• Title/Summary/Keyword: Anti-inflammatory agent

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Synthesis of Bufexamac (Bufexamac의 합성)

  • Choi, Hong-Dae;Ma, Jung-Jeo
    • YAKHAK HOEJI
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    • v.34 no.3
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    • pp.212-214
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    • 1990
  • A new synthetic method for bufexamac, which is a potent anti-inflammatory agent, was described. Friedel-Crafts reaction of butoxybenzene (2) with ethyl ${\alpha}-chloro-{\alpha}-(methylthio)acetate$ (1) gave ethyl 2-methylthio-2-(p-butoxyphenyl) acetate (3). Ethyl 2-(p-butoxyphenyl)acetate (4) was prepared by desulfurization of compound (3) with zinc dust-acetic acid. Bufexamac (5) could be easily synthesized by treatment of compound (4) with hydroxylamine HCl.

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A Pharmacological Review on Portulaca oleracea L.: Focusing on Anti-Inflammatory, Anti- Oxidant, Immuno-Modulatory and Antitumor Activities

  • Rahimi, Vafa Baradaran;Ajam, Farideh;Rakhshandeh, Hasan;Askari, Vahid Reza
    • Journal of Pharmacopuncture
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    • v.22 no.1
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    • pp.7-15
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    • 2019
  • Portulaca oleracea L. (PO) or Purslane is an annual grassy plant that is distributed in many parts of the world, especially the tropical and subtropical areas. PO has some pharmacological properties such as analgesic, antibacterial, skeletal muscle-relaxant, wound-healing, anti- inflammatory and a radical scavenger. This review article is focused on the anti-inflammatory, immuno-modulatory, anti-oxidant and anti-tumor activities of the PO. Anti-inflammatory, immuno-modulatory, anti-oxidant and Anti-tumor effects of PO were searched using various databases until the end of August 2018. The online literature was searched using PubMed, Science Direct, Scopus, Google Scholar and Web of Science. Our review showed that PO exerts its effects through anti-inflammatory properties and balancing the adaptive and innate immune system depending on situations. PO acts as immune-modulator and anti-oxidant agent in both inflammatory states by the dominance of Th2 response such as asthma, cancer and atopic dermatitis and evoked Th1 disorders including hepatitis and multiple sclerosis.

Developmental toxicity and anti-inflammatory effect of the soft coral Dendronephthya gigantea collected from Jeju Island in zebrafish model

  • Lee, Seung-Hong
    • Fisheries and Aquatic Sciences
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    • v.20 no.12
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    • pp.32.1-32.7
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    • 2017
  • Recent in vitro studies have demonstrated that extract of soft coral Dendronephthya gigantea (SCDE) had strong anti-inflammatory activities. However, the direct effects of SCDE on anti-inflammatory activities in vivo model remained to be determined. Therefore, the present study was designed to assess in vivo anti-inflammatory effect of SCDE using lipopolysaccharide (LPS)-stimulated zebrafish model. We also investigated whether SCDE has toxic effects in zebrafish model. The survival, heart beat rate, and developmental abnormalities were no significant change in the zebrafish embryos exposed to at a concentration below $100{\mu}g/ml$ of SCDE. However, lethal toxicity was caused after exposure to 200 and $400{\mu}g/ml$ of SCDE. Treating zebrafish model with LPS treatment significantly increased the reactive oxygen species (ROS) and nitric oxide (NO) generation. However, SCDE inhibited this LPS-stimulated ROS and NO generation in a dose-dependent manner. These results show that SCDE alleviated inflammation by inhibiting the ROS and NO generation induced by LPS treatment. In addition, SCDE has a protective effect against the cell damage induced by LPS exposure in zebrafish embryos. This outcome could explain the profound anti-inflammatory effect of SCDE both in vitro as well as in vivo, suggesting that the SCDE might be a strong anti-inflammatory agent.

UHPLC/TOFHRMS analysis and anti-inflammatory effect of leaf extracts from Zizyphus jujuba in LPS-stimulated RAW264.7 cells

  • Hyun Ji Eo;Sun-Young Lee;Gwang Hun Park
    • Journal of Plant Biotechnology
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    • v.50
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    • pp.27-33
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    • 2023
  • Zizyphus jujube is a plant in the buckthorn family (Rhamnaceae) that has been the subject of research into antibacterial, antifungal and anti-inflammatory properties of its fruit and seed. However, few studies have investigated its leaves. In this study, the anti-inflammatory activity of ZJL (an extract of Z. jujube leaf) was evaluated to verify its potential as an anti-inflammatory agent and SARS-CoV-2 medicine, using nitric oxide (NO) assay, RT-PCR, SDSPAGE, Western blotting, and UHPLC/TOFHRMS analysis. We found that ZJL suppresed pro-inflammatory mediators such as NO, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and tumor necrosis factor α (TNF-α) in lipopolysaccharide (LPS)-induced RAW264.7 cells. ZJL acted by inhibiting NF-KB and MAPK signaling pathway activity. We also confirmed that ZJL contains a phenol compound and flavonoids with anti-inflammatory activity such as trehalose, maleate, epigallocatechin, hyperoside, catechin, 3-O-coumaroylquinic acid, rhoifolin, gossypin, kaempferol 3-neohesperidoside, rutin, myricitrin, guaiaverin, quercitrin, quercetin, ursolic acid, and pheophorbide a. These findings suggest that ZJL may have great potential for the development of anti-inflammatory drugs and vaccines via inhibition of NF-κB and MAPK signaling in LPS-induced RAW264.7 cells.

Anti-inflammatory effects of a methanol extract from Pulsatilla koreana in lipopolysaccharide-exposed rats

  • Lee, Sang-Hyun;Lee, Eun;Ko, Young-Tag
    • BMB Reports
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    • v.45 no.6
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    • pp.371-376
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    • 2012
  • To investigate the therapeutic effect of a Korean herbal medicine Pulsatilla koreana as an anti-septic agent, anti-inflammatory effects of the herbal medicine were determined in lipopolysaccharide (LPS)-exposed rats. Treatment with a methanol extract from Pulsatilla koreana significantly inhibited LPS-induced inflammatory responses. Results from ELISA analysis showed that Pulsatilla koreana decreased the plasma and hepatic levels of pro-inflammatory cytokines such as IL-$1{\beta}$, IL-6, TNF-${\alpha}$ while increased the level of anti-inflammatory cytokine IL-10 in LPS-exposed rats. Pulsatilla koreana also decreased the plasma levels of other inflammatory mediators such as $NO_3{^-}/NO_2{^-}$, ICAM-1, $PGE_2$, and CINC-1 in LPS-exposed rats. Although no significant effects were observed in the phagocytic activities, the distribution of lymphocyte population was significantly shifted by the treatment with Pulsatilla koreana. All together, Pulsatilla koreana exerts anti-inflammatory activities in the immune-challenged animals implicating that this Korean herbal medicine is therapeutically useful for the treatment of inflammatory diseases like sepsis.

Anti-inflammatory Effect of MeOH Extract of Cibotium barometz in IFN-$\gamma$ and LPS-stimulated Mouse Peritoneal Macrophage (IFN-$\gamma$와 LPS로 자극된 쥐의 복강 대식세포에서 구척 메탄올 추출물의 항염증 효과)

  • Lee, Ji-Young;Ko, Sung-Hoon;Lee, Yong-Jae;Lee, Se-Yeoun;Park, Ho-Jun;Shin, Tae-Yong;Jeon, Hoon
    • Korean Journal of Pharmacognosy
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    • v.41 no.2
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    • pp.108-114
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    • 2010
  • The rhizome of Cibotium barometz has been used for variety of bone disease as a traditional medicine. In the present study, we examined the antioxidant and anti-inflammatory activities of 85% methanol extract of C. barometz. C. barometz exhibited potent scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, superoxide radical and nitric oxide radical. In IFN-$\gamma$/LPS-stimulated mouse peritoneal macrophage model, C. barometz suppressed nitric oxide production and IL-6 secretion dose-dependently. Moreover, C. barometz showed decreased iNOS and COX-2 expression without notable cytotoxicity. These results suggest that C. barometz may be an useful agent as an antioxidant and anti-inflammatory agent.

A new Potential Anti-inflammatory Agent

  • Kim, Hee-Kee;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.406-410
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    • 1998
  • Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

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Binding Model of Fisetin and Human c-Jun NH2-Terminal Kinase 1 and Its Anti-inflammatory Activity

  • Jnawali, Hum Nath;Lee, Eunjung;Jeong, Ki-Woong;Heo, Yong-Seok;Kim, Yangmee
    • Bulletin of the Korean Chemical Society
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    • v.34 no.9
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    • pp.2629-2634
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    • 2013
  • Fisetin is a naturally occurring flavonoid with some anti-cancer and anti-inflammation capabilities. In this study, we perform docking studies between human c-Jun N-terminal kinase 1 (JNK 1) and fisetin and proposed a binding model of fisetin and JNK 1, in which the hydroxyl groups of the B ring and oxygen at the 4-position of the C ring play key roles in binding interactions with JNK. Fluorescence quenching and saturation-transfer difference (STD) NMR experiments showed that fisetin exhibits good binding affinity to JNK, $1.32{\times}10^8M^{-1}$. The anti-inflammatory activity of fisetin was also investigated. Fisetin significantly suppressed tumor necrosis factor, the NO production, and macrophage inflammatory cytokine release in LPS-stimulated RAW264.7 mouse macrophages. We found that the anti-inflammatory cascade of fisetin was mediated through the JNK, and cyclooxygenase (COX)-2 pathways. Our findings suggest the potential of fisetin as an anti-inflammatory agent.

Recent Prospect of Compounds Derived from Marine Macroalgae for Medicinal Application of Anti-Inflammation for Chemoprevention of Cancer

  • Kim, Moon-Moo
    • Journal of Marine Bioscience and Biotechnology
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    • v.5 no.4
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    • pp.8-14
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    • 2011
  • Although marine living organism contains a numerious number of compounds, it is difficult to collect these compounds in a large scale for medicinal application. However, in recent years, several bioactive compounds isolated from marine macroalgae have been proved to be able to provide potential sources for development of medicinal products because they can be obtained in large amount from marine. A number of studies have reported a variety of effects of marine macroalgae but a few anti-inflammatory activity of marine macroalgae have recently been published. Herein, we reviewed novel anti-inflammatory compounds recently isolated from marine brown algae, green algae and red algae. From this survey, in particular, some compounds contained in edible macroalgae exert anti-inflammatory effects with inhibition on cyclooxygenase-2 (COX-2), inducible nitric oxide synthase(iNOS) and matrix metalloproteinases (MMPs) activity regulated by nuclear factor-kappa B transcription factor that play a key role in cancer as well as inflammation, demonstrating to be able to potentially apply to development of anti-inflammatory agent for chemoprevention of cancer. Furthermore, some macroalgae and their compounds with both excellent anti-inflammatory activity and very low toxicity can select a potential candidates capable of preventing or treating several chronic inflammation such as colitis, hepatitis and gastritis, leading to cancer.

Anti-inflammatory Effect of Evodia Officinalis $D_{ODE}$ in Mouse Macrophage and Human Vascular Endotherial Cells (마우스 대식세포 및 사람 혈관 내피세포에서 오수유(Evodia officinalis $D_{ODE}$) 메탄올 추출물의 항염증 효과)

  • Yun, Hyun-Jeung;Heo, Sook-Kyoung;Lee, Young-Tae;Park, Won-Hwan;Park, Sun-Dong
    • The Korea Journal of Herbology
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    • v.23 no.1
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    • pp.29-38
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    • 2008
  • Objectives : Evodia officinalis DODE (EO), an herbal plant, has been widely used in traditional Korean medicine for the treatment of vascular diseases such as hypertension. The crude extract of EO contains phenolic compounds that are effective in protecting liver microsomes, hepatocytes, and erythrocytes against oxidative damage. But EO has been little found to have an anti-inflammatory activity. We investigated anti-inflammatory activity of EO in RAW 264.7 cells and human umbilical vein endothelial cells (HUVECs). Methods : Cytotoxic activity of EO on RAW 264.7 cells was investigated by using 5-(3-caroboxymeth-oxyphenyl)-2H-tetra-zolium inner salt (MTS) assay. The nitric oxide (NO) production was measured by Griess reagent system. And proinflammatory cytokines were measured by ELISA kit. The levels of intracellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) expression were measured by flow cytometer. Results : EO decreased LPS-induced NO production in RAW 264.7 cells. The inhibitory activity of EO on LPS-induced NO release is probably associated with suppressing TNF-${\alpha}$, IL-6 and MCP-1 formation. These results indicate that EO has potential as an anti-inflammatory agent. Moreover, EO decreased TNF-${\alpha}$-induced IL-8, IL-6 production, and ICAM-1 and VCAM-1 expression in HUVECs. Conclusions : EO inhibits TNF-${\alpha}$-induced inflammation via decreasing cytokines production and adhesion molecules expression. These results indicate that EO has potential as an anti-inflammation and anti-artherosclerosis agent.

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