할 것으로 생각된다.

• Asian Pacific Journal of Cancer Prevention
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• 제15권22호
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• pp.9967-9972
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• 2014

In order to prove whether downregulation of COX-2 (Cyclooxygenase-2) could modulate the epithelial-mesenchymal transition (EMT) of breast cancer, celecoxib and siRNA were respectively used to inhibit COX-2 function and expression in MDA-MB-231 cells. The EMT reversal effect in the RNAi treated group was better than that of the celecoxib group while there were no obvious differences in the medium $PGE_2$ levels between the two groups. The results show that COX-2 pathways may contribute considerably to EMT of breast cancer cells, partially dependent on the PGE2 cascade. Akt2, ZEB2 and Snail were measured to clarify the underlying mechanisms of COX-2 on EMT; COX-2 may modulate EMT of breast cancer by regulating these factors. This finding may be helpful to elucidate the mechanisms of selective COX-2 inhibitor action in EMT modulation in breast cancer.

• 한국자원식물학회지
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• 제28권3호
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• pp.333-340
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• 2015

This study measured the plasma and liver concentrations of cytokines, the distribution of blood lymphocyte subpopulations (CD4 and CD8), plasma levels of nitrite (NO₃^–) and nitrate (NO₂^–), intercellular adhesion molecule 1 (ICAM-1), cytokine-induced neutrophil chemoattractant 1 (CINC-1), prostaglandin E2 (PGE2), and peritoneal lavage fluid (PLF) levels of monocyte chemotactic protein 1 (MCP-1) and CINC-1 in order to examine the anti-inflammatory activity of the cinnamon extract in lipopolysaccharide (LPS)-exposed rats. The plasma concentrations of interleukin (IL)-1β, IL-6, and tumor necrosis factor α (TNF-α) were lower in the cinnamon extract groups than in the control group at both 2 and 5 h after LPS injection. Furthermore, the liver concentrations of IL-1β, IL-6, and TNF-α were lower in the cinnamon extract groups than in the control group at 5 h after LPS injection. Plasma IL-10 concentrations were higher in the cinnamon extract groups than in the control group at both 2 and 5 h after LPS injection, and liver concentrations of IL-10 did not differ significantly among all treatment groups at 5 h after LPS injection. The distribution of CD4 tended to increase, and that of CD8 tended to decrease in the cinnamon extract groups. The CD4/CD8 ratio was increased in the cinnamon extract groups. The plasma concentrations of NO₃^–/NO₂^–, ICAM-1, CINC-1, and PGE2 and the PLF concentrations of MCP-1 and CINC-1 exhibited a tendency to decrease in the cinnamon extract groups. These results indicate that cinnamon extract can exert functional anti-inflammatory effects.

• Bulletin of the Korean Chemical Society
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• 제35권11호
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• pp.3219-3223
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• 2014

Ochnaflavone, a naturally occurring biflavonoid composed of two units of apigenin (5,7,4'-trihydroxyflavone) joined via a C-O-C linkage, was first synthesized and evaluated its inhibitory activity on $PGE_2$ production. Total synthesis was accomplished through modified Ullmann diaryl ether formation as a key step. Coupling reactions of 4'-halogenoflavones and 3'-hydroxy-5,7,4'-trimethoxyflavone were explored in diverse reaction conditions. The reaction of 4'-fluoro-5,7-dimethoxyflavone (2c) and 3'-hydroxy-5,7,4'-trimethoxyflavone (2d) in N,N-dimethylacetamide gave the coupled compound 3 in 58% yield. Synthetic ochnaflavone strongly inhibited PGE2 production ($IC_{50}=1.08{\mu}M$) from LPS-activated RAW 264.7 cells, which was due to reduced expression of COX-2. On the contrary, the inhibition mechanism of wogonin was somewhat different from that of ochnaflavone although wogonin, a natural occurring anti-inflammatory flavonoid, showed strong inhibitory activity of $PGE_2$ production ($IC_{50}=0.52{\mu}M$), and seems to be COX-2 enzyme inhibition. Our concise total synthesis of ochnaflavone enable us to provide sufficient quantities of material for advanced biological studies as well as to efficiently prepare derivatives for structure-activity relationship study.

• 한국임상수의학회지
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• 제34권3호
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• pp.172-177
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• 2017

Fucoidan, a cell wall polysaccharide found in the brown seaweed, is reported to have broad-spectrum biological activities. The objectives of this study were to examine the effect of fucoidan on prostaglandin $E_2$ ($PGE_2$) and cyclooxygenase-2 (COX-2) expression in lipopolysaccharide (LPS)-stimulated porcine peripheral blood mononuclear cells (PBMCs) and to determine whether these effects are involved in Akt activation. The levels of $PGE_2$ production in the culture supernatants from PBMCs were determined by the enzyme-linked immunosorbent assay (ELISA) kit and the levels of COX-2 mRNA were measured by real time polymerase chain reaction (RT-PCR). Akt activity was determined by Western blot analysis. Fucoidan in LPS-$na{\ddot{i}ve}$ PBMCs has no effect on $PGE_2$ production and COX-2 mRNA expression. Furthermore, fucoidan does not affect Akt activation in LPS- $na{\ddot{i}ve}$ PBMCs. However, $PGE_2$ production and COX-2 mRNA expression on PBMCs were remarkably enhanced by LPS stimulation. Akt activity was also increased by LPS. Increasing effects of $PGE_2$ production and COX-2 mRNA expression in PBMCs induced by LPS were suppressed by addition of fucoidan. In addition, fucoidan reduced an increase in Akt activity in LPS-stimulated PBMCs. These results suggested that fucoidan exerts potent anti-inflammatory properties by suppression of $PGE_2$ production, COX-2 mRNA expression and Akt activation in LPS-stimulated PBMCs.

• BMB Reports
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• 제47권1호
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• pp.45-50
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• 2014

Aspirin has been demonstrated to be effective in inhibiting COX-2 and $PGE_2$ in Alveolar macrophages (AMs). However, the mechanisms have not been fully understood. In the present study, we found that pretreatment with aspirin inhibited LPS-induced COX-2 and$PGE_2$ upregulation, $I{\kappa}B{\alpha}$ degradation, NF-${\kappa}B$ activation and the increase of PKC activity, but elevated LPS-induced the decrease of PTP activity. The PKC inhibitor calphostin C dramatically reduced the COX-2 mRNA and $PGE_2$ levels, but the PTP inhibitor peroxovanadium (POV) significantly increased the COX-2 mRNA and$PGE_2$ levels. Furthermore, the PTP inhibitor mitigated the inhibitory effect of aspirin on COX-2 and$PGE_2$ upregulation and NF-${\kappa}B$ activation, whereas the PKC inhibitor enhanced the inhibitory effects of aspirin on the production of COX-2 and$PGE_2$. Our data indicate a novel mechanism by which aspirin acts as a potent anti-inflammatory agent in alveolus macrophages and ALI.

• 한방안이비인후피부과학회지
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• 제33권2호
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• pp.100-111
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• 2020

Objectives : The aim of experiment is to examine anti-inflammatory effect and anti-oxidant effect of Naesohwangryun-tang (NSHRT) in LPS-stimulated RAW264.7 macrophage cells. Methods : In the present study, The cell viability was performed by MTT assay. Nitric oxide (NO) production and prostaglandin E₂ (PGE₂) synthesis were performed by NO assay and ELISA KIT. The anti-oxidant effect was performed by DPPH and ABTS radical scavenging activity. The inhibitory effects of pro-inflammatory mediators and cytokines were confirmed by realtime PCR and western blotting. Results : NSHRT was no cytotoxicity at treated group. NO and PGE2 production were inhibited compared to the LPS treated group and also mRNA and protein expressions were significantly decreased compared to the LPS treated group. Conclusions : According to the above experiments, we confirmed that NSHRT has anti-inflammatory and anti-oxidant effects. It is suggested that NSHRT is potential ingredient of skin diseases.

• 대한약침학회지
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• 제14권3호
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• pp.81-90
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• 2011

Objectives : Angelicae Gigantis Radix has been known traditional medicine with antimicrobial activities and it has been widely used for treatment of blood and inflammatory diseases. In the present study, some studies examined anti-inflammation effects of Angelicae Gigantis Radix but they usually were performed by ethanol extracted Angelicae Gigantis Radix pharmacopuncture. So We investigated the inhibitory effects of Angelicae Gigantis Radix pharmacopuncture by hot water and ethanol extract on Nitric oxide(NO) and Prostaglandin $E_2$($PGE_2$) production in lipopolysaccharide(LPS) induced macrophage cell. Methods : Angelicae Gigantis Radix was extracted by ethanol and hot water. Cell viability was determined by MTT assay. To evaluate anti-inflammation effects of Angelicae Gigantis Radix pharmacopuncture, we examined NO and $PGE_2$ production in LPS induced macrophages. The concentrations of NO and $PGE_2$ were measured by Griess assay and Enzyme Immuno-Assay. Results : 1) The MTT assay demonstrated that cytotoxic effect of Angelicae Gigantis Radix pharmacopuncture by hot water extract and ethanol extract in RAW 264.7 macrophage cells were not appeared. 2) Angelicae Gigantis Radix pharmacopuncture by ethanol extract and hot water extract inhibited NO production in LPS induced macrophages significantly. 3) Angelicae Gigantis Radix pharmacopuncture by ethanol extract tended to inhibiting $PGE_2$ production in LPS induced macrophages. And Angelicae Gigantis Radix pharmacopuncture by hot water extract inhibited LPS induced production of $PGE_2$ in RAW 264.7 macrophage cells significantly. Conclusions : This study suggests that Angelicae Gigantis Radix pharmacopuncture may have an anti-inflammatory property through the inhibition of NO and $PGE_2$ production in LPS induced macrophages. It may have a therapeutic potential for the treatment of various inflammatory diseases.

• Journal of Dental Anesthesia and Pain Medicine
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• 제22권4호
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• pp.277-287
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• 2022

Background: Inflammatory dental diseases that occur during pregnancy can cause preterm labor and/or intrauterine growth restriction. Therefore, proactive treatment of dental diseases is necessary during pregnancy. Dexmedetomidine (DEX) is a widely used sedative in the dental field, but research on the effect of DEX on pregnancy is currently insufficient. In this study, we investigated the effects of co-treatment with DEX and lipopolysaccharide (LPS) on inflammatory responses in human amnion-derived WISH cells. Methods: Human amnion-derived WISH cells were treated with 0.001, 0.01, 0.1, and 1 ㎍/mL DEX with 1 ㎍/mL LPS for 24 h. Cytotoxicity of WISH cells was evaluated by 3-(4,5-dimethylthiazol)-2,5-diphenyltetrazolium bromide (MTT) assay. The protein expression of cyclooxygenase-2 (COX-2), prostaglandin E₂ (PGE₂), p38, and nuclear factor kappa B (NF-𝜅B) was examined by western blot analysis. The mRNA expression of pro-inflammatory cytokines such as interleukin (IL)-1𝛽 and tumor necrosis factor (TNF)-𝛼 was analyzed by real-time quantitative polymerase chain reaction. Results: Co-treatment with DEX and LPS showed no cytotoxicity in the WISH cells. The mRNA expression of IL-1𝛽 and TNF-𝛼 decreased after co-treatment with DEX and LPS. DEX and LPS co-treatment decreased the protein expression of COX-2, PGE₂, phospho-p38, and phospho-NF-𝛋B in WISH cells. Conclusion: Co-treatment with DEX and LPS suppressed the expression of COX-2 and PGE₂, as well as pro-inflammatory cytokines such as IL-1𝛽 and TNF-𝛼 in WISH cells. In addition, the anti-inflammatory effect of DEX and LPS co-treatment was mediated by the inhibition of p38/NF-𝜅B activation.