• Title/Summary/Keyword: novel compound

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KMS99220 Exerts Anti-Inflammatory Effects, Activates the Nrf2 Signaling and Interferes with IKK, JNK and p38 MAPK via HO-1

  • Lee, Ji Ae;Kim, Dong Jin;Hwang, Onyou
    • Molecules and Cells
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    • v.42 no.10
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    • pp.702-710
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    • 2019
  • Neuroinflammation is an important contributor to the pathogenesis of neurodegenerative disorders including Parkinson's disease (PD). We previously reported that our novel synthetic compound KMS99220 has a good pharmacokinetic profile, enters the brain, exerts neuroprotective effect, and inhibits $NF{\kappa}B$ activation. To further assess the utility of KMS99220 as a potential therapeutic agent for PD, we tested whether KMS99220 exerts an anti-inflammatory effect in vivo and examined the molecular mechanism mediating this phenomenon. In 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated mice, oral administration of KMS99220 attenuated microglial activation and decreased the levels of inducible nitric oxide synthase and interleukin 1 beta ($IL-1{\beta}$) in the nigrostriatal system. In lipopolysaccharide (LPS)-challenged BV-2 microglial cells, KMS99220 suppressed the production and expression of $IL-1{\beta}$. In the activated microglia, KMS99220 reduced the phosphorylation of $I{\kappa}B$ kinase, c-Jun N-terminal kinase, and p38 MAP kinase; this effect was mediated by heme oxygenase-1 (HO-1), as both gene silencing and pharmacological inhibition of HO-1 abolished the effect of KMS99220. KMS99220 induced nuclear translocation of the transcription factor Nrf2 and expression of the Nrf2 target genes including HO-1. Together with our earlier findings, our current results show that KMS99220 may be a potential therapeutic agent for neuroinflammation-related neurodegenerative diseases such as PD.

Cobalt Recovery by Oxalic Acid and Hydroxide Precipitation from Waste Cemented Carbide Scrap Cobalt Leaching Solution (폐초경 스크랩 코발트 침출용액으로부터 옥살산 및 수산화물 침전에 의한 코발트 분말 회수)

  • Lee, Jaesung;Kim, Mingoo;Kim, Seulgi;Lee, Dongju
    • Journal of Powder Materials
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    • v.28 no.6
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    • pp.497-501
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    • 2021
  • Cobalt (Co) is mainly used to prepare cathode materials for lithium-ion batteries (LIBs) and binder metals for WC-Co hard metals. Developing an effective method for recovering Co from WC-Co waste sludge is of immense significance. In this study, Co is extracted from waste cemented carbide soft scrap via mechanochemical milling. The leaching ratio of Co reaches approximately 93%, and the leached solution, from which impurities except nickel are removed by pH titration, exhibits a purity of approximately 97%. The titrated aqueous Co salts are precipitated using oxalic acid and hydroxide precipitation, and the effects of the precipitating agent (oxalic acid and hydroxide) on the cobalt microstructure are investigated. It is confirmed that the type of Co compound and the crystal growth direction change according to the precipitation method, both of which affect the microstructure of the cobalt powders. This novel mechanochemical process is of significant importance for the recovery of Co from waste WC-Co hard metal. The recycled Co can be applied as a cemented carbide binder or a cathode material for lithium secondary batteries.

In Vitro and In Vivo Anti-Clostridioides difficile Effect of a Probiotic Bacillus amyloliquefaciens Strain

  • Islam, Md Imtiazul;Seo, Hoonhee;Redwan, Asma;Kim, Sukyung;Lee, Saebim;Siddiquee, Mashuk;Song, Ho-Yeon
    • Journal of Microbiology and Biotechnology
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    • v.32 no.1
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    • pp.46-55
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    • 2022
  • Clostridioides difficile infection (CDI) is a significant cause of hospital-acquired and antibiotic-mediated intestinal diseases and is a growing global public health concern. Overuse of antibiotics and their effect on normal intestinal flora has increased the incidence and severity of infections. Thus, the development of new, effective, and safe treatment options is a high priority. Here, we report a new probiotic strain, Bacillus amyloliquefaciens (BA PMC-80), and its in vitro/in vivo anti-C. difficile effect as a prospective novel candidate for replacing conventional antibiotics. BA PMC-80 showed a significant anti-C. difficile effect in coculture assay, and its cell-free supernatant (CFS) also exhibited a considerable anti-C. difficile effect with an 89.06 ㎍/ml 50% minimal inhibitory concentration (MIC) in broth microdilution assay. The CFS was stable and equally functional under different pHs, heat, and proteinase treatments. It also exhibited a high sensitivity against current antibiotics and no toxicity in subchronic toxicity testing in hamsters. Finally, BA PMC-80 showed a moderate effect in a hamster CDI model with reduced infection severity and delayed death. However, further studies are required to optimize the treatment condition of the hamster CDI model for better efficacy and identify the antimicrobial compound produced by BA PMC-80.

Cure Properties of Novel Epoxy Resin Systems for WLP (Wafer Level Package) According to the Change of Hardeners (경화제 변화에 따른 WLP(Wafer Level Package)용 신규 Epoxy Resin System의 경화특성)

  • Kim, Whan Gun
    • Journal of the Semiconductor & Display Technology
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    • v.21 no.2
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    • pp.57-67
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    • 2022
  • The curing characteristics of naphthalene type epoxy resin systems according to the change of curing agent were investigated to develop a new next-generation EMC(Epoxy Molding Compound) with excellent warpage characteristics, low thermal expansion, and excellent fluidity for WLP(Wafer Level Package). As epoxy resins, DGEBA, which are representative bisphenol type epoxy resins, NE-16, which are the base resins of naphthalene type epoxy resins, and NET-OH, NET-MA, and NET-Epoxy resins newly synthesized based on NE-16 were used. As a curing agent, DDM (Diamino Diphenyl Methane) and CBN resin with naphthalene moiety were used. The curing reaction characteristics of these epoxy resin systems with curing agents were analyzed through thermal analysis experiments. In terms of curing reaction mechanism, DGEBA and NET-OH resin systems follow the nth curing reaction mechanism, and NE-16, NET-MA and NET-Epoxy resin systems follow the autocatalytic curing reaction mechanism in the case of epoxy resin systems using DDM as curing agent. On the other hand, it was found that all of them showed the nth curing reaction mechanism in the case of epoxy resin systems using CBN as the curing agent. Comparing the curing reaction rate, the epoxy resin systems using CBN as the curing agent showed a faster curing reaction rate than them with DDM as a hardener in the case of DGEBA and NET-OH epoxy resin systems following the same nth curing reaction mechanism, and the epoxy resin systems with a different curing mechanism using CBN as a curing agent showed a faster curing reaction rate than DDM hardener systems except for the NE-16 epoxy resin system. These reasons were comparatively explained using the reaction rate parameters obtained through thermal analysis experiments. Based on these results, low thermal expansion, warpage reduction, and curing reaction rate in the epoxy resin systems can be improved by using CBN curing agent with a naphthalene moiety.

α-Pinene Sensing Properties of Rhombohedral In2O3 Nanoparticles Prepared using the Microwave-assisted Hydrothermal Method (마이크로파 보조 수열 합성법으로 제조한 Rhombohedral In2O3 나노입자의 α-pinene 감지 특성)

  • Byeong-Hun, Yu;Hyo Jung, Lee;Joo Ho, Hwang;Ji-Wook, Yoon
    • Journal of Sensor Science and Technology
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    • v.31 no.6
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    • pp.418-422
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    • 2022
  • α-pinene is a natural volatile organic compound secreted by coniferous trees to protect themselves from attacks by insects, microorganisms, and viruses. Recently, studies have reported that α-pinene possesses pharmacological effects on various biological reactions such as anxiolytic, sleep-enhancing, anti-nociceptive, and inflammatory activity. Thus, forest bathing has recently received great attention as a novel therapy for treating severe diseases as well as psychological issues. However, appropriate places and timings for effective therapies are still veiled, because on-site monitoring of α-pinene gas in forests is barely possible. Although portable chemosensors could allow real-time analysis of α-pinene gas in forests, the α-pinene sensing properties of chemosensors have never been reported thus far. Herein, we report for the first time, the α-pinene sensing properties of an oxide semiconductor gas sensor based on rhombohedral In2O3 (h-In2O3) nanoparticles prepared by a microwave-assisted hydrothermal reaction. The h-In2O3 nanoparticle sensor showed a high response to α-pinene gas at ppm levels, even under humid conditions (for example, relative humidity of 50 %). The purpose of this research is to identify the potential of oxide semiconductor gas sensors for implementing portable devices that can detect α-pinene gas in forests in real-time.

Evaluation of the antinociceptive effects of a selection of triazine derivatives in mice

  • Hajhashemi, Valiollah;Khodarahmi, Ghadamali;Asadi, Parvin;Rajabi, Hamed
    • The Korean Journal of Pain
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    • v.35 no.4
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    • pp.440-446
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    • 2022
  • Background: The authors showed in a previous study that some novel triazine derivatives had an anti-inflammatory effect. The present study was designed to evaluate the antinociceptive effect of five out of nine compounds including two vanillintriazine (5c and 5d) and three phenylpyrazole-triazine (10a, 10b, 10e) derivatives which showed the best anti-inflammatory effect. Methods: Male Swiss mice (25-30 g) were used. To assess the antinociceptive effect, acetic acid-writhing, formalin, and hot plate tests were used after intraperitoneal injection of each compound. Results: All compounds significantly (P < 0.001) reduced acetic acid-induced writhing at tested doses (50, 100, and 200 mg/kg). Also, the percent inhibition of writhing in the acetic acid test showed that at the maximum tested dose of these compounds (200 mg/kg), the order of potencies is as follows: 10b > 10a > 10e > 5d > 5c. In the formalin test, compounds 5d, 10a, and 10e showed an antinociceptive effect in the acute phase and all compounds were effective in the chronic phase. In the hot plate test, compounds 5c, 5d, and 10a demonstrated an antinociceptive effect. Conclusions: The results clearly showed that both vanillin-triazine and phenylpyrazole-triazine derivatives had an antinociceptive effect. Also, some compounds which showed activity in the early phase of formalin test as well as in the hot plate test could control acute pain in addition to chronic or inflammatory pain.

Effect of Calamansi Pulp Ethanol Extracts on the Meat Quality and Biogenic Amine Formation of Pork Patty during Refrigerated Storage

  • Jinwoo Cho;Farouq Heidar Barido;Hye-Jin Kim;Hee-Jin Kim;Dongwook Kim;Dong-Jin Shin;Aera Jang
    • Food Science of Animal Resources
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    • v.43 no.1
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    • pp.25-45
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    • 2023
  • This study evaluated the antibacterial and antioxidant activities of ethanol extract of calamansi pulp (CPE) and its effect on quality and biogenic amine (BAs) formation in pork patties during storage. The CPE were prepared in various conditions (ethanol concentrations of 50%, 70%, and 90% with extraction periods of 3 and 6 days). The extract with potent antibacterial and antioxidant activities (90%, 6 days) was selected for addition to pork patties. Three groups were tested: Control (without extract addition), CPE addition at 0.2% w/w (0.2PCPE), and 0.4% w/w (0.4PCPE). The addition of CPE inhibited the formation of BAs, mainly cadaverine, histamine, and tyramine, in pork patties during storage. The pH and bacterial count of pork patties decreased significantly in a concentration-dependent manner following the addition of CPE. The instrumental color (CIE L*, CIE a*, and CIE b*) tended to be higher in 0.4PCPE than in the control during storage. The thiobarbituric acid reactive substances and volatile basic nitrogen (VBN) values of pork patties were affected by CPE, showing a reduction toward lipid oxidation at any storage period, and maintaining the lowest VBN value in 0.4PCPE at the final storage day. Similarly, the reduction of total BAs in pork patties was observed ranged between 3.4%-38.1% under treatment with 0.2% CPE, whereas 18.4%-51.4% under 0.4% CPE addition, suggesting significant effect of CPE to improve meat quality. These novel findings demonstrate the efficacy of 0.4% CPE as a natural compound to preserve the quality and reduce BAs formation in pork patties during storage.

Properties of a Novel Glutamate Decarboxylase (GAD) from Levilactobacillus brevis B737 Isolated from Cabbage Kimchi

  • Tae Jin Kim;Min Jae Kim;Bong Sin Kim;Ji Yeon Yoo;Yun Ji Kang;Jeong Hwan Kim
    • Microbiology and Biotechnology Letters
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    • v.50 no.3
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    • pp.319-327
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    • 2022
  • γ-Aminobutyric acid (GABA) is a multi-functional compound with broad applications for food industry. GABA producing bacteria were isolated from cabbage kimchi. Among them, B737 was the best GABA producer when culture supernatants were analyzed by TLC. B737 was identified as Levilactobacillus brevis by 16S rRNA gene sequencing. Its glutamate decarboxylase (GAD) gene was cloned by PCR and the nucleotide sequence determined. B737 GAD consisting of 485 amino acids is the largest in size among GADs reported from LAB so far. gadB from L. brevis B737 was overexpressed in Escherichia. coli BL21(DE3) using pET26b(+).pET26b(+). The recombinant GAD was purified and its size was 55 kDa by SDS-PAGE. Maximum GAD activity was observed at pH 5 and 40℃ and the activity was dependent on pyridoxal 5'-phosphate. Km and Vmax of recombinant GAD were 6.2 ± 0.06 mM and 0.34 ± 0.002 mM/min, respectively. L. brevis B737 can be used as a starter for fermented foods with high GABA contents.

Anti-inflammatory activity of 6-O-phospho-7-hydroxycoumarin in LPS-induced RAW 264.7 cells

  • Hong, Hyehyun;Park, Tae-Jin;Jang, Sungchan;Kim, Min-Seon;Park, Jin-Soo;Chi, Won-Jae;Kim, Seung-Young
    • Journal of Applied Biological Chemistry
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    • v.65 no.1
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    • pp.33-41
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    • 2022
  • Esculetin (also known as 6, 7-dihydroxycoumarin) a type of coumarin, has been exhibited anti-inflammatory and anti-aging effects. Biorenovation is the microbe-mediated enhancement of biological efficacies and structurally diversified compounds relative to their substrate compounds. The production of different kinds of esculetin derivatives using Bacillus sp. JD3-7 and their effects on lipopolysaccharide (LPS)-triggered inflammatory response in RAW 26.7 cells were assessed. One of the biorenovation products, identified as esculetin 6-O-phosphate (ESP), at concentrations of 1.25, 2.5, and 5 μM inhibited the LPS-stimulated production of inflammation markers of nitric oxide synthase 2 and cyclooxygenase 2 as well as their respective enzymatic reaction products of nitric oxide and prostaglandin E2 in the order of increasing concentrations (1.25, 2.5, and 5 μM). Additionally, ESP treatment suppressed the LPS-stimulated secretion of pro-inflammatory cytokines of interleukin (IL)-1β, IL-6, and tumor necrosis factor- α. Furthermore, these anti-inflammatory effect of ESP was associated with the downregulation of mitogen-activated protein kinase signaling, that is, extracellular signal-regulated kinase, c-Jun NH2-terminal kinase, and p38 mitogen-activated protein kinase signaling pathways. This study would therefore provide interesting insights into the biorenovation-assisted generation of a novel anti-inflammatory compound. ESP may be used to develop treatments for inflammatory disorders.

Microtubule Acetylation-Specific Inhibitors Induce Cell Death and Mitotic Arrest via JNK/AP-1 Activation in Triple-Negative Breast Cancer Cells

  • Suyeon Ahn;Ahreum Kwon;Youngsoo Oh;Sangmyung Rhee;Woo Keun Song
    • Molecules and Cells
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    • v.46 no.6
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    • pp.387-398
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    • 2023
  • Microtubule acetylation has been proposed as a marker of highly heterogeneous and aggressive triple-negative breast cancer (TNBC). The novel microtubule acetylation inhibitors GM-90257 and GM-90631 (GM compounds) cause TNBC cancer cell death but the underlying mechanisms are currently unknown. In this study, we demonstrated that GM compounds function as anti-TNBC agents through activation of the JNK/AP-1 pathway. RNA-seq and biochemical analyses of GM compound-treated cells revealed that c-Jun N-terminal kinase (JNK) and members of its downstream signaling pathway are potential targets for GM compounds. Mechanistically, JNK activation by GM compounds induced an increase in c-Jun phosphorylation and c-Fos protein levels, thereby activating the activator protein-1 (AP-1) transcription factor. Notably, direct suppression of JNK with a pharmacological inhibitor alleviated Bcl2 reduction and cell death caused by GM compounds. TNBC cell death and mitotic arrest were induced by GM compounds through AP-1 activation in vitro. These results were reproduced in vivo, validating the significance of microtubule acetylation/JNK/AP-1 axis activation in the anti-cancer activity of GM compounds. Moreover, GM compounds significantly attenuated tumor growth, metastasis, and cancer-related death in mice, demonstrating strong potential as therapeutic agents for TNBC.