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Screening of Inflammatory Phospholipase $A_2$ Inhibitors from Natural Products (천연물로부터 염증성 포스포리파제 $A_2$ 저해제 검색)

  • Moon, Tae-Chul;Chung, Kwang-Won;Chung, Kyu-Charn;Son, Kun-Ho;Kim, Hyun-Pyo;Kang, Sam-Sik;Chang, Hyeun-Wook
    • YAKHAK HOEJI
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    • v.41 no.5
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    • pp.565-570
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    • 1997
  • High levels of extracellular phospholipase $A_2$ (Plase $A_2$) associated with inflammatory process in man and animal models have been extensively reported elsew here. Thus, a logical approach to the treatment of inflammatory diseases should involve the inhibitors of Plase $A_2$. To develop new Plase $A_2$ inhibitors from natural products, two hundred crude drugs were screened using group II PLA$A_2$ inhibitory activity. Among them, methanol extract of 5 medicinal plants such as, Raphani Semen, Moutan cortex radicis, Arecae semen, Caryophylli Cortex and Betulae Cortex inhibited more than 90% of PLase $A_2$ activity at a concentration 2.5${\mu}g/ml$. Then, 10 methanol extracts sample were transferred into organic solvents, PLase $A_2$ inhibitory effects were found mainly in CHCl3 and EtoAc fractions.

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Reactions of Pyrimidinonethione Derivatives;Synthesis of 2-Hydrazinopyrimidin-4-one, Pyrimido[1,2-a]-1,2,4-triazine, Triazolo-[1,2-a]pyrimidine, 2-(1-pyrazolo)Pyrimidine and 2-Arylhydrazonopyrimidine Derivatives

  • Attaby, Fawzy-A.;Eldin, Sanaa-M.;Hanafi, Eman-A.Z.
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.620-628
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    • 1997
  • 6-Aryl-5-cyano-4-pyrimidinon-2-thione derivatives 1a-c reacted with ethyl iodide to give the corresponded 2-S-ethylpyrimidin-4-one-derivatives 2a-c. Compounds 2a-c was, in turn, reacted with hydrazine hydrate to give the sulfur free reaction products, 3a-c. These reaction products were taken as the starting materials for the synthesis of several newly synthesized heterocyclic derivatives. Reactions with several halogenated ketones, esters, chloroacetic acid and chloroacetamide give pyrimidotriazines 8,12 and 15 while their reactions with formic acid, acetic acid and carbon disulfide gave the corresponded triazolopyrimidines 17 and 21. The reaction with both acetyl acetone and ethylacetoacetate gave the corresponded 2-$(3^{I},5^{I}-dimethyl-1^{I}-pyrazoly$pyrimidine derivatives 20a-c and 24a-c respectively while the reaction with cinnamonitriles 25a-h afforded the corresponded aryl hydrazopyrimidines 27a-f. The structure of these reaction products were eatablished based on both elemental anlayses and spectral data studies.

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Clostridium difficile Toxin A Upregulates Bak Expression through PGE2 Pathway in Human Colonocytes

  • Kim, Young Ha;Kim, Ho
    • Journal of Microbiology and Biotechnology
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    • v.29 no.10
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    • pp.1675-1681
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    • 2019
  • Clostridium difficile toxin A is known to cause colonic epithelial cell apoptosis, which is considered the main causative event that triggers inflammatory responses in the colon, reflecting the concept that the essential role of epithelial cells in the colon is to form a physical barrier in the gut. We previously showed that toxin A-induced colonocyte apoptosis and subsequent inflammation were dependent on prostaglandin E2 ($PGE_2$) produced in response to toxin A stimulation. However, the molecular mechanism by which $PGE_2$ mediates cell apoptosis in toxin A-exposed colonocytes has remained unclear. Here, we sought to identify the signaling pathway involved in toxin A-induced, $PGE_2$-mediated colonocyte apoptosis. In non-transformed NCM460 human colonocytes, toxin A exposure strongly upregulated expression of Bak, which is known to form mitochondrial outer membrane pores, resulting in apoptosis. RT-PCR analyses revealed that this increase in Bak expression was attributable to toxin A-induced transcriptional upregulation. We also found that toxin A upregulation of Bak expression was dependent on $PGE_2$ production, and further showed that this effect was recapitulated by an Prostaglandin E2(PGE2) receptor-1 receptor agonist, but not by agonists of other EP receptors. Collectively, these results suggest that toxin A-induced cell apoptosis involves $PGE_2$-upregulation of Bak through the EP1 receptor.

Effects of Different Exercise Intensities on Cytosolic and Mitochondrial LDH Isozymes of Cardiac Muscle in Rats (운동강도의 차이가 흰쥐의 심근 세포기질 및 미토콘드리아 LDH 동위효소 변화에 미치는 영향)

  • Lee Sang-Hak;Yoon Jin-Hwan
    • Journal of Life Science
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    • v.15 no.1 s.68
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    • pp.80-86
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    • 2005
  • To achieve the purpose of this study, forty-eight male Sprague-Dawley rats were assigned to control and three endurance exercise group. 36 rats were forced to exercise according to exercise intensity for 8 weeks and 12 rats were untrained for control group. Cardiac cytosol was extracted from cardiac tissue and cardiac mitochondria was purified from the cytosol. Purified mitochondria were separated into four fraction: inner membrane, outer membrane inter membrane space and matrix. The changes of cytosolic and mitochondrial LDH isozymes activity were measure. Relative activity $(\%)$ of cytosol for low and control group showed the following order of prevalence $AB_3>A_2B_2>B_4>A_3B>A_4$ for moderate and high group : $AB_3>B_4>A_2B_2>A_3B>A_4$. Outer membrane for low group showed $AB_3>B_4>A_2B_2$, for moderate group:$ B_4>AB_3>A_2B_2$, for high and control group: $B_4>A_3B$. Inter membrane space for low, moderate and high group showed $B_4>AB_3>A_2B_2>A_3B>A_4$, for control group: $B_4>A_3B>AB_3>A_2B_2>A_4$. Inner membrane for all group showed $B_4>AB_3>A_2B_2>A_3B>A_4$. Matrix for control, low, moderate and high group showed $B_4>AB_3>A_2B_2>A_3B>A_4$. These results suggest that long term exercise intensity effect on cardiac tissue cytosolic and mitochondrial activity and $A_4,\;A_3B,\;A_2B_2,\;AB_3\;and\;B_4$ isozymes were found entirely in mitochondrial fraction.

Effect of Annealing Time on Electrical Performance of SiZnSnO Thin Film Transistor Fabricated by RF Magnetron Sputtering

  • Ko, Kyung Min;Lee, Sang Yeol
    • Transactions on Electrical and Electronic Materials
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    • v.16 no.2
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    • pp.99-102
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    • 2015
  • Thin film transistors (TFTs) with amorphous 2 wt% silicon-doped zinc tin oxide (a-2SZTO) channel layer were fabricated using an RF magnetron sputtering system, and the effect of post-annealing treatment time on the structural and electrical properties of a-2SZTO systems was investigated. It is well known that Si can effectively reduce the generation of oxygen vacancies. However, it is interesting to note that prolonged annealing could have a bad effect on the roughness of a-2SZTO systems, since the roughness of a-2SZTO thin films increases in proportion to the thermal annealing treatment time. Thermal annealing can control the electrical characteristics of amorphous oxide semiconductor (AOS) TFTs. It was observed herein that prolonged annealing treatment can cause bumpy roughness, which led to increase of the contact resistance between the electrode and channel. Thus, it was confirmed that deterioration of the electrical characteristics could occur due to prolonged annealing. The longer annealing time also decreased the field effect mobility. The a-2SZTO TFTs annealed at 500℃ for 2 hours displayed the mobility of 2.17 cm2/Vs. As the electrical characteristics of a-2SZTO annealed at a fixed temperature for long periods were deteriorated, careful optimization of the annealing conditions for a-2SZTO, in terms of time, should be carried out to achieve better performance.

Cancer-Upregulated Gene 2 (CUG2), a New Component of Centromere Complex, Is Required for Kinetochore Function

  • Kim, Hyejin;Lee, Miae;Lee, Sunhee;Park, Byoungwoo;Koh, Wansoo;Lee, Dong Jun;Lim, Dae-Sik;Lee, Soojin
    • Molecules and Cells
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    • v.27 no.6
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    • pp.697-701
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    • 2009
  • We previously identified cancer-upregulated gene 2 (CUG2) as a commonly up-regulated gene in various human cancer tissues, especially in ovary, liver, and lung (Lee et al., 2007a). CUG2 was determined to be a nuclear protein that exhibited high proto-oncogenic activities when overexpressed in NIH3T3 mouse fibroblast cells. To identify other cellular functions of CUG2, we performed yeast two-hybrid screening and identified CENP-T, a component of CENP-A nucleosome complex in the centromere, as an interacting partner of CUG2. Moreover, CENP-A, the principle centromeric determinant, was also found in complex with CENP-T/CUG2. Immunofluorescent staining revealed the co-localization of CUG2 with human centromeric markers. Inhibition of CUG2 expression drastically affected cell viability by inducing aberrant cell division. We propose that CUG2 is a new component of the human centromeric complex that is required for proper chromosome segregation during mitosis.

$F_2$-Monosomic Analysis of Plant Height in Triticum Cultivar Crosses Involving 'Diplomat' and 'Caribo' Monosomic Lines (밀의 초장결정 유전자분석)

  • Young-am, Chae
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.27 no.3
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    • pp.235-237
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    • 1982
  • $F_2$ progenies from the crosses between 'Caribo' monosomic lines and 'Diplomat' revealed significant differences in plant height in 7 $F_2$ populations. Well known effects of monosomic constritution of group 2 homoeologues and chromosome 5A sufficiently well explain reduced or increased plant height in these crosses respectively. Minor gene effects were recognized from 'Diplomat' chromosomes 3B, 6A and 7A and interpreted to explain or to contribute to genetic control of the rather small differences in plant height between cv. 'Caribo' and 'Diplomat'.

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On Weakly Prime and Weakly 2-absorbing Modules over Noncommutative Rings

  • Groenewald, Nico J.
    • Kyungpook Mathematical Journal
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    • v.61 no.1
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    • pp.33-48
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    • 2021
  • Most of the research on weakly prime and weakly 2-absorbing modules is for modules over commutative rings. Only scatterd results about these notions with regard to non-commutative rings are available. The motivation of this paper is to show that many results for the commutative case also hold in the non-commutative case. Let R be a non-commutative ring with identity. We define the notions of a weakly prime and a weakly 2-absorbing submodules of R and show that in the case that R commutative, the definition of a weakly 2-absorbing submodule coincides with the original definition of A. Darani and F. Soheilnia. We give an example to show that in general these two notions are different. The notion of a weakly m-system is introduced and the weakly prime radical is characterized interms of weakly m-systems. Many properties of weakly prime submodules and weakly 2-absorbing submodules are proved which are similar to the results for commutative rings. Amongst these results we show that for a proper submodule Ni of an Ri-module Mi, for i = 1, 2, if N1 × N2 is a weakly 2-absorbing submodule of M1 × M2, then Ni is a weakly 2-absorbing submodule of Mi for i = 1, 2

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.

Design and fabrication of the 2.4 to 2.5 GHz voltage controlled oscillator using microstrip patch antenna (마이크로스트립 패치 안테나를 이용한 2.4 ~ 2.5GHz 에서 동작하는 전압 조정 발진기의 설계 및 제작)

  • 황재호;명노훈
    • Journal of the Korean Institute of Telematics and Electronics A
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    • v.33A no.2
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    • pp.78-86
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    • 1996
  • Solid-state devices can be directly integrated with a planar antenna to form active antenna elements. In this paper, the voltage controlled oscillator (VCO) is designed and fabricated at 2.4 to 2.5 GHz using a microstrip patch antenna. A varactor diode is used as avariable reactance. The predicted frequency tuning range of the VCO is 2.448 to 2.498 GHz in the design procedure and the fabricated VCO has 2.446 to 2.498 GHz frequency tuning range when the varactor tuning voltage is varied from 0 to 11V. Transmitted power output of the patch antenna which serves both as a rsonator and a radiating element for VCO is about 18 mW over this tuning range.

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