• Title/Summary/Keyword: Inflammatory reaction

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Synthesis of Ochnaflavone and Its Inhibitory Activity on PGE2 Production

  • Kim, Sung Soo;Vo, Van Anh;Park, Haeil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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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.

A Case of Steroid Induced Intractable Hiccup - A Rare Side Reaction - (Steroid 약제 투여에 의한 Intractable Hiccup)

  • Lim, Byung-Sung;Choi, Wan-Young;Choi, Jin-Won;Shin, Dong-Ho;Park, Sung-Soo;Lee, Jung-Hee
    • Tuberculosis and Respiratory Diseases
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    • v.38 no.3
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    • pp.304-308
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    • 1991
  • Corticosteroid has been extensively used for the treatment of many medical diseases caused by immune and inflammatory response. And recently it becomes the first choice of treatment for bronchial asthma in a point of it's anti-inflammatory effects. However, this therapy has been associated with many well-known complications including truncal obesity, diabetes mellitus, excerbation of hypertension, delayed wound healing, easy bruisy, atropy of proximal muscles, psychotic symptoms, and/or osteoporosis. We report a case of patient with bronchial asthma who developed an uncommon side reaction, intractable hiccup persisting longer than 48 hours after treatment with oral corticosteroid.

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An investigation on the infection of Encephalitozoon cuniculi and pathological changes in laboratory rabbits (실험용 토끼에서 Encephalitozoon cunuculi의 감염과 병리학적 변화)

  • Yoon, Byong-Ill;Lee, Sang-Koo
    • Korean Journal of Veterinary Pathology
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    • v.1 no.1
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    • pp.66-71
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    • 1997
  • Eighteen NZW rabbits used for local skin irritation study were examined grossly and microscopically for natural infection with Encephalitozoon cuniculi. For microscopic tissue evaluation histochemical techniques such as PAS Gram iron hematoxylin and HE stain were used. Although rabbits in the study had no abnormal clinical signs 7/18(38.9%) animals were microscopically infected with E. cuniculi. The affected rabbits had gray-whitish and depressed approximately 0.1∼0.6 cm diameter lesions in the kidneys. All other organs examined were grossly unremarkable. Histopathologically however in addition to segmental interstitial nephritis focal lymphocytic myocarditis and granulomatous inflammatory reaction in portal areas of the liver multifocal granulomatous foci with vasculitis were present in the brain kidney and lungs. Aggregates of minute oval organisms were observed in brain and kidney sections frequently within the granulomatous foci and sometimes without any inflammatory reaction particularly in the renal tubules. in histochemical stains the organisms were gram positive stained with iron hematoxylin and had PAS positive granule at one pole. They measured approximately 1.5×2.5μm consistent with E. cuniculi. Histochemical characterization is important to differentiate E. cuniculi from other common protozoal infection such as Toxoplasma gondii. This study demonstrate the importance of subclinical. E. cunuculi infection and the associated histological alterations may interfere with tissue evaluation in toxicologic studies.

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A Case of Urticarial Drug Eruption Assumed to be Caused by non-steroidal anti- inflammatory drugs (NSAIDs) (비스테로이드성 소염진통제 (NSAIDs) 에 의한 것으로 추정되는 담마진성 약진 치험 1례)

  • Yu, Hyun-Jung;Hong, Seung-Ug
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.20 no.1 s.32
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    • pp.256-264
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    • 2007
  • Objective : This study describes a case of urticarial drug eruption assumed to be caused by non-steroidal anti- inflammatory drugs (NSAIDs) treated with oriental medicine and acupuncture. Methods : We studied the case of 20-years-old drug eruption patient. The patient complained of urticaria, angioedema, itching and burning sensation after taking NSAIDs. The indications for NSAIDs prescribed were common cold symptom and sore throat. For diagnosis, blood test and urinalysis were done. For treatment, acupuncture and herbal-medicine treatment were applied. Results : The patient of this report were examined for 13 days. The radiological finding was within normal limits. The WBC, neutrophil, lymphocyte and eosinophil level normalized during admission. After 3 days, itching and wheal reaction of whole body disappeared except facial symptom. The angioedema, itching and wheal reaction in the face was almost improved in the 4th day after discharge. Conclusions : We may expect that the oriental medical therapy improves the urticarial drug eruption caused by NSAIDs.

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Effect of Radish on Inflammatory Reaction in Human Epithelial Gastric Cell (사람 위 상피세포의 염증반응에 대한 무의 효과)

  • Shon, Yun-Hee;Chung, Yoo-Sun;Suh, Jeong-Ill;Park, In-Kyung;Nam, Kyung-Soo
    • Journal of Life Science
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    • v.16 no.1
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    • pp.17-21
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    • 2006
  • The effects of Korean and Japanese radishes on inflammatory reaction that involves arachidonic acid cascades were investigated in human epithelial gastric cell. The activities of type I (porcine pancreas) and type II (Crotalus atrox) phospholipase $A_2(PLA_2$) were inhibited by radish. Cyclooxygenase-2 (COX-2) activity was significantly suppressed by radish (p<0.05, p<0.01 and p<0.005). The nitric oxide production was also inhibited by radish. The Korean radish was more effective in inhibition of $PLA_2$ and COX-2 activities and nitric oxide production than Japanease radish. These results indicate that radish has a protective effect on gastric epithelial cell inflammation by suppressing the activities of $PLA_2$ and COX-2 activities and nitric oxide production from gastric epithelial cell.

The Anti-allergic Effect of Vinegar Treated Small Black Soybean (Glycine max Merr.) is Mediated Through Inhibition of Histamine Release and Inflammatory Cytokine Secretion

  • Shin, Tae-Yong;Shin, Hye-Young;Lim, Jong-Pil;Jeon, Hoon;Kim, Dae-Keun;Chae, Byeong-Suk;Kwon, Young-Ee;Kang, Sin-Myoung;Chang, Ik-Jun;Park, Jeong-Suk;Lee, Jae-Hyeok
    • Natural Product Sciences
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    • v.13 no.4
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    • pp.337-341
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    • 2007
  • In this report, we investigated the effect of aqueous extract of vinegar treated small black soybean (Glycine max Merr.) (Leguminosae) (VSBS) on mast cell-mediated allergic reaction and pro-inflammatory cytokine secretion. VSBS inhibited compound 48/80-induced systemic reactions. VSBS attenuated immunoglobulin (Ig) E-mediated passive cutaneous anaphylaxis. In addition, VSBS decreased the phorbol 12-myristate 13-acetate plus calcium ionophore A23187-stimulated secretion of tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-6 and interleukin (IL)-8 in human mast cells. Our findings provide evidence that VSBS inhibits mast cell-derived allergic reactions.

Anti-inflammatory and Anti-allergic Effects of Herbal Extracts on Atopic Dermatitis(Part I) (약용식물추출물의 아토피성피부염에 대한 항염증 및 항알레르기효과(제 1보))

  • Rang, Moon-Jeong
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.1
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    • pp.75-84
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    • 2011
  • Atopic dermatitis is a chronic inflammatory skin disease associated with cutaneous hyper-reactivity to environmental triggers. In order to develop effective therapeutic herbal extracts for atopic dermatitis, cytotoxicity, antioxidant, anti-inflammatory and anti-allergic activities were investigated for various herbal extracts. Among candidate extracts, we selected Aloe vera L. (AV), Viola mandshurica W. Becker (VM), Punica granatum L. (PG), Dendrobium nobile L. (DN) and mixture of the above extracts (MX) for further investigations. All of them did not show cytotoxic activities to macrophage RAW264.7 cells below the concentration of 100 ppm. All showed antioxidant, anti-inflammatory and anti-allergic effects, although to various extents. In antioxidant effects, AV showed the highest effect, followed by PG and VM, while DN did the lowest. In evaluation for anti-inflammatory activities in macrophage RAW264.7 cells, AV and DN inhibited almost completely the LPS-induced production of nitric oxide, while AV, DN and VM showed strong inhibitory activities on the LPS-induced production of TNF-${\alpha}$. In anti-allergy effect in mast cell HMC-1, DN showed the highest effect, followed by AV and PG, while VM did the lowest. In the topical allergy reaction induced by compound 48/80 in Sprague-Dawley rat, DN exhibited significant anti-allergic effect, while PG, VM and AV did slight effect. These results suggest that AV, VM, PG and DN have antioxidant, anti-inflammatory and anti-allergic activities, and thus have the potential to reduce and alleviate the symptoms of atopic dermatitis.

Effects of 1,7-Substituted Methylxanthine Derivatives on LPS-Stimulated Expression of Cytokines and Chemokines in Raw 264.7 and HK-2 Cells

  • Kang, Joo-Yeon;Shin, Hea-Soon
    • Journal of Microbiology and Biotechnology
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    • v.25 no.2
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    • pp.296-301
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    • 2015
  • Chronic kidney diseases are based on uncontrolled immunological and inflammatory responses to pathophysiological renal circumstances such as glomerulonephritis, which is caused by immunological mechanisms of glomerular inflammation with increased production of renal pro-inflammatory cytokines. Pentoxifylline (PTX) exhibits anti-inflammatory properties by inhibiting cytokine and chemokine production through aggregation of erythrocytes and thrombocytes. We synthesized a series of 1,7-substituted methylxanthine derivatives by the Traube purine reaction, and the formation of purine ring was completed through nitrosation, a reduction of the nitroso to the amine by catalytic hydrogenation as derivatives of PTX. Then we studied biological activities such as renal anti-inflammatory effects of the synthesized compounds in the production of cytokines such as nitric oxide (NO), interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF-α) and of chemokines such as monocyte chemoattractant protein-1 and IL-8 in Raw 264.7 and HK-2 cells. Renal antiinflammatory activities of this novel series of N-1 and N-7-substituted methylxanthine showed that the N-7 methyl-group-substituted analogs (S7b) showed selective 61% and 77% inhibition of the production of NO and IL-8. The other replacement of the N-1-(CH2)4COCH3 roup, as in the case of compound S6c, also showed an effective 50% and 77% inhibition of TNF-α and IL-8 production in LPS-stimulated Raw 264.7 and HK-2 cells.

The improvement effect of anti-inflammation of Aronia extract that fermented by Lactic acid bacteria isolated from the fermented seafoods

  • Lim, Jeong-Muk;Choi, Ui-Lim;Lee, Jeong-Ho;Moon, Kwang Hyun;Kim, Dae Geun;Jeong, Kyung Ok;Im, So Yeon;Oh, Byung-Taek
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2018.10a
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    • pp.111-111
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    • 2018
  • Aronia (black chokeberry), a species of berries is source to a very large number of bioactive compounds like polyphenols, flavonoids, anthocyanins, and tannins in comparison to any other species. Owing to its antioxidant, anti-carcinogenic, anti-aging and anti-inflammatory properties. Fermentation- a bioconversion process exploiting the biological metabolic reaction of micro-organisms, has several benefits like improving the efficacy and safety of physiologically active substances, generation of new functional material, improving the adsorption rate and many others. Antigens like pathogens, food, pollen etc., generate a protective immune response in body tissues, and the process be referred to as inflammation. However, this when excessive results in a condition referred to as refractory inflammatory disease, whose incidence is increasing in the recent times, especially amongst children. The current study intended to assess the anti-oxidant activity, presence of polyphenols and anti-inflammatory efficacy of Aronia extract fermented by Lactic acid bacteria isolated from fermented sea foods. Aronia fruits collected from Sunchang, Chonbuk were lyophilized for fermentation. So as to maximise the efficacy of the fermented Aronia extract, the quantitative effects of lactic acid bacteria species, composition of extraction solution, influence of temperature and time on antioxidant activity and total polyphenol contents were investigated using an experimental design. Anti-inflammatory activity was evaluated on NO and cytokine ($TNF-{\alpha}$, IL-6) production in LPS activated Raw 264.7 cells. Results indicated that antioxidant effect and total polyphenol contents were best improved in extract of Aronia fermented by P. pentosaceus. In addition, NO and cytokine ($TNF-{\alpha}$, IL-6) levels were decreased significantly after fermentation. Thus, it was found that the anti-inflammatory activity of Aronia greatly increased after fermentation process using P. pentosaceus.

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Anti-Oxidant Activity and Anti-Inflammatory Effects of Spiraea fritschiana Schneid Extract (참조팝나무 추출물의 항산화 활성 및 항염증 효과)

  • Choi, Eun Yeong;Heo, Seong Il;Kwon, Yong Soo;Kim, Myong Jo
    • Korean Journal of Medicinal Crop Science
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    • v.24 no.1
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    • pp.31-37
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    • 2016
  • Background : We studied the anti-oxidant activity and anti-inflammatory effects of Spiraea fritschiana Schneid extract (SFSE). Methods and Results : The SFSE was prepared using methanol and was evaluated for its total phenol and flavonoid content, DPPH (1,1-diphenyl-2-picrylhydrazyl) free-radical scavenging activity, reducing power, and effect on nitric oxide (NO) production, and cell viability by using real-time polymerase chain reaction (PCR). The total phenol content was $212.78{\mu}g{\cdot}galli$c acid equivalent (GAE)/mg and the total flavonoid content was $66.84{\mu}g{\cdot}quercetin$ equivalent (QE)/mg. The extract showed antioxidant activity (DPPH free-radical scavenging activity) with $RC_{50}$ value of $76.61{\mu}g/m{\ell}$. The reducing power of the extract was Abs 0.58 at $250{\mu}g/m{\ell}$. Cell viability was determined using the MTT 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. To evaluate anti-inflammatory activity, we examined the inhibitory effects on lipopolysaccharide-(LPS)-induced NO production in RAW 264.7 cells. The NO inhibition rate was 90% at $200{\mu}g/m{\ell}$ SFSE. At the same concentration, the expression of pro-inflammatory genes such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 also decreased. Conclusions : Our results suggest that SFSE is a novel resource for the development of foods and drugs that possess anti-oxidant and anti-inflammatory activity.