• Journal of Integrative Natural Science
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• v.7 no.3
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Archives of Pharmacal Research
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• v.27 no.2
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• pp.189-193
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• 2004

Clerodendron trichotomum Thunberg Leaves (CTL) have been used for centuries in Chinese folk medicine for their anti-inflammatory properties. We have studied the anti-inflammatory effects of CTL extracts in rats, mice and in Raw 264.7 cells. 1 mg/kg solutions of the 30％ and 60％ methanol extracts of CTL were used and a 1 mg/kg of indomethacin was used as a positive anti-inflammatory standard; these were then administrated to rats. Carrageenan was injected subcutaneously to induce hind paw edema in rats. The result of carrageenan-induced rat paw oedema showed that a 1 mg/kg of the 30％, and 60％ methanol fraction of CTL and 1 mg/kg of indomethacin inhibited the hind paw edema by 19.5％, 23.0％, and 20.5％ respectively. The effect of CTL on inflammation in mice by a capillary permeability assay was examined by detecting Evans blue leakage from capillaries after the intraperitoneal injection of acetic acid, a potent inflammatory stimulus. The 60％ methanol fraction of CTL inhibited Evans blue dye leakage by 47.0％, which was 10％ higher than that of the inhibition of 1 mg/kg of indomethacin. Also, the 60％ methanol fraction of CTL suppressed the prostaglandin $E_2$ ($PGE_2$) generation in RAW 264.7 macrophage cells after treatment with lipopolysaccharide (LPS) by as much as the inhibition of 1 mg/kg of indomethacin and this led to the synthesis of $PGE_2$ by COX-2 induction. The inhibition of the carrageenan-induced rat paw oedema, vascular permeability and the $PGE_2$ generation demonstrates that the 60％ methanol fraction of CTL contains a potent anti-inflammatory activity.

• The Korea Journal of Herbology
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• v.37 no.5
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• pp.83-88
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• 2022

Objectives : Jakyakgamcho-tang (JGT) has been traditionally used to treat muscular convulsion and pain in South Korea. According to recent studies, JGT has been reported to have anti-depression, anti-inflammation, anti-oxidative, anti-diabetics, anti-spasm and analgesic effects, but studies on its anti-neuroinflammatory and neuroprotective effect have not been deeply conducted. Thus, we investigated the anti-neuroinflammatory activity of JGT on lipopolysaccharide (LPS)-stimulated mouse microglia cells. Methods : To investigate the anti-neuroinflammatory effects of JGT on BV2 microglial cells, we examined the production of nitric oxide (NO) using griess assay, and mRNA expressions of pro-inflammatory cytokines such as interleukin (IL)-1𝛽, IL-6, and tumor necrosis factor (TNF)-𝛼 using real time RT-PCR. Furthermore, to determine the regulating mechanisms of JGT, we investigated the heme oxygenase (HO)-1 by real time RT-PCR. Results : Pre-treatment of JGT effectively decreased NO production in LPS-stimulated BV2 cells at concentrations without cytotoxicity. Additionally, JGT significantly suppressed the production of IL-1𝛽, IL-6, and TNF-𝛼 in LPS-stimulated BV2 cells. Furthermore, JGT activated the HO-1 expression, which is one of the immunomodulatory signaling molecules. And the abolishment of HO-1 by tin protoporphyrin IX (SnPP, the HO-1 inhibitor) reversed the anti- inflammatory activity of JGT in LPS-stimulated BV2 cells. Conclusions : Our results suggest that the JGT has anti-neuroinflammatory effect through the activation of HO-1 in LPS-stimulated BV2 cells. Thereby, JGT could expected to be used for the prevention and treatment of neurodegenerative disease related to neuroinflammation.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.5
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• pp.439-448
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• 2021

DA-9601 is an extract obtained from Artemisia asiatica, which has been reported to have anti-inflammatory effects on gastrointestinal lesions; however, its possible anti-inflammatory effects on the small intestine have not been studied yet. Therefore, in this study, we investigated the protective effects of DA-9601 against the ACF-induced small intestinal inflammation. Inflammation of the small intestine was confirmed by histological studies and the changes in the CD4⁺ T cell fraction induced by the inflammation-related cytokines, and the inflammatory reactions were analyzed. Multifocal discrete small necrotic ulcers with intervening normal mucosa were frequently observed after treatment with ACF. The expression of IL-6, IL-17, and TNF-α genes was increased in the ACF group; however, it was found to have been significantly decreased in the DA-9601 treated group. In addition, DA-9601 significantly decreased the levels of proinflammatory mediators such as IL-1β, GM-CSF, IFN-γ, and TNF-α; the anti-inflammatory cytokine IL-10, on the other hand, was observed to have increased. It is known that inflammatory mediators related to T cell imbalance and dysfunction continuously activate the inflammatory response, causing chronic tissue damage. The fractions of IFN-γ⁺ Th1 cells, IL-4⁺ Th2 cells, IL-9⁺ Th9 cells, IL-17⁺ Th17 cells, and Foxp3⁺ Treg cells were significantly decreased upon DA-9601 treatment. These data suggest that the inflammatory response induced by ACF is reduced by DA-9601 via lowering of the expression of genes encoding the inflammatory cytokines and the concentration of inflammatory mediators. Furthermore, DA-9601 inhibited the acute inflammatory response mediated by T cells, resulting in an improvement in ACF-induced enteritis.

• Journal of Sasang Constitutional Medicine
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• v.22 no.4
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• pp.56-64
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• 2010

1. Objectives 4 herbal formulas (Yanggyeoksanhwa-tang, Yeoldahanso-tang, Cheongsimyeonja-tang and Taeeumjowi-tang) were applied to investigate the anti-inflammatory activities. In many studies, plant-derived anti-inflammatory efficacies have been investigate for their potential inhibitory effects on lipopolysaccharide (LPS)-stimulated macrophages. This study was performed to examine the anti-inflammatory activities of 4 herbal formulas on LPS-stimulated RAW 264.7 cells. 2. Methods The productions of nitric oxide (NO), prostaglandin (PG)$E_2$, interleukin(IL)-6 and tumor necrosis factor (TNF)-${\alpha}$ were examined in the presence of the 4 herbal formulas in RAW 264.7 cells. The cells were incubated with LPS 1 ${\mu}g/mL$ and 4 herbal formulas for 18 hrs. The anti-inflammatory activity of 4 herbal formulas were investigate by carrageenin-induced paw edema in rats. The paw volume was measured at 2 and 4 hrs following carrageenininduced paw edema in rats. 3. Results Yanggyeoksanhwa-tang and Cheongsimyeonja-tang showed inhibitory effect on $PGE_2$ production in LPS-stimulated RAW 264.7 cells and a reduction in carrageenin-induced paw edema on rats. Yanggyeoksanhwa-tang showed inhibitory effect on IL-6 in LPS-stimulated RAW 264.7 cells. 4 herbal formulas not affect on NO and TNF-${\alpha}$ inhibition in LPS-stimulated RAW 264.7 cells. 4. Conclusions These results suggested that Yanggyeoksanhwa-tang and Cheongsimyeonja-tang have anti-inflammatory activity.

• The Journal of Korean Medicine
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• v.31 no.3
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• pp.47-54
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• 2010

Objective: To derive information on the efficacy of Sam-chul-kun-bi-tang (SKT), by evaluating its anti-inflammatory effect. SKT is a widely-used herbal formula in traditional Korean medicine. In man y studies, plant-derived anti-inflammatory efficacies have been investigated for their potential inhibitory effects on lipopolysaccharide (LPS)-stimulated macrophages. This study was performed to examine the anti-inflammatory effects of SKT extract on LPS-stimulated RAW 264.7 cells. Methods: The production of nitric oxide (NO), prostaglandin $(PG)E_2$, tumor necrosis factor (TNF)-$\alpha$ and interleukin (IL)-6 were examined in a macrophage cell line, RAW 264.7 cells, in the presence of SKT. RAW 264.7 cells were incubated with LPS 1 ${\mu}g/mL$ and SKT for 18 hrs. The anti-inflammatory activity of SKT was investigated by carrageenan-induced paw edema in rats. The paw volume was measured at 2 and 4 hrs following carrageenan-induced paw edema in rats. Results: SKT showed inhibitory effect on $PGE_2$, TNF-$\alpha$ and IL-6 in LPS-stimulated RAW 264.7 cells. But SKT was not inhibitory effect on NO by LPS-stimulated RAW 264.7 cells. Administration of SKT (1 g/kg) also showed a reduction in carrageenan-induced paw edema on rats. Conclusion: These results suggest that SKT has anti-inflammatory activities in both in vitro and in vivo models.

• Journal of Physiology & Pathology in Korean Medicine
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• v.34 no.5
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• pp.238-244
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• 2020

Yangdan-tang (YD) is recorded as a treatment to treat exterior-related fever illness in the Korean medicine. In this study, we examined the anti-inflammatory effects of YD, using YD water extract and lipopolysaccharide (LPS)-induced RAW 264.7 cells. First of all, we measured the amount of nitric oxide (NO) and prostaglandin E2 (PGE2), the products of inflammatory metabolism. Also, we measured enzymes such as inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), as well as cytokines such as tumor necrosis factor alpha (TNF-α), interleukin 6 (IL-6), interleukin 1 alpha (IL-1α), and interleukin 1 beta (IL-1β). YD suppressed the production of NO and PGE2 in a dose dependent manner and reduced the amount of protein and the mRNA expression of iNOS and COX-2. Also, YD reduced the mRNA expression of TNF-α, IL-6, IL-1α and IL-1β. In conclusion, YD decreased production of LPS-induced inflammatory factor, which could be a clinical basic subject for inflammatory diseases.

• Journal of Physiology & Pathology in Korean Medicine
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• v.34 no.6
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• pp.319-325
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• 2020

Mahwanghangingamchosukgo-tang (MH) is recorded as a treatment to treat exterior-related respiratory diseases in the Korean medicine. In this study, we examined the anti-inflammatory effects of MH, using MH water extract and lipopolysaccharide (LPS)-induced RAW 264.7 cells. First of all, we measured the amount of nitric oxide (NO) and prostaglandin E2 (PGE2), the products of inflammatory metabolism. Also, we measured enzymes such as inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), as well as cytokines such as interleukin 6 (IL-6), interleukin 1 alpha (IL-1α), and interleukin 1 beta (IL-1β). MH suppressed the production of NO and PGE2 in a dose dependent manner and reduced the amount of protein and the mRNA expression of iNOS and COX-2. Also, MH reduced the mRNA expression of IL-6, IL-1α and IL-1β. In conclusion, MH decreased production of LPS-induced inflammatory factor, which could be a clinical basic subject for inflammatory diseases.

• Archives of Pharmacal Research
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• v.8 no.2
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• pp.59-65
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• 1985

Besides (-) pimara-8(14), 15-dien-19-oic acid [I] which had already been isolated as an active anti-inflammtory principle of Aralia continentalis, (-) kaur-16-en-19-oic acid [II] was separated as another active component of the plant, by tracing albumin stabilizing activity. $IC_{50}$ of [II] for the protein stabilizing activity was 0.026mg/3ml, when those of [I] and phenylbutazone were 0.032 and 0.32 mg/3ml, respectively. Being investigated employing carrageenin-induced edema test in rat hind paw, the anti-inflammatory activity of [II] administered s. c. was slightly lower than that of phenylbutazone, whereas the activity of [II] administered p. p. was three times greater than that of phenylbutazone. These results of [II] were contrary to those of [I] in the aspect of administration routes.

• Natural Product Sciences
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• v.25 no.1
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• pp.34-37
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• 2019

Phytochemical studies were performed to identify the active principles of Phryma leptostachya var. asiatica (Phyrymaceae) for anti-inflammation. The anti-inflammatory activity was assessed by measuring the inhibition rate on nitric oxide (NO) formation in lipopolysaccharide (LPS)-activated macrophage 264.7 cells. Of the five compounds including ursolic acid, phrymarolin I, harpagide, haedoxancoside A, and acteoside isolated from this plant, ursolic acid showed the most prominent inhibition of NO formation. Therefore, ursolic acid may be the anti-inflammatory principle of Phryma leptostachya var. asiatica.