• Title/Summary/Keyword: Selective agent

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Induction of Pacemaker Currents by DA-9701, a Prokinetic Agent, in Interstitial Cells of Cajal from Murine Small Intestine

  • Choi, Seok;Choi, Jeong June;Jun, Jae Yeoul;Koh, Jae Woong;Kim, Sang Hun;Kim, Dong Hee;Pyo, Myoung-Yun;Choi, Sangzin;Son, Jin Pub;Lee, Inki;Son, Miwon;Jin, Mirim
    • Molecules and Cells
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    • v.27 no.3
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    • pp.307-312
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    • 2009
  • The interstitial cells of Cajal (ICC) are pacemaking cells required for gastrointestinal motility. The possibility of whether DA-9701, a novel prokinetic agent formulated with Pharbitis Semen and Corydalis Tuber, modulates pacemaker activities in the ICC was tested using the whole cell patch clamp technique. DA-9701 produced membrane depolarization and increased tonic inward pacemaker currents in the voltage-clamp mode. The application of flufenamic acid, a non-selective cation channel blocker, but not niflumic acid, abolished the generation of pacemaker currents induced by DA-9701. Pretreatment with a $Ca^{2+}$-free solution and thapsigargin, a $Ca^{2+}$-ATPase inhibitor in the endoplasmic reticulum, abolished the generation of pacemaker currents. In addition, the tonic inward currents were inhibited by U-73122, an active phospholipase C inhibitor, but not by $GDP-{\beta}-S$, which permanently binds G-binding proteins. Furthermore, the protein kinase C inhibitors, chelerythrine and calphostin C, did not block the DA-9701-induced pacemaker currents. These results suggest that DA-9701 might affect gastrointestinal motility by the modulation of pacemaker activity in the ICC, and the activation is associated with the non-selective cationic channels via external $Ca^{2+}$ influx, phospholipase C activation, and $Ca^{2+}$ release from internal storage in a G protein-independent and protein kinase C-independent manner.

CHANGE OF THE INVASIVENESS WITH SELECTIVE COX-2 INHIBITION IN AN ORAL SQUAMOUS CELL CARCINOMA CELL LINE, KB ; PRELIMINARY IN VITRO STUDY (선택적 COX-2 저해를 통한 구강암세포주 KB의 침습성 변화에 관한 예비연구)

  • Lee, Eun-Jin;Kim, Myung-Jin;Myoung, Hoon
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.33 no.2
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    • pp.103-108
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    • 2007
  • Cyclooxygenase-2 (Cox-2) is known as one of the critical factor in carcinomas of various organs. However, the importance of Cox-2 in oral squamous cell carcinoma has not been fully described yet. The purpose of this study is to evaluate the anti-cancer effect of selective cox-2 inhibitor, celecoxib in an oral squamous cell carcinoma cell line, KB with respect to cytotoxicity test, in vitro invasion and MMP-2 expression. In cytotoxicity test, celecoxib treated group showed definitely concentration dependent cytotoxicity. In addition, administration of celecoxib reduced the invasive potential of KB cell line significantly in invasion assay. However, there was no remarkable difference of the MMP-2 expression between the celecoxib treated group and the control group. Considering these data, celecoxib had a potential cytotoxic agent to oral squamous cell carcinoma cells. Also, it had anti-invasive property without acting on the MMP-2 expression mechanism. Therefore, it was postulated that celecoxib had the possibility of anti-cancer agent in treatment strategies of oral squamous cell carcinoma.

A study on selective hybrid-structure film fabricated by 355nm UV-pulsed laser processing (355nm UV 레이저를 이용한 선택적 하이브리드 구조 필름의 제작에 관한 연구)

  • Kim, Myung-Ju;Lee, Sang-Jun;Shin, Bo-Sung
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.16 no.5
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    • pp.2979-2984
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    • 2015
  • This paper has presented a new foaming technology of selective hybrid-structured polymer film with expanded pores. The porous structure of closed pore was firstly fabricated by applying the 355nm UV-pulsed laser to 0.1mm thick film that was uniformly mixed with PP pellets, copper powder, and CBA (Chemical Blowing Agent). In order to expand pore size of closed-cell shape, LAMO(Laser Aided Micro pore Opening) processing was conducted to heat the copper powder, and then the bigger pore size of closed-cell more than existing pore size was successfully formed because of rapid conduction of heated metal powder. From the experimental results, various process parameters such as laser fluence, intensity, scan rate, spot size and density of powder and CBA were considerably considered to reveal the correlation among the pore characteristics. In the future, a function experiment will be carried out to use the hybrid film of industrial applications.

Simultaneous Removal of NO and SO2 using Microbubble and Reducing Agent (마이크로버블과 환원제를 이용한 습식 NO 및 SO2의 동시제거)

  • Song, Dong Hun;Kang, Jo Hong;Park, Hyun Sic;Song, Hojun;Chung, Yongchul G.
    • Clean Technology
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    • v.27 no.4
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    • pp.341-349
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    • 2021
  • In combustion facilities, the nitrogen and sulfur in fossil fuels react with oxygen to generate air pollutants such as nitrogen oxides (NOX) and sulfur oxides (SOX), which are harmful to the human body and cause environmental pollution. There are regulations worldwide to reduce NOX and SOX, and various technologies are being applied to meet these regulations. There are commercialized methods to reduce NOX and SOX emissions such as selective catalytic reduction (SCR), selective non-catalytic reduction (SNCR) and wet flue gas desulfurization (WFGD), but due to the disadvantages of these methods, many studies have been conducted to simultaneously remove NOX and SOX. However, even in the NOX and SOX simultaneous removal methods, there are problems with wastewater generation due to oxidants and absorbents, costs incurred due to the use of catalysts and electrolysis to activate specific oxidants, and the harmfulness of gas oxidants themselves. Therefore, in this research, microbubbles generated in a high-pressure disperser and reducing agents were used to reduce costs and facilitate wastewater treatment in order to compensate for the shortcomings of the NOX, SOX simultaneous treatment method. It was confirmed through image processing and ESR (electron spin resonance) analysis that the disperser generates real microbubbles. NOX and SOX removal tests according to temperature were also conducted using only microbubbles. In addition, the removal efficiencies of NOX and SOX are about 75% and 99% using a reducing agent and microbubbles to reduce wastewater. When a small amount of oxidizing agent was added to this microbubble system, both NOX and SOX removal rates achieved 99% or more. Based on these findings, it is expected that this suggested method will contribute to solving the cost and environmental problems associated with the wet oxidation removal method.

A Study on New Selective Agent Attack Technology in Windows System (윈도우시스템에서 새로운 선택적 에이전트 공격 기술에 관한 연구)

  • Kim, Yeong-Woo;Lim, Young-Hwan;Park, Won-Hyung
    • Journal of Korea Multimedia Society
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    • v.15 no.2
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    • pp.226-233
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    • 2012
  • Recently, Like we saw with 3.4 DDoS Cyber Terror, a behavior of cyber terror becomes increasingly more complicated, sophisticated and larger, and there has been largely damage on industry, the general economy. For responding cyber terrors which occur in the future, we should recognize security holes of system which isn't exposed yet before attacker in advance as we anticipate and implement new technique of cyber attack which not exist hitherto. We design and implement a new technique of cyber attack; it seems to us that a server denies agent' service by altering value of registry in windows system. Network connections of agent are restricted to the new technique we suggest as the a value of registry is changed to a less value than a necessary value and there has happened packet loss by attacker.

Effects of Contrast Agent Concentration on the Signal Intensity and Turbo Factor of TSE and Slice-selective IR in T1-weighted Contrast Imaging

  • Han, Yong Soo;Lee, Soo Chul;Lee, Dong Yong;Choi, Jiwon;Lee, Jong Woong;Kweon, Dae Cheol
    • Journal of Magnetics
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    • v.21 no.1
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    • pp.115-124
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    • 2016
  • The present study analyzes T1 TSE and T1 slice sel. IR (dark_fluid) signal strength according to the degree of gadolinium contrast agent dilution and analyzes the turbo factors with regard to changes in the maximum and overall signal strength to study correlations between changes and signal-to-noise ratios (SNRs) and compare peak-to-peak SNR (PSNR) enhancement in order to improve the quality of T1-weighted images. Enhancement TR (600 msec) evaluated to determine the T1 TSE turbo factor and obtain the maximum signal strength, T1WI were used sequentially to experiment with turbo factors_1-4. T1 slice sel. IR (dark-fluid) was used to sequentially test turbo factors_2-5 but not turbo factor_1 at a TR (1500 msec) and compare data at an increase in T1 of 900 msec. The T1 TSE was reduced according to the contrast agent concentration. Phantom signal strength increased, whereas turbo factors_1-4 exhibited maximum signal strength at a concentration of 3 mmol, followed by a gradual decrease. In the turbo factors_2-5, the signal strength increased sharply to maximum signal strength at 0.7 mmol, followed by a reduction. T1 TSE had a greater maximum signal strength than did T1 slice sel. IR (dark_fluid). A comparison of SNR found that T1 TSE imaging was superior (33.3 dB) in turbo factor_1 and T1 slice sel. IR (dark_fluid) was highest (33.9 dB) at turbo factor_5. A PSNR comparison analysis was not sufficient to distinguish between the images obtained with both techniques at 30 dB or higher under all experimental conditions.

Effects of Seman Armenicae and Radix Trichosanthis on the iNOS expression and superoxide formation in the RAW264.7 cells (행인 과루인 추출물이 마우스 대식세포주인 RAW264.7 세포주의 iNOS 발현 및 Superoxide 형성에 미치는 영향)

  • Park, Joug-Un;Moon, Seok-Jae;Moon, Goo;Won, Jin-Hee
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.5 no.1
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    • pp.137-150
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    • 1999
  • Macrophage play a major role in host defence against infection and tumor development and this activity is regulated through the production of several mediators. In particular, the production of NO by macrophages mediates killing or growth inhibition of tumor cells, bacteria, fungi and parasites. However, over-expression of iNOS by various stimuli, resulting in over-production of NO, contributes to the pathogenesis of septic shock and some inflammator and auto-immune disease. Therefore, it would be valuable to develop potent and selective inhibitors of for potential therapeutic use. Thus the agent that supprees the expression of iNOS mRNA or enzyme protein will be usefull for the prevention of various diseases. We are intersted in identifying selective inhibitiors of iNOS which might be useful intreating inflammatory human diseases. In summary, we have demenstrated that scopoletin, isolated from Seman Armenicae and Radix Trichosanthis the production of NO induced by $IFN-\gammer$ plus LPS in RAW 264.7 macrophages, The mechanism for the inhibition of NO production was due to suppression of the expression of iNOS mRNA or enzyme protein.

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Selective Cytotoxicity of New Platinum (II) Complex Containing 1,3-Bis-phenylthiopropane (1,3-비스페닐치오 프로판을 배위자로 한 백금 (II)착체의 선택적 세포독성)

  • 노영수;윤기주;이경태;장성구;정지창
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.369-377
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    • 1999
  • A new series of highly water soluble platinum(II) complexes {Pt(II)[1,3-bis(phenylthio) propane](trans- -1,2-diaminocyclohexane) (PC-1) and Pt(II)[1,3-bis-(phenythio)propane] cis-1,2-diaminocyclohexane(PC-2)} were synthesized, and characterized by their elemental analysis and by various spectroscopic techniques[infrared(IR), 13C-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new Pt(II) complexes was tested against P-388 and L-1210 mouse lymphocytic leukemia cell lines, PC-14 / P, PC-14/ADM and PC-14 / CDDP human pulmonary adenocarcinima, DU-145 human prostate carcinoma, HT-1376 human bladder carcinoma, ZR-75-1 human breast carcinoma, MKN-45/P and MKN-45/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2.5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 showed active against L-1210, P-388 leukemia, human lung, stomach, prostate, bladder and breast cancer cell lines, and the antitumor activity of these compounds were comparable or superior to those of PC-2 and displatin. The nephrotoxicities of PC-1 and PC-2 were found quite less than that of cisplatin using MTT and [3H] thymidine uptake in rabbit proximal tubule cells and human kidney cortical cells. Based on these results, this novel platinum (II) complex compound (PC-1) represents a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

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Selective Reduction by Lithium Bis- or Tris(dialkylamino)aluminum Hydrides. VIII. Reaction of Lithium Tripiperidinoaluminum Hydride in Tetrahydrofuran with Selected Organic Compounds Containing Representative Functional Groups

  • 차진순;이재철;주영철
    • Bulletin of the Korean Chemical Society
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    • v.18 no.8
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    • pp.890-895
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    • 1997
  • The approximate rates and stoichiometry of the reaction of excess lithium tripiperidinoaluminum hydride (LTPDA), an alicyclic aminoaluminum hydride, with selected organic compounds containing representative functional groups under the standardized conditions (tetrahydrofuran, 25°) were examined in order to define the reducing characteristics of the reagent for selective reductions. The reducing ability of LTPDA was also compared with those of the parent lithium aluminum hydride (LAH) and lithium tris(diethylamino)aluminum hydride (LTDEA), a representative aliphatic aminoaluminum hydride. In general, the reactivity of LTPDA toward organic functionalities is weaker than LTDEA and much weaker than LAH. LTPDA shows a unique reducing characteristics. Thus, benzyl alcohol, phenol and thiols evolve a quantitative amount of hydrogen rapidly. The rate of hydrogen evolution of primary, secondary and tertiary alcohols is distinctive. LTPDA reduces aldehydes, ketones, esters, acid chlorides and epoxides readily to the corresponding alcohols. Quinones, such as p-benzoquinone and anthraquinone, are reduced to the corresponding diols without hydrogen evolution. Tertiary amides and nitriles are also reduced readily to the corresponding amines. The reagent reduces nitro compounds and azobenzene to the amine stages. Disulfides are reduced to thiols, and sulfoxides and sulfones are converted to sulfides. Additionally, the reagent appears to be a good partial reducing agent to convert primary carboxamides into the corresponding aldehydes.

Enhancing Anti-Cancer Therapy with Selective Autophagy Inhibitors by Targeting Protective Autophagy

  • Jae-Sung Park;Min Ju Lee;Seong Bin Jo;Young Ae Joe
    • Biomolecules & Therapeutics
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    • v.31 no.1
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    • pp.1-15
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    • 2023
  • Autophagy is a process of eliminating damaged or unnecessary proteins and organelles, thereby maintaining intracellular homeostasis. Deregulation of autophagy is associated with several diseases including cancer. Contradictory dual roles of autophagy have been well established in cancer. Cytoprotective mechanism of autophagy has been extensively investigated for overcoming resistance to cancer therapies including radiotherapy, targeted therapy, immunotherapy, and chemotherapy. Selective autophagy inhibitors that directly target autophagic process have been developed for cancer treatment. Efficacies of autophagy inhibitors have been tested in various pre-clinical cancer animal models. Combination therapies of autophagy inhibitors with chemotherapeutics are being evaluated in clinal trials. In this review, we will focus on genetical and pharmacological perturbations of autophagy-related proteins in different steps of autophagic process and their therapeutic benefits. We will also summarize combination therapies of autophagy inhibitors with chemotherapies and their outcomes in pre-clinical and clinical studies. Understanding of current knowledge of development, progress, and application of cytoprotective autophagy inhibitors in combination therapies will open new possibilities for overcoming drug resistance and improving clinical outcomes.