• Title/Summary/Keyword: $A_2$ inhibitor

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Application of thromboxane synthetase inhibitor (Ozagrel HCl) in feline infectious peritonitis (고양이 전염성 복막염에 thromboxane synthetase inhibitor (Ozagrel HCl)의 적용)

  • Kim, Tae-Sin;Lee, Sun-Hee;Lim, Soo-Jung;Park, Hyung-Jin;Song, Eun-Sik;Jung, Dae-Wook;Kim, Duck-Hwan;Song, Kun-Ho
    • Korean Journal of Veterinary Research
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    • v.50 no.1
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    • pp.63-69
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    • 2010
  • A Persian chinchila (2 years old, intact female) and a Korean domestic shorthaired cat (3 months, intact male) were referred to the Veterinary Medical Teaching Hospital of Chungnam National University with tachypnea. The two cats were diagnosed as feline infectious peritonitis (FIP) by blood and blood chemical examination, radiographic examination, RT-PCR and electrophoresis analysis of pleural effusion. Thromboxane synthetase inhibitor (Ozagrel HCl, 5 mg/kg, twice a day) was administered to the Persian chinchila and Korean domestic shorthair for 13 days and 16 days, respectively. Pleural effusion disappeared after treatment with Ozagrel HCl. Further study is needed to establish a new application protocol of Ozagrel HCl for FIP cases.

The expressions of inflammatory factors and tissue inhibitor of matrix metalloproteinase-2 in human chronic periodontitis with type 2 diabetes mellitus

  • Shin, Dong-Seok;Park, Jin-Woo;Suh, Jo-Young;Lee, Jae-Mok
    • Journal of Periodontal and Implant Science
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    • v.40 no.1
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    • pp.33-38
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    • 2010
  • Purpose: The purpose of this study was to observe and quantify the expression of interleukin-4 (IL-4), interferon-$\gamma$ (IFN-$\gamma$), and tissue inhibitor of matrix metalloproteinase-2 (TIMP-2) in the gingival tissue of patients with type 2 diabetes mellitus (DM) and healthy adults with chronic periodontitis. Methods: Twelve patients with type 2 DM and chronic periodontitis (Group 3), twelve patients with chronic periodontitis (Group 2), and twelve healthy individuals (Group 1) were included in the study. Clinical criteria of gingival (sulcus bleeding index value, probing depths) and radiographic evidences of bone resorption were divided into three groups. The concentrations of cytokines were determined by a western blot analysis and compared using one-way ANOVA followed by Tukey's test. Results: The expression levels of IFN-$\gamma$ and TIMP-2 showed an increasing tendency in Groups 2 and 3 when compared to Group 1. On the other hand, the expression of IL-4 was highest in Group 1. Conclusions: The findings suggest that IFN-$\gamma$ and TIMP-2 may be involved in the periodontal inflammation associated with type 2 DM. IL-4 may be involved in the retrogression of the periodontal inflammation associated with type 2 DM.

The effect of Woohwangchungsimwon on the learning and memory in NOS inhibitor treated rats in Morris water maze. (우황청심원(牛黃淸心元)이 NOS inhibitor에 의한 흰쥐의 학습(學習) 및 기억장애(記憶障碍)에 미치는 영향(影響))

  • Baek Ji-Seong;Kim Jong-Woo
    • Journal of Oriental Neuropsychiatry
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    • v.10 no.2
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    • pp.115-126
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    • 1999
  • This study was conducted to find out the effects of Woohwangchungsimwon on learning and memory in the NOS inhibitor treated rats. The Morris water maze was used in evaluating them. The result of the study was summarized as follows. 1. In the learning test, three groups have showed a gradual improvement of learning ability by repeating the trials in Morris water maze. WHCS group have showed statistical improvement than control group at 4,5,6 trial(p<0.05, p<0.01, p<0.01). 2. In the memory test, the first latency of WHCH group was statistically shortened than that of control group(p<0.05). 3. In the memory test, there was no statistical difference in the entry number between WHCH group and control. 4. In the memory test, there was no statistical difference in the memory score between WHCH group and control. The result of this experimental study presents that Woohwangchungsimwon has the improving effect on impaired learning and memory in NOS inhibitor treated rats, and implies that Woohwangchungsimwon may be one of the useful prescription for the treatment of vascular dementia after cerebral ischemia.

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Characteristics of Protease Inhibitor Purified from the Eggs of Alaska pollock (Theragra chalcogramma) (명란 단백분해효소 저해제의 특성)

  • STADI U;KIM Keun Yeong;KIM Sang Moo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.38 no.2
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    • pp.83-88
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    • 2005
  • Protease inhibitors were purified from the eggs of Alaska pollock (Theragra chalcogramma) using the following purification steps: ammonium sulfate precipitation, ion exchange, gel permeation, and high performance liquid chromatographies (HPLC). The protease inhibitor from the heated eggs of Alaska pollock was not as well purified. In addition, the heated eggs showed lower specific inhibitory activity than the unheated eggs. The purification yields after ammonium sulfate precipitation, ion exchange, and gel permeation chromatographies were 22.7$\%,\;15.3\%$,and $4.4\%$, respectively. There were two kinds of protease inhibitors on the gel permeation chromatography pattern Their molecular weights were estimated to be 66,700 and 16,000 Da, respectively. Both were classified as a cysteine protease inhibitor because of the existence of inhibiting papain, which is one of cysteine proteases.

Distribution and Inheritance of Trypsin Inhibitor Variant in Soybeans Grown in Korea (한국대두에서의 Trypsin Inhibitor Variant의 분포와 유전)

  • Choi, J.Y.;Chang, B.H.
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.26 no.1
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    • pp.51-55
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    • 1981
  • Seed proteins of 51 varieties of soybean were separated by disc electrophoresis. Nine varieties had Rf 0.79 electrophoretic band, and 42 varieties had Rf 0.83 band. The frequency for Rf 0.79 was 0.176 and the frequency for Rf 0.83 was 0.824. The F_1 seeds of crossed between Kumgangdaepp (Rf 0.79) and Uidu (Rf 0.83) possessed both bands. Analysis of 96 F_2 seeds showed a ratio of 22 : 53 : 21 (Rf 0.79 : Rf 0.79/Rf 0.83 : Rf 0.83), suggesting single gene control with two co dominant alleles.

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Preparation and Characterization of ${\alpha}$-D-Glucopyranosyl- ${\alpha}$-Acarviosinyl-D-Glucopyranose, a Novel Inhibitor Specific for Maltose-Producing Amylase

  • Kim, Myo-Jeong;Park, Kwan-Hwa
    • Proceedings of the Korean Society of Life Science Conference
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    • 2003.05a
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    • pp.23-37
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    • 2003
  • A novel inhibitor against maltose-producing a-amylase was prepared via stepwise degradation of a high molecular weight acarbose (HMWA) using Thermus maltogenic amylase (ThMA). The structure of the purified inhibitor was determined to be ${\alpha}$-D-glucopyranosyl-${\alpha}$-acarviosinyl-D-glucopyranose (GlcAcvGlc). Progress curves of p-nitrophenyl-${\alpha}$-D-maltoside (PNPG2) hydrolysis by various amylolytic enzymes, including maltogenase (MGase), ThMA, and cyclodextrinase(CDase) I-5, in the presence of acarbose or GlcAcvGlc indicated a slow-binding mode of inhibition. The inhibition potency of GlcAcvGlc for MGase, ThMA, and CDase I-5 was 3 orders of magnitude higher than that of acarbose.

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Proteasome Inhibitor-Induced IκB/NF-κB Activation is Mediated by Nrf2-Dependent Light Chain 3B Induction in Lung Cancer Cells

  • Lee, Kyoung-Hee;Lee, Jungsil;Woo, Jisu;Lee, Chang-Hoon;Yoo, Chul-Gyu
    • Molecules and Cells
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    • v.41 no.12
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    • pp.1008-1015
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    • 2018
  • $I{\kappa}B$, a cytoplasmic inhibitor of nuclear factor-${\kappa}B$ ($NF-{\kappa}B$), is reportedly degraded via the proteasome. However, we recently found that long-term incubation with proteasome inhibitors (PIs) such as PS-341 or MG132 induces $I{\kappa}B{\alpha}$ degradation via an alternative pathway, lysosome, which results in $NF-{\kappa}B$ activation and confers resistance to PI-induced lung cancer cell death. To enhance the anti-cancer efficacy of PIs, elucidation of the regulatory mechanism of PI-induced $I{\kappa}B{\alpha}$ degradation is necessary. Here, we demonstrated that PI up-regulates nuclear factor (erythroid-derived 2)-like 2 (Nrf2) via both de novo protein synthesis and Kelch-like ECH-associated protein 1 (KEAP1) degradation, which is responsible for $I{\kappa}B{\alpha}$ degradation via macroautophagy activation. PIs increased the protein level of light chain 3B (LC3B, macroautophagy marker), but not lysosome-associated membrane protein 2a (Lamp2a, the receptor for chaperone-mediated autophagy) in NCI-H157 and A549 lung cancer cells. Pretreatment with macroautophagy inhibitor or knock-down of LC3B blocked PI-induced $I{\kappa}B{\alpha}$ degradation. PIs up-regulated Nrf2 by increasing its transcription and mediating degradation of KEAP1 (cytoplasmic inhibitor of Nrf2). Overexpression of dominant-negative Nrf2, which lacks an N-terminal transactivating domain, or knock-down of Nrf2 suppressed PI-induced LC3B protein expression and subsequent $I{\kappa}B{\alpha}$ degradation. Thus, blocking of the Nrf2 pathway enhanced PI-induced cell death. These findings suggest that Nrf2-driven induction of LC3B plays an essential role in PI-induced activation of the $I{\kappa}B$/$NF-{\kappa}B$ pathway, which attenuates the anti-tumor efficacy of PIs.

In Vitro Antifungal Activity and Mode of Action of 2',4'-Dihydroxychalcone against Aspergillus fumigatus

  • Seo, Young Ho;Kim, Sung-Su;Shin, Kwang-Soo
    • Mycobiology
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    • v.43 no.2
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    • pp.150-156
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    • 2015
  • 2',4'-Dihydroxychalcone (2',4'-DHC) was identified from a heat shock protein 90 (Hsp90)-targeting library as a compound with Hsp90 inhibitory and antifungal effects. In the presence of 2',4'-DHC ($8{\mu}g/mL$), radial growth of Aspergillus fumigatus was inhibited 20% compared to the control, and green pigmentation was completely blocked. The expression of the conidiation-associated genes abaA, brlA, and wetA was significantly decreased (approximately 3- to 5-fold) by treatment with 2',4'-DHC. The expression of calcineurin signaling components, cnaA and crzA, was also significantly reduced. The inhibitory effects of 2',4'-DHC on metabolic activity and mycelial growth were significantly enhanced by combination treatment with itraconazole and caspofungin. Docking studies indicated that 2',4'-DHC bind to the ATPase domain of Hsp90. These results suggest that 2',4'-DHC act as an Hsp90-calcinurin pathway inhibitor.

Mechanism of Endothelium dependent Relaxation induced by $Mg^{++}-deficiency$ in isolated Canine Coronary Arteries (개의 관상동맥에서 $Mg^{++}$ 결핍에 의한 혈관 확장반응의 기전)

  • Ann, Hyung-Soo
    • YAKHAK HOEJI
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    • v.33 no.1
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    • pp.1-9
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    • 1989
  • We have recently reported that $Mg^{++}-deficiency$ showed endothelium dependent relaxation in isolated canine coronary arteries precontracted with $PGF_{2{\alpha}}$. To differentiate the release of EDRF or $PGI_2$ from the endothelium cells as the cause of vasorelaxation by $Mg^{++}-deficiency$, effects of several inhibitors of arachidonic acid metabolism on the relaxation by $Mg^{++}-deficiency$ were evaluated and also compared with that of acetylcholine. Ibuprofen and tranylcypromine ($10{\mu}M$), an inhibitor of cyclo-oxygenase and $PGI_2$ synthetase, respectively, did not effect on $Mg^{++}-free$ induced vasorelaxation. Pretreatment of quinacrine ($10{\mu}M$), an inhibitor of phospholipase $A_2$ and also $Ca^{++}$ uptake, blocked vasorelaxation by $Mg^{++}-free$. But trifluoperazine ($10{\mu}M$), which is about as potent as quinacrine in the inhibition of $Ca^{++}$ uptake, did not effect on $Mg^{++}-deficiency$ induced vasorelaxation. NDGA ($10{\mu}M$), an inhibitor of lipoxygenase, completely restored $Mg^{++}-free$ induced vasorelaxation, even though pretreatment of that was not blocked which might be due to the characteristics of vasorelaxation of NDGA itself. Pretreatment of methylene blue ($10{\mu}M$), which is known as a inhibitor of EDRF through the blocking effect of guanylate cyclase, completely blocked vasorelaxation by $Mg^{++}-free$ as well as acetylcholine ($0.1{\mu}M$). Acetylcholine-induced dose response curve was also antagonized by pretreatment of quinacrine ($10{\mu}M$), but not by ibuprofen, tranylcypromine and NDGA. These results appear to suggest that $Mg^{++}-free$ induced vasorelaxation was mediated by the release of EDRF through the activation of phospholipase $A_2$ and noncyclo-oxygenase on arachidonate metabolism.

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Potential application of urease and nitrification inhibitors to mitigate emissions from the livestock sector: a review

  • Eska, Nugrahaeningtyas;Eska, Nugrahaeningtyas;Jun-Ik, Song;Jung-Kon, Kim;Kyu-Hyun, Park
    • Journal of Animal Science and Technology
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    • v.64 no.4
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    • pp.603-620
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    • 2022
  • Human activities have caused an increase in greenhouse gas emissions, resulting in climate change that affects many factors of human life including its effect on water and food quality in certain areas with implications for human health. CH4 and N2O are known as potent non-CO2 GHGs. The livestock industry contributes to direct emissions of CH4 (38.24%) and N2O (6.70%) through enteric fermentation and manure treatment, as well as indirect N2O emissions via NH3 volatilization. NH3 is also a secondary precursor of particulate matter. Several approaches have been proposed to address this issue, including dietary management, manure treatment, and the possibility of inhibitor usage. Inhibitors, including urease and nitrification inhibitors, are widely used in agricultural fields. The use of urease and nitrification inhibitors is known to be effective in reducing nitrogen loss from agricultural soil in the form of NH3 and N2O and can further reduce CH4 as a side effect. However, the effectiveness of inhibitors in livestock manure systems has not yet been explored. This review discusses the potential of inhibitor usage, specifically of N-(n-butyl) thiophosphoric triamide, dicyandiamide, and 3,4-dimethylpyrazole phosphate, to reduce emissions from livestock manure. This review focuses on the application of inhibitors to manure, as well as the association of these inhibitors with health, toxicity, and economic benefits.