• Title/Summary/Keyword: Anti-inflammatory drug

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Biological effects of zinc oxide nanoparticles on inflammation

  • Kim, Min-Ho
    • CELLMED
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    • v.6 no.4
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    • pp.23.1-23.6
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    • 2016
  • With the rapid developments in nanotechnology, an increasing number of nanomaterials have been applied in various aspects of our lives. Recently, pharmaceutical nanotechnology with numerous advantages has growingly attracted the attention of many researchers. Zinc oxide nanoparticles (ZnO-NPs) are nanomaterials that are widely used in many fields including diagnostics, therapeutics, drug-delivery systems, electronics, cosmetics, sunscreens, coatings, ceramic products, paints, and food additives, due to their magnetic, catalytic, semiconducting, anti-cancer, anti-bacterial, anti-inflammatory, ultraviolet-protective, and binding properties. The present review focused on the recent research works concerning role of ZnO-NP on inflammation. Several studies have reported that ZnO-NP induces inflammatory reaction through the generation of reactive oxygen species by oxidative stress and production of inflammatory cytokines by activation of nuclear factor-${\kappa}B$ ($NF-{\kappa}B$). Meanwhile, other researchers reported that ZnO-NP exhibits an anti-inflammatory effect by inhibiting the up-regulation of inflammatory cytokines and the activation of $NF-{\kappa}B$, caspase-1, $I{\kappa}B$ $kinase{\beta}$, receptor interacting protein2, and extracellular signal-regulated kinase. Previous studies reported that size and shape of nanoparticles, surfactants used for nanoparticles protection, medium, and experimental conditions can also affect cellular signal pathway. This review indicated that the anti-inflammatory effectiveness of ZnO-NP was determined by the nanoparticle size as well as various experimental conditions. Therefore, the author suggests that pharmaceutical therapy with the ZnO-NP is one of the possible strategies to overcome the inflammatory reactions. However, further studies should be performed to maximize the anti-inflammatory effect of ZnO-NP to apply as a potential agent in biomedical applications.

Anti-Inflammatory Herbal Extracts and Their Drug Discovery Perspective in Atopic Dermatitis

  • Jae-Won Lee;Eun-Nam Kim;Gil-Saeng Jeong
    • Biomolecules & Therapeutics
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    • v.32 no.1
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    • pp.25-37
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    • 2024
  • Atopic dermatitis (AD) is an allergic disorder characterized by skin inflammation. It is well known that the activation of various inflammatory cells and the generation of inflammatory molecules are closely linked to the development of AD. There is accumulating evidence demonstrating the beneficial effects of herbal extracts (HEs) on the regulation of inflammatory response in both in vitro and in vivo studies of AD. This review summarizes the anti-atopic effects of HEs and its associated underlying mechanisms, with a brief introduction of in vitro and in vivo experiment models of AD based on previous and recent studies. Thus, this review confirms the utility of HEs for AD therapy.

Synthesis of Mefenamic Acid Derivatives and Antioxidative and Anticoagulant Activities

  • Cha, Bae-Cheon
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.349-353
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    • 2000
  • Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

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Nanodiamonds Conjugated with Nonsteroidal Anti-inflammatory Drugs for Transdermal Delivery

  • Rhee, Changkyu;Puzyr, Alexey P.;Burov, Andrey E.;Burova, Olga G.;Kim, Whungwhoe;Bondar, Vladimir S.
    • Journal of Powder Materials
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    • v.25 no.6
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    • pp.459-465
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    • 2018
  • Most commercially available detonation nanodiamonds (DNDs) require further processing to qualify for use in biomedical applications, as they often contain many impurities and exhibit poor dispersibility in aqueous media. In this work, DNDs are modified to improve purity and impart a high colloidal stability to the particles. The dispersive and adsorption properties of modified DNDs are evaluated in terms of the suitability of DNDs as carriers for non-steroidal anti-inflammatory drugs (NSAIDs) in transdermal delivery. The study of adsorption on strongly positively and strongly negatively charged DNDs showed their high loading capacity for NSAIDs, and a pronounced relationship between the drugs and the particles' charges. Experiments on long-term desorption carried out with DND/NSAID complexes indicate that the nanoparticles exert a sustained effect on the drug release process.

Anti-inflammatory Effects in LPS-treated RAW 264.7 Cells and the Influences on Drug Metabolizing Enzyme Activities by the Traditional Herbal Formulas, Yongdamsagan-Tang and Paljung-san

  • Ha, Hyekyung;Jin, Seong Eun;Seo, Chang-Seob;Shin, Hyeun-kyoo
    • The Journal of Korean Medicine
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    • v.42 no.4
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    • pp.10-24
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    • 2021
  • Objectives: Yongdamsagan-tang (YST) and Paljung-san (PJS) in traditional medicine and finasteride in modern medicine are used to treat benign prostatic hyperplasia (BPH). In recent, the use of combination herbal remedies with conventional drugs has been increasing. Therefore, we investigated the anti-inflammatory effects of these drugs to treat BPH and the influence of herbal formulas on finasteride metabolism. Methods: The inhibitory effects of the herbal formulas and finasteride on the production of inflammatory mediators and cytokines were determined in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Additionally, the influence of herbal formulas on activities of human drug metabolizing enzymes (DMEs) was assessed using human microsomal enzymes. Results: We observed that YST, PJS and finasteride inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2) and interleukin-6 (IL-6) in RAW 264.7 cells. The half maximal inhibitory concentration (IC50) of YST on PGE2 production was calculated to be below 25 ㎍/mL. YST inhibited the activity of uridine diphosphate-glucuronosyltransterase (UGT) 1A4 with an IC50 value of 49.35 ㎍/mL. The activities of cytochrome P450 (CYP) 1A2, CYP2B6, CYP2C19, CYP3A4, and UGT1A1 were inhibited by PJS (IC50 < 100 ㎍/mL, each). Although PJS and YST inhibited the activities of CYP3A4 and UGT1A4, respectively, these formulas may not influence the metabolism of finasteride because the IC50 values of herbal formulas on DMEs are too high to affect metabolism. Conclusions: Our results suggest that the combination of finasteride and YST or PJS might not influence their drug metabolism and that the drugs may have synergistic effects against BPH.

Biological Activity of Chemical Constituents Isolated from Strain Chlamydomonassp. KSF108 (Chlamydomonadaceae)

  • Tran, Huynh Nguyen Khanh;Youn, Ui Joung;Kim, Minji;Cao, Thao Quyen;Kim, Jeong Ah;Woo, Mi Hee;Kim, Sanghee;Min, Byung Sun
    • Natural Product Sciences
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    • v.26 no.1
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    • pp.59-63
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    • 2020
  • This study focused on investigation of the immunosuppressive inhibitory effect through determination of IL-2 production of nine compounds (1 - 9) isolated from Chlamydomonas sp. KSF108. Among them, compounds 1, 5, and 6 displayed moderately inhibitory effects on IL-2 production at a concentration of 100 µM. In addition, the related ones including cytotoxic, anti-inflammatory, and anti-oxidant activities were also elucidated. 6 further displayed cytotoxic activity against the MCF-7 cell line, with an IC50 value of 17.2 µM and 4, 6 - 7, and 9 possessed significant DPPH radical scavenging activity, with IC50 values ranging from 3.1 to 4.4 µM. To the best of our knowledge, this is the first report on the bioactivity of isolated chemical constituents from the genus Chlamydomonas. Compounds 1 and 5 investigated for the first time in the activity of immunosuppressivity and 6 may come to serve as the most important marker in broad-spectrum activities of the secondary metabolites identified from C. sp. KSF108.

Anti-inflammatory activity of AP-SF, a ginsenoside-enriched fraction, from Korean ginseng

  • Baek, Kwang-Soo;Hong, Yong Deog;Kim, Yong;Sung, Nak Yoon;Yang, Sungjae;Lee, Kyoung Min;Park, Joo Yong;Park, Jun Seong;Rho, Ho Sik;Shin, Song Seok;Cho, Jae Youl
    • Journal of Ginseng Research
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    • v.39 no.2
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    • pp.155-161
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    • 2015
  • Background: Korean ginseng is an ethnopharmacologically valuable herbal plant with various biological properties including anticancer, antiatherosclerosis, antidiabetic, and anti-inflammatory activities. Since there is currently no drug or therapeutic remedy derived from Korean ginseng, we developed a ginsenoside-enriched fraction (AP-SF) for prevention of various inflammatory symptoms. Methods: The anti-inflammatory efficacy of AP-SF was tested under in vitro inflammatory conditions including nitric oxide (NO) production and inflammatory gene expression. The molecular events of inflammatory responses were explored by immunoblot analysis. Results: AP-SF led to a significant suppression of NO production compared with a conventional Korean ginseng saponin fraction, induced by both lipopolysaccharide and zymosan A. Interestingly, AP-SF strongly downregulated the mRNA levels of genes for inducible NO synthase, tumor necrosis factor-${\alpha}$, and cyclooxygenase) without affecting cell viability. In agreement with these observations, AP-SF blocked the nuclear translocation of c-Jun at 2 h and also reduced phosphorylation of p38, c-Jun N-terminal kinase, and TAK-1, all of which are important for c-Jun translocation. Conclusion: Our results suggest that AP-SF inhibits activation of c-Jun-dependent inflammatory events. Thus, AP-SF may be useful as a novel anti-inflammatory remedy.

Anti-inflammatory and Anti-gastritis Effect of Sogunjung-tang Mixed Soft Extract (소건중탕 혼합단미연조엑스의 항염증 및 항위염 효과)

  • Kim, Myoung-Jin;Choi, Hye-Min;Nam, Won-Hee;Kim, Se-Jin;Son, Su-Mi;Kim, Jung-Ok
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.35 no.6
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    • pp.235-241
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    • 2021
  • Sogunjung-tang (SGJT) is traditional herbal prescriptions used to treat abdominal pain. In this study, we evaluated the effect on inflammation and gastritis through SGJT formulation development. SGJT composition herbal medicine was boiled in water at 95~100℃ for 3 hours and then concentrated. Sogunjung-tang mix soft extract (STM) was prepared using pharmaceutical excipients such as purified water, sodium benzoate, β-cyclodextrin and CMC-Na. Anti-inflammatory experiment was conducted using STM and lipopolysaccharide (LPS) in RAW 264.7 cells. Cell survival was measured by MTT method. Nitric oxide (NO) was measured using griess reagents, and pro inflammatory cytokines were measured by enzyme-linked immunosorbent assay and RT-PCR. Also, we verified STM validity in acute gastritis using the ICR mouse. STM was administered oral for three days. And 150 mM HCl in 60% ethanol was oral administered 0.5 mL one hour after the last drug administration. Mice were sacrificed 1 hour after 150 mM HCl in 60% ethanol administration. The gastric mucosa was visually observed. STM were not toxic in RAW 264.7 cells. Treatment of STM inhibited the production of NO and inflammatory cytokine at the protein and mRNA levels. Also, in the acute gastritis model with the mouse, the treatment of STM improved gastric mucosal bleeding and edema. In summary, it was confirmed that the treatment of STM exerts anti-inflammatory and anti-gastritis effects. Therefore, we suggest that STM may provide a preclinical evidence for the prevention and treatment of inflammatory and gastritis diseases.

Analysis of Drug Utilization for Patients with Ankylosing Spondylitis (강직성 척추염 환자에 대한 약물사용 현황 분석)

  • Kang, Han-Bin;Je, Nam Kyung
    • Korean Journal of Clinical Pharmacy
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    • v.25 no.4
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    • pp.246-253
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    • 2015
  • Background & Object: Ankylosing spondylitis (AS) is a chronic inflammatory disease that causes ankylosis and deformation of axial joints. Since current medicine cannot cure the disease yet, alleviating pain and preventing deformation with medications are the main therapy for patients with AS. The key medications for these purposes include nonsteroidal anti-inflammatory drugs (NSAIDs), and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$) inhibitors. This study aims to analyze prescribing patterns of AS patients in South Korea. Method: National Patients Sample data compiled by the Health Insurance Review and Assessment Service from 2013 was analyzed. Patients with AS were identified with Korean Standard Classification of Diseases code-6, which was M45. The rates of prescription, discontinuation, and switching ingredients were calculated for each medication during 2013. Results: Total number of patients was 655, and most of them were male (n = 514, 78.5%). Of all age groups, the proportion of 30-40 year old patients was the greatest (35.1%). The most utilized drug class was NSAIDs (82.4%). Less than half of patients were prescribed $TNF-{\alpha}$ inhibitors (n = 212, 32.4%). Meloxicam, aceclofenac, and celecoxib were the most frequently prescribed NSAIDs. In case of $TNF-{\alpha}$ inhibitors, adalimumab, etanercept and infliximab were the top three most prescribed drugs. Although not recommended by the current practice guideline, significant proportions of patients were identified using disease modifying anti-rheumatic drugs (DMARDs). Conclusion: Considering the current practice guideline and previous studies about the efficacy, the use of DMARDs should be reduced and medical insurance term in South Korea should be re-examined.

4,5-Diaryl-2,2-Dimethyl-3(2Η)Furanone Derivatives as COX-2 Inhibitors-Next Generation Anti-Arthritis Candidate-

  • Shin, Song-Seok;Noh, Min-Soo;Byun, Young-Joo;Park, Jin-Kyu;Kim, Ji-Young;Lim, Kyung-Min;Ha, Jun-Yong;Kim, Jin-Kwan;Lee, Chang-Hoon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.3-6
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    • 2001
  • Inflammation is an outcome or an end effect of disruption of complex immunological balance. A variety of approaches to control immunological unbalance have been tried, and some of them are in practice in the clinic. Since inflammatory disorders are reflection of very complex immunological responses, it should be difficult to have such disorders under complete control. Thus, most of the drugs, being marketed and under development, possess some degrees of undesired side offsets originating from disruption of immunological balance. Steroids are excellent drugs suppressing inflammation in short term, however, long-term use of steroids would incur a serious side effect of "rebound". Another example is TNF-${\alpha}$-neutralizing agents, such as enbrel and infliximab. TNF-${\alpha}$ has been known to play a key role in the exacerbation of inflammation, and knock-out of TNF-${\alpha}$ is regarded essential to control of chronic inflammation. The TNF-${\alpha}$-neutralizing drugs in the market are regarded very efficient in the management of rheumatoid arthritis. Upon long term use, however, those drugs cause sepsis to a certain proportion of patients. It is ironical that a high plasma level of TNF-${\alpha}$ is known to be responsible for sepsis, and that the drugs scavenging TNF-${\alpha}$ cause sepsis. The above two examples illustrate well the difficulty of discovering an anti-inflammatory drug without unwanted immunological side effects. An anti-inflammatory drug would make a case in the market, as long as the drug has huge therapeutic benefits compared to its expected but unwanted immunological side effects, where cyclooxygenase-2 inhibitors are positioning. In this presentation, will be discussed general aspects of cyclooxygenase-2 inhibition in conjunction with 3(2Η)furanone derivatives, a novel class of COX-2 inhibitors.

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