• 한국식품과학회지
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• 제39권6호
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• pp.669-675
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• 2007

본 연구자들은 Cumin(Cuminum cymium L.) seed로부터 정제한 $2-hydroxyethyl-{\beta}-undecenate$의 항치주염 활성을 사람의 백혈구를 이용하여 염증 매개물질 $LTB_4$ 및 PGs의 생성 효소인 5-lipoxygenase와 cyclooxygenase, 및 조직파괴 효소인 collagenase와 elastase의 저해 효과를 규명하여 다음과 같은 결론을 얻었다. HPS의 항치주염 활성을 사람의 백혈구를 이용하여 염증 매개물질 $LTB_4$ 및 PGs의 생성 효소인 5-lipoxygenase와 cyclooxygenase 및 조직파괴효소인 collagenase와 elastase의 저해효과를 규명한 결과, HPS은 $5\;{\times}\;10^{-2}\;M$ 첨가 시 97%의 PMNL로부터 $LTB_4$ 생합성이 저해되었으며 이때 $IC_{50}$ 값은 $2\;{\times}\;10^{-4}\;M$ 이었다. 균질화된 사람의 PMNL 5-lipoxygenase 및 시판 정제 5-lipoxygenase 활성에 대한 HPS의 저해 효과는 $5\;{\times}\;10^{-2}\;M$첨가 시 92%의 효소 활성이 저해되었다. 또한 효소 활성에 대한 $IC_{50}$ 값은 $2.5\;{\times}\;10^{-4}\;M$이었으며, 정제 5-lipoxygenase에 대한 $IC_{50}$ 값은 $2.3\;{\times}\;10^{-4}\;M$이었다. 또한 백혈구 COX 활성에 대한 $IC_{50}$ 값은 $5.1\;{\times}\;10^{-4}\;M$이었고, 정제 COX에 대한 $IC_{50}$ 값은 $2.3\;{\times}\;10^{-4}\;M$이었으며, 백혈구 collagenase 활성에 대한 $IC_{50}$ 값은 $2\;{\times}\;10^{-3}\;M$이었고 정제 collagenase에 대한 $IC_{50}$ 값은 $5\;{\times}\;10^{-2}\;M$이었다. 백혈구 elastase의 경우 $5\;{\times}\;10^{-2}\;M$ 첨가 시 66%의 활성이 저해된 반면 정제 elastase의 경우 $5\;{\times}\;10^{-2}\;M$ 첨가 시 25%의 효소 활성이 저해되었다. 또한 백혈구 elastase 활성에 대한 $IC_{50}$ 값은 $7.5\;{\times}\;10^{-3}\;M$이었다. 인체 치은세포에 대한 독성 시험 결과 $5\;{\times}\;10^{-2}\;M$의 HPS 첨가시 세포의 활성은 배양 2일째 47.83%로 나타났으며, $1\;{\times}\;10^{-2}\;M$의 HPS 첨가시에도 68.53%로 나타나 비교적 세포독성이 강한 것으로 나타났다.

• 한방재활의학과학회지
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• 제24권1호
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• pp.31-45
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• 2014

Objectives This study intends to clarify how Leejung-tang (here in after reffered to LJT) affect Wistar Rat whose osteoarthritis was induced by MIA. Methods Osteoarthritis was induced into rat by injecting MIA in its knee joint. Rats are divided into a total of 4 groups (n=6). Normal group are not treated at all without inducing osteoarthritis whereas control group were induced for osteoarthritis by MIA and oral medicated with 2 ml of physiological saline per day. Positive comparison group (Indomethacin) was injected with MIA and after 7 days, 2 mg/kg of Indomethacin was medicated. Experimental group (LJT) was injected with MIA and after 7 days that was medicated with 23 mg/kg of LJT. Indomethacin and LJT were oral medicated for each substance a total of 4 weeks with one time per day. After experiments (from 1 week after injection of MIA to 4 weeks elapsed), Hind paw weight bearing ability, Functions of liver and kidney, Serum prostaglandin $E_2$, TNF-${\alpha}$, IL-1${\beta}$, IL-6, Osteocalcin, TIMP-1, MMP-9, LTB4 and amount of cartilage were measured and histopathological variations for knee joint structures were observed. Results 1) Hind paw weight bearing ability of LJT administration group was increased but there was no statistical significance. 2) Functions of liver and kidney were not affected. 3) Serum prostaglandin $E_2$, IL-1${\beta}$, Osteocalcin, MMP-9 were significantly decreased and TNF-$\alpha$, IL-6, TIMP-1, LTB4 were also decreased but there were no statistical significance. 4) In H&E staining and Safranin-O staining, there were small histopathological changes in LJT administration group than control group. 5) In micro CT (computed tomography)-arthrography, cartilage destruction was more suppressed in LJT administration group than control group. Conclusions Based on all results mentioned above, Leejung-tang (LJT) is believed to be meaningful for suppressing the progress of osteoarthritis and its treatments because of its anti-inflammatory effects and alleviation of pain with histopathological effective efficacy.

• Restorative Dentistry and Endodontics
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• 제15권1호
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• pp.153-164
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• 1990

Human dental pulps obtained from normal teeth, hypersensitive teeth and teeth with inflamed pulp were studied to measure and to compare the endogenous levels of arachidonic acid metabolites in order to see the relative activities of the different pathways involved in arachidonic acid metabolism. Pulp homogenates were incubated with $^{14}C$-arachidonic acid and lipid solvent extracts were separated by thin layer chromatography (TLC) to be analyzed by autoradiography and TLC analyzer. 1. The most significant metabolite was HETEs showing $96.9{\pm}37.8$pmol/mg tissue protein/hr in normal pulp, $169.2{\pm}76.7$ in hypersensitive pulp and $385.4{\pm}113.2$ in inflamed pulp. In normal pulp $LTB_4$, 6-keto-$PGF_{1\alpha}+PGE_2$, $TXB_2$ and unidentified metabolite were formed in decreasing order. While in hypersensitive and inflamed pulp 6-keto-$PGF_{1\alpha}+PGE_2$, $LTB_4$, $TXB_2$ and unidentified metabolite were formed in decreasing order. 2. In hypersensitive pulp only HETEs were significantly increased when compared with that in normal pulp. The levels of all the converted metabolites in inflamed pulp were significantly increased compared with those in normal pulp. In inflamed pulp, the levels of $TXB_2$ and HETEs were significantly increased compared with those in hypersensitive pulp. 3. The ratio of each metabolites to the total converted metabolites showed an increased value of $TXB_2$ and 6-keto-$PGF_{1\alpha}+PGE_2$, as the degree of inflammation was increased, while that of HETEs decreased both in hypersensitive pulp and inflamed pulp more than in normal pulp. 4. The relative amounts of the total metabolites formed in lipoxygenase pathway to cyclo-oxygenase pathway were 6.8 fold in normal pulp, 4.4 fold in hypersensitive pulp and 3.8 fold in inflamed pulp.

• 한방재활의학과학회지
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• 제25권2호
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• pp.51-64
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• 2015

Objectives This study was carried out to investigate the effects of Gyejigabuja-tang extracts on the Monosodium iodoacetate (MIA) induced osteoarthritis in rats. Methods Osteoarthritis was induced by injection of MIA into knee joint cavity of rats. Rats are divided into 4 groups (normal, control, positive comparison group, GBT group, each n=5). Normal group was injected by normal saline into knee joint cavity only. Control group was induced for osteoarthritis by MIA and oral medicated with distilled water. Positive comparison group was injected with MIA and taken Joins tablet 25 mg/kg. GBT group was injected with MIA and taken Gyejigabuja-tang extracts 300 mg/kg. Positive comparison group and GBT group were oral medicated for each substance once a day for 4 weeks. ALT, AST and creatinine were evaluated for hepatotoxicity and nephrotoxicity. Hind paw weight bearing ability was examined and inflammatory cytokines (IL-$1{\beta}$, IL-6, TNF-${\alpha}$), $PGE_2$, $LTB_4$, osteocalcin and deoxypyridinoline (DPD) within serum were analysed. Knee joint structures were observed by Hematoxylin & Eosin (H&E), Safranin-O staining method. Results 1. Function of liver and kidney was not affected. 2. Hind paw weight bearing ability was significantly improved. 3. IL-$1{\beta}$, IL-6 and TNF-${\alpha}$ in experimental group were significantly decreased compared with control group. 4. $PGE_2$, $LTB_4$, Osteocalcin and DPD in experimental group were decreased compared with control group. 5. In histopathologic observation, injury on synovial membrane and cartilage of experimental group was lesser than control group (H&E, Safranin-O staining). Conclusions Based on these results, it can be suggested that Gyejigabuja-tang has anti-inflammation effects on the MIA-induced osteoarthritis in rats.

• 대한의생명과학회지
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• 제27권4호
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• pp.223-230
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• 2021

Tumor necrosis factor alpha (TNF-α) is a principal regulator of inflammation and immunity. The proinflammatory properties of TNF-α can be attributed to its ability to activate the enzyme cytosolic phospholipase A₂ (cPLA₂), which generates potent inflammatory lipid mediators, eicosanoids. L-glutamine (Gln) plays physiologically important roles in various metabolic processes. We have reported that Gln has a potent anti-inflammatory activity via rapid upregulation of mitogen-activated protein kinases (MAPKs) phosphatase (MKP)-1, which preferentially dephosphorylates the key proinflammatory enzymes, p38 MAPK and cytosolic phospholipase A₂ (cPLA₂). In this study, we have investigated whether Gln could inhibit TNF-α-induced cPLA₂ activation. Gln inhibited TNF-α-induced increases in cPLA₂ phosphorylation in the lungs and blood levels of the cPLA₂ metabolites, leukotrine B4 (LTB4) (lipoxygenase metabolite) and prostaglandin E2 (PGE2) (cyclooxygenase metabolite). TNF-α increased p38 and cPLA₂ phosphorylation and blood levels of LTB4 and PGE2, which were blocked by the p38 inhibitor SB202190. Gln inhibited TNF-α-induced p38 and cPLA₂ phosphorylation and production of the cPLA₂ metabolites. Such inhibitory activity of Gln was no longer observed in MKP-1 small interfering RNA-pretreated animals. Our data indicate that Gln inhibited TNF-α-induced cPLA₂ phosphorylation through MKP-1 induction/p38 inhibition, and suggest that the utility of Gln in inflammatory diseases in which TNF-α plays a major role in their pathogenesis.

• 대한한방내과학회지
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• 제39권4호
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• pp.480-494
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• 2018

Objectives: To investigate the effect of fermented extract of Artemisiae Iwayomogii Herba, Curcumae Longae, Crataegi Fructus and Salviae Miltiorrhizae Radix (FMH) on anti-inflammation associated with dyslipidemia and anti-oxidation in RAW264.7 and HUVEC cells. Methods: The total polyphenols, total flavonoids, DPPH radical scavenging activity, ABTS radical scavenging activity, and cytotoxicity of FMH were measured. RAW264.7 cells treated with FMH were tested for production of NO, and for cytokine and LTB4 levels and HUVEC cells treated with FMH were examined for production of cDNA of genes related to inflammation. Results: 1. FMH contained polyphenols and flavonoids. The DPPH and ABTS radical scavenging activity of FMH increased in a concentration-dependent manner. 2. FMH treatment inhibited the production of nitric oxide (NO), cytokines, and LTB4 in RAW264.7 cell when compared to the untreated control group. 3. FMH decreased the transcription of pro-inflammatory genes, whereas it increased transcription of anti-inflammatory genes, in HUVEC cells. Conclusion: FMH is effective as an antioxidant and for treatment and prevention of dyslipidemia, atherosclerosis, ischemic heart disease, stroke, and other cardiocerebrovascular diseases.

• The Korean Journal of Physiology and Pharmacology
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• 제16권5호
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• pp.313-320
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• 2012

In this study, we focused to identify whether eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone), an extract from Artemisia argyi folium, prevents $H_2O_2$-induced injury of cultured feline esophageal epithelial cells. Cell viability was measured by the conventional MTT reduction assay. Western blot analysis was performed to investigate the expression of 5-lipoxygenase by $H_2O_2$ treatment in the absence and presence of inhibitors. When cells were exposed to 600 ${\mu}M$ $H_2O_2$ for 24 hours, cell viability was decreased to 40%. However, when cells were pretreated with 25~150 ${\mu}M$ eupatilin for 12 hours, viability was significantly restored in a concentration-dependent manner. $H_2O_2$-treated cells were shown to express 5-lipoxygenase, whereas the cells pretreated with eupatilin exhibited reduction in the expression of 5-lipoxygenase. The $H_2O_2$-induced increase of 5-lipoxygenase expression was prevented by SB202190, SP600125, or NAC. We further demonstrated that the level of leukotriene $B_4$ ($LTB_4$) was also reduced by eupatilin, SB202190, SP600125, NAC, or nordihydroguaiaretic acid (a lipoxygenase inhibitor) pretreatment. $H_2O_2$ induced the activation of p38MAPK and JNK, this activation was inhibited by eupatilin. These results indicate that eupatilin may reduce $H_2O_2$-induced cytotoxicity, and 5-lipoxygenase expression and $LTB_4$ production by controlling the p38 MAPK and JNK signaling pathways through antioxidative action in feline esophageal epithelial cells.

• Molecules and Cells
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• 제44권12호
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• pp.893-899
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• 2021

BLT2 is a low-affinity receptor for leukotriene B₄, a potent lipid mediator of inflammation generated from arachidonic acid via the 5-lipoxygenase pathway. The aim of this study was to investigate whether BLT2 plays any role in sepsis, a systemic inflammatory response syndrome caused by infection. A murine model of cecal ligation and puncture (CLP)-induced sepsis was used to evaluate the role of BLT2 in septic inflammation. In the present study, we observed that the levels of ligands for BLT2 (LTB₄ [leukotriene B₄] and 12(S)-HETE [12(S)-hydroxyeicosatetraenoic acid]) were significantly increased in the peritoneal lavage fluid and serum from mice with CLP-induced sepsis. We also observed that the levels of BLT2 as well as 5-lipoxygenase (5-LO) and 12-LO, which are synthesizing enzymes for LTB₄ and 12(S)-HETE, were significantly increased in lung and liver tissues in the CLP mouse model. Blockade of BLT2 markedly suppressed the production of sepsis-associated cytokines (IL-6 [interleukin-6], TNF-α [tumor necrosis factor alpha], and IL-1β [interleukin-β] as well as IL-17 [interleukin-17]) and alleviated lung inflammation in the CLP group. Taken together, our results suggest that BLT2 cascade contributes to lung inflammation in CLP-induced sepsis by mediating the production of inflammatory cytokines. These findings suggest that BLT2 may be a potential therapeutic target for sepsis patients.

• 한국자기공명학회논문지
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• 제8권2호
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• pp.70-76
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• 2004

ZORA-DFT calculations of $^{11}$B EFG (electric field gradient) tensors for lithium borates, LiB$_3O_5$ (LBO) and Li$_2B_4O_7$ (LTB), were performed. The calculated values of 11B quadrupole coupling constant and asymmetry parameter are in good agreement with the experimental values. The sign of the quadrupole coupling constant for the tetrahedral boron site was deduced from the distortion from the ideal tetrahedral symmetry.

• 동의생리병리학회지
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• 제31권1호
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• pp.46-51
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• 2017

The aim of this study is to investigate anti-arthritis activity using a KV pharmacopuncture. KV pharmacopuncture was inserted at BL40 for 4 weeks to SD-Rat, where arthritis was induced by monosodium iodoacetate (MIA) at 60 mg/ml. MMP-9, CTX II, LTB4, calcitonin and glycosaminoglycan level in serum were measured by ELISA. The cartilage of patella volume was examined and 3-D high-resolution reconstructions of the cartilage of patella were obtained using a Micro-CT system. Also, The histopathological change of knee was observed by H&E and safranin-O staining. Production of MMP-9, CTX II and LTB4 level in serum was decreased, respectively, in comparison with control. The other way, production of calcitonin and glycosaminoglycan level in serum was increased, respectively, in comparison with control. The cartilage of patella volume increased significantly. In addition, the KV group showed a increase in the cartilage volume and proteoglycan. These results may be used a remedy for new korea medicine to ease the symptoms mentioned above.