• 대한본초학회지
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• 제27권1호
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• pp.41-49
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• 2012

Objectives : The purpose of this study was to investigate the anti-oxidative and anti-atopic dermatitis effects of persimmon leaf extract obtained from Cheongdo-gun, where more than 60% of Korean persimmon is produced. Methods : Anti-oxidative effects of the crude persimmon leaf extract harvested monthly between May and November were determined by in vitro assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and superoxide dismutase (SOD)-like reaction. Anti-atopic dermatitis effects of the crude persimmon leaf extract were determined by using collagenase type I inhibition assay and by quantitative assays including serum histamine, prostaglandin E metabolite and leukotriene $B_4$ levels in animal model of atopic dermatitis using Balb/c mice. Results : Persimmon leaf extract harvested in May had higher levels of total phenolic compounds (182.24 mg/g) and flavonoids (23.05 mg/g) than the ones of different month extract. Also, persimmon leaf extract harvested in May showed the most effective extract scavenging activities of DPPH free radical ($13.39{\pm}0.21\;{\mu}g/ml$) and superoxide anion radical ($40.52{\pm}2.32\;{\mu}g/ml$), leading to use the persimmon leaf extract harvested in May for the experiments hereafter. Persimmon leaf extract showed $326.71{\pm}4.6\;{\mu}g/ml$ of 50% inhibitory concentration ($IC_{50}$) for collagenase type I which is responsible for the degradation of extracellular matrix. In addition, persimmon leaf extract application group could decrease serum levels of histamine, prostaglandin E metabolite and leukotriene $B_4$ compared to the negative control in animal model of atopic dermatitis. Especially, persimmon leaf extract showed a significantly decreased serum leukotriene $B_4$ level relative to the levels of histamine and prostaglandin E metabolite. Conclusions : Persimmon leaf extract showed anti-oxidative and anti-atopic dermatitis effects in vitro and in vivo. These results suggest that persimmon leaf extract may have immunoregulatory function for alleviating atopic dermatitis by decreasing collagenase activity and mast cell activation.

• The Korean Journal of Pain
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• 제32권3호
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• pp.168-177
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• 2019

Background: Brennan's rodent paw incision model has been extensively used for understanding mechanisms underlying postoperative pain in humans. However, alterations of physiological parameters like blood pressure and heart rate, or even feeding and drinking patterns after the incision have not been documented as yet. Moreover, though eicosanoids like prostaglandins and leukotrienes contribute to inflammation, tissue levels of these inflammatory mediators have never been studied. This work further investigates the antinociceptive effect of protein C after intra-wound administration. Methods: Separate groups of Sprague-Dawley rats were used for quantitation of cyclooxygenase (COX) activity and leukotriene B4 level by enzyme-linked immunosorbent assay, as well as estimation of cardiovascular parameters and feeding and drinking behavior after paw incision. In the next part, rats were subjected to incision and $10{\mu}g$ of protein C was locally administered by a micropipette. Both evoked and non-evoked pain parameters were then estimated. Results: COX, particularly COX-2 activity and leukotriene B4 levels increased after incision. Hemodynamic parameters were normal. Feeding and drinking were affected on days 1 and 3, and on day 1, respectively. Protein C attenuated non-evoked pain behavior alone up to day 2. Conclusions: Based upon current observations, Brennan's rodent paw incision model appears to exhibit a prolonged period of nociception similar to that after surgery, with minimal interference of physiological parameters. Protein C, which is likely converted to activated protein C in the wound, attenuated the guarding score, which probably represents pain at rest after surgery in humans.

• Biomolecules & Therapeutics
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• 제22권1호
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• pp.27-34
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• 2014

Curcumin is naturally occurring polyphenolic compound found in turmeric and has many pharmacological activities. The present study was undertaken to evaluate anti-allergic inflammatory activity of curcumin, and to investigate its inhibitory mechanisms in immunoglobulin E (IgE)/Ag-induced mouse bone marrow-derived mast cells (BMMCs) and in a mouse model of IgE/Ag-mediated passive systemic anaphylaxis (PSA). Curcumin inhibited cyclooxygenase-2 (COX-2) dependent prostaglandin $D_2$ ($PGD_2$) and 5-lipoxygenase (5-LO) dependent leukotriene $C_4$ ($LTC_4$) generation dose-dependently in BMMCs. To probe the mechanism involved, we assessed the effects of curcumin on the phosphorylation of Syk and its downstream signal molecules. Curcumin inhibited intracellular $Ca^{2+}$ influx via phospholipase $C{\gamma}1$ ($PLC{\gamma}1$) activation and the phosphorylation of mitogen-activated protein kinases (MAPKs) and the nuclear factor-${\kappa}B$ (NF-${\kappa}B$) pathway. Furthermore, the oral administration of curcumin significantly attenuated IgE/Ag-induced PSA, as determined by serum $LTC_4$, $PGD_2$, and histamine levels. Taken together, this study shows that curcumin offers a basis for drug development for the treatment of allergic inflammatory diseases.

• 대한약리학회지
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• 제31권1호
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• pp.123-133
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• 1995

삼환계 항우울제들은 calmodulin 억제 작용을 갖고 있으며, 칼슘 유입, 산화성 인산화 반응 및 ATPase 활성도를 억제하는 것으로 제시되고 있지만 사람 호중구에서의 기능 표현에 대한 효과는 밝혀져 있지 않다. 본 연구에서는 amitriptyline, imipramine과 doxepine이 superoxide와 $H_2O_2$ 생성, myeloperoxidase 유리, leukotriene $B_4$ 생성과 세포내 칼슘의 상승에 나타나는 효과를 조사하였다. 변성된 IgG에 의하여 활성화된 호중구에서 superoxide와 $H_2O_2$ 생성은 amitriptyline, imipramine과 doxepine에 의하여 억제되었고 EDTA, EGTA, verapamil과 bepredil은 superoxide 생성을 억제하였다. Chlorpromazine, trifluoperazine, staurosporine 및 H-7 또한 superoxide 생성을 억제하였다. PMA에 의한 superoxide 생성은 amitriptyline, imipramine과 doxepine, chlorpromazine과 H-7에 의하여 억제되었다. Amitriptyline, imipramine, chlorpromazine과 trifluoperazine은 변성된 IgG에 의한 myeloperoxidase 유리를 억제하였다. 변성된 IgG에 의하여 활성화된 호중구에서 $LTB_4$와 5-HETE 형성은 amitriptyline, imipramine과 doxepine에 의하여 억제되었다. 변성된 IgG에 의한 세포내 칼슘의 증가는 amitriptyline, imipramine, doxepine, chlorpromazine과 EGTA에 의하여 억제되었고, verapamil은 세포내 칼슘의 증가를 약간 억제하였으나 H-7은 세포내 칼슘의 증가에 영향이 없었다. 이상의 결과로부터 변성된 IgG에 의하여 활성화된 호중구에서의 respiratory burst, myeloperoxidase 유리와 LTB, 생성에 대한 amitriptyline, imipramine과 doxepine의 억제효과는 칼슘동원, calmodulin과 protein kinase C의 억제에 기인할 것으로 추정된다.

• Restorative Dentistry and Endodontics
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• 제21권2호
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• pp.451-469
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• 1996

The purpose of this study was to investigate the effect of calcium hydroxide and glass ionomer cement fillings on the levels of $LTB_4$ and $LTC_4$ in experimentally inflamed rat dental pulp. The dental pulp in the mandibular incisor of wistar rat was irritated by cutting a 5mm deep hole in the dentin with a twist drill bur of 0.5mm diameter, without cooling. The cavities were filled with calcium hydroxide(light-cured) and glass ionomer cement(light cured). The untreated pulp served as control tissue specimen. After cavity preparations, the rat with or without various treatment were sacrificed in various time by decapitation. The dental pulp tissue were carefully removed and the concentrations of $LTB_4$ and $LTC_4$ were determined by radioimmunoassay. And pulps were examined histologically to observe inflammatory feature. The result were obtained as follows : 1. The inflammatory features of pulps were observed microscopically in all experimental groups. And degree of inflammation was decreased with time. 2. The concentrations of $LTB_4$ and $LTC_4$ for all experimental groups were significantly higher than those for control group 6 hours after cavity preparation(p<0.05). 3. The group filled with calcium hydroxide was the lowest, and the group filled with glass ionomer cement, the group of irritation in that order showed increased concentrations of $LTB_4$ and $LTC_4$ 6 hours after cavity preparation. In the concentrations of $LTB_4$, significant differences among 3 groups were noted(p<0.05). 4. The group filled with calcium hydroxide was the lowest, and the group filled with glass ionomer cement, the group of irritation in that order showed increased concentrations of $LTB_4$ and $LTC_4$ 24 hours after cavity preparation. And there were statistically significant difference in concentrations of $LTB_4$ between the group of irritation and the group filled with calcium hydroxide(p<0.05). 5. The group filled with calcium hydroxide was the lowest, and the group filled with glass ionomer cement, the group of irritation in that order showed increased concentrations of $LTB_4$ and $LTC_4$ 48 hours after cavity preparation. But no statistically difference was found (p>0.05). 6. The concentrations of $LTB_4$ and $LTC_4$ in all experimental groups were highest level at 6 hour after experiment and decreased as time progresses(correlation coefficient>0.8).

• 약학회지
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• 제55권4호
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• pp.295-300
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• 2011

We investigated the effects of butanol fraction of Asterias amurensis (BFA) on the anti-allergic activity. BFA inhibited both cyclooxygenase-2 dependent prostaglandin $D_2$ and 5-lipoxygenase dependent leukotriene $C_4$ generation in a concentration-dependent manner with $IC_{50}$ values of 174.6 and 22.2 ${\mu}g$/ml, respectively. In addition, BFA also inhibited the degranulation in a dose dependent manner. Furthermore, oral administration of BFA inhibited IgE-mediated passive cutaneous anaphylaxis in mice. These results suggested that BFA may be useful in regulating mast cell-mediated allergic diseases.

• 대한한방부인과학회지
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• 제34권3호
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• pp.29-48
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• 2021

Objectives: Banchong-san (BCS) is a herbal formula composed of 13 korean medicinal herbs and is traditionally used to treat inflammatory diseases and pain. The object of this study was to research the antioxidant, anti-inflammatory, antipruritic and antimicrobial effects of the BCS in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Methods: In this experiment, effects of BCS on the following four were measured as follows: (1) Anti-oxidative effects were evaluated by 1,1-diphenyl-2-picryl-hydrazyl (DPPH) Radical scavenging activity, 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) Radical scavenging activity. (2) Anti-inflammatory effects were evaluated by the production amount of Reactive oxygen species (ROS), Nitric oxide (NO), Interleukin-1β (IL-1β), Interleukin 6 (IL-6), tumor necrosis factor-α (TNF-α), Prostaglandin E2 (PGE₂), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2)(the previous two are "mRNA"), extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), p38 mitogen-activated protein kinases (p38), inhibitor of nuclear factor kappa B (IκBα), nuclear factor kappa B (NF-κB) (the previous five are "Protein") in LPS-Stimulated RAW 264.7 cells. (3)Antipruritic effects were evaluated by the production amount of histamine, Leukotriene B4 (LTB4), LeukotrieneC4 (LTC4) Levels in phorbol 12-myristate 13-acetate(PMA)/ionomycin-stimulated MC/9 mast cell. (4) Anti-microbial effects were evaluated by the growth suppression of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Aspergillus niger. Results: The following results were obtained through each measurement: (1) DPPH Radical Scavenging Activity, ABTS Radical Scavenging Activity evoked a significant concentration-dependent increase. (2) ROS, NO, IL-1β, IL-6, TNF-α, PGE₂ production amount, iNOS, COX-2 mRNA expression were significantly reduced in the BCS extraction group compared with the control group and significantly decreased the amount of ERK, JNK, p38, NF-κB Protein expression. The amount of IκB-α Protein Expression have increased significantly. (3) The amounts of histamine, LTB4, LTC4 were significantly decreased. (4) The antibacterial efficacy, BCS inhibited the growth of Escherichia coli, Pseudomonas aeruginosa at concentrations of 5 ㎍/ml, but did not suppress the growth of staphylococcus aureus and aspergillus niger. Conclusions: The experimental results show that BCS has anti-oxidant, anti-inflammatory, antipruritic and antimicrobial properties.

• Bulletin of the Korean Chemical Society
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• 제31권1호
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• pp.199-201
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• 2010

• Biomolecules & Therapeutics
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• 제17권1호
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• pp.86-91
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• 2009

In our ongoing search for biological components from the Korea endemic plants, the MeOH extract of Ailanthus altissima leaves (Simaroubaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). In further study, eight compounds, squalene (1), ${\beta}$-sitosterol (2), scopoletin (3), quercetin (4), luteolin (5), astragalin (6), scopolin (7), and daucosterol (8) were isolated, the chemical structures were elucidated on the basis of physicochemical and spectroscopic data and by comparison with those of published literatures. Among the compounds, 2, 4, and 5 strongly inhibited both the COX-2-dependent PGD2 generation with $IC_{50}$ values of 2.6, 7.3 and 2.5 ${\mu}M$, respectively and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 2.0, 5.1 and 1.8 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of A. altissima might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 2, 4 and 5.

• 대한치과교정학회지
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• 제24권4호
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• pp.871-883
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• 1994

This experiment was designed to study possible roles of $interleukin-1\beta$, interleukin-6 and tumor necrosis $factor-\alpha$ in bone remodeling by measuring their effects on $PGE_2,\; LTB_4$ and collagenase production when they were administered to human periodontal ligament fibroblasts. Human periodontal ligament fibroblasts were collected from first premolars extracted for orthodontic treatment. They were incubated in the environment of $37^{\circ}C,\;5\%\;Co^2,\;and\;100\%$ humidity. They were treated with $0.25\%$ trypsin-EDTA solution and centrifuged. PDL cells in the fifth to seventh passage were used for the experiment. Cells were seeded onto the culture dishes and when they were successfully attached, human recombinant $interleukin-1\beta$, interleukin-6, and tumor necrosis $factor-\alpha$ were administered, alone or in combination. They were incubated for 4, 8 and 24 hours and the levels of $PGE_2,\;LTB_4$ and collagenase released into the culture media were assessed by enzymeimmunoassay and collagenase activity assay. The conclusions are as follows: 1. $IL-1\beta\;and\;TNF-\alpha$ were very active in stimulating the production of $PGE_2$ and collagenase by human periodontal ligament fibroblasts, while IL-6 increased $LTB_4$ production. 2. $IL-1\beta$ significantly increased $PGE_2$, but $LTB_4$ Production was not increased. $IL-1\beta$ is thought to act mainly via the cyclooxygenase pathway of arachidonic acid metabolism. 3. IL-6 tended to inhibit $IL-1\beta$ in the production of $PGE_2$ and collagense whereas IL-6 and $TNF-\alpha$ showed auditive effect in the level of $PGE_2$. The above cytokines increased the release of at least one of $PGE_2,\;LTB_4$ and collagenase. It suggests that cytokines are involved in bone remodeling process by stimulating PDL fibroblasts to produce various bone-resorptive agents. The roles of cytokines in bone remodeling as a whole would need further study.