• Title/Summary/Keyword: irreversible inhibition

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Role of glutamine synthetase as as regulator of nitrogenase in rhodopseudomonas sphaeroides D-230 (광합성 세균에 있어서의 질소고정효소 합성 조절자로서의 glutamine synthetase의 역할)

  • 이혜주
    • Korean Journal of Microbiology
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    • v.24 no.2
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    • pp.113-118
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    • 1986
  • Optimum temperature and pH of glutamine synthetase activity (E.C. 3.6.1.2.) of R. sphaeroides D-230 was $35^{\circ}C$ and 6.8, respectively. The adenylated state of GS in R. sphaeroides D-230 was stabilized by addition of 0.2mg/ml of cethyltrimethylammoniumbromide. Valine, histidine, proline, isoleucine, and lysine were good nitrogen source for the growth of R. sphaeroides D-230. The growth of R. sphaeroides D-230 in $N_2,\;NaNO_3\;or\;NH_4Cl$ as sole nitrogen source was lower than in any otherculture conditions. GS activity was inhibited, more or less, by various amino acid. THe relative inhibition rate of the enzyme by added 7mM arginine, $NH_4Cl,\;N_2,\;and\;NaNO_3$ was 63.8%, 26.79%, 6.24%, and 10.64%, drespectively. THe hydrogen evolution of R. sphaeroides D-230 grown in N-limited media was inhibited by 0.1mM MSX, irreversible GS inhibitor. GS activity was completely inhibited by 1.0mM MSX but ammonia released maximally at the same concentration of MSX. Ammonia release by added MSX was increased up to 1.0mM MS, but decreased above 1.0mM MSX. It is probably due to inhibition of nitrogenase actixity by MSX. Nitrogenase activity was not inhibited at low concentration of MSX. These results suggests that the inhibition of nitrogenase activity by ammonia is mediated by products of ammonia assimilation rather than by ammonia itself.

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A Study on the Inhibition Effect of Metal Corrosion Using Organic Compound Containing an Amine Group (아민기를 가진 유기물을 사용한 금속의 부식억제효과)

  • Park, Keun-Ho
    • Journal of the Korean Applied Science and Technology
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    • v.27 no.3
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    • pp.361-369
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    • 2010
  • A study on the corrosion inhibition of metals is important in many industrial applications (carbon steel, copper, aluminum, SUS 304, nickel). In this study, we investigated the C-V diagrams related to the surface corrosion of metals. It was observed through the SEM that the surface corrosion state of the various metals had the corrosion potential by the scan rate and the organic inhibitor containing an amine group. We determined to measure cyclic voltammetry using the three-electrode system. The measurement of oxidation and reduction ranged from -1350mV to 1650mV. The scan rate was 50, 100, 150, and 200mV/s. It turned out that the C-V characterization of SUS 304 was irreversible process caused by the oxidation current from the cyclic voltammogram. After adding organic inhibitors, the adsorption film was constituted, and the passive phenomena happened. As a result, it was revealed that the inhibition effect of metal corrosion depends on the molecular interaction, and the interaction has influence on the adsorption complex.

Role of Phospholipase $A_2$ in Oxidant-induced Alteration in Phosphate Transport in Primary Cultured Rabbit Renal Proximal Tubule Cells

  • Park, Kwon-Moo;Ko, Sun-Hee;Woo, Jae-Suk;Jung, Jin-Sup;Lee, Sang-Ho;Kim, Yong-Keun
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.5
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    • pp.601-609
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    • 1998
  • The present study was undertaken to examine the role of phospholipase $A_2\;(PLA_2)$ in oxidant-induced inhibition of phosphate transport in primary cultured rabbit renal proximal tubule cells. Uptakes of phosphate and glucose were dose-dependently inhibited by an oxidant t-butylhydroperoxide (tBHP), and the significant inhibition appeared at 0.025 mM of tBHP, whereas tBHP-induced alterations in lipid peroxidation and cell viability were seen at 0.5 mM. tBHP stimulated arachidonic acid (AA) release in a dose-dependent fashion. A $PLA_2$ inhibitor mepacrine prevented tBHP-induced AA release, but it did not alter the inhibition of phosphate uptake and the decrease in cell viability induced by tBHP. tBHP-induced inhibition of phosphate transport was not affected by a PKC inhibitor, staurosporine. tBHP at 0.1 mM did not produce the inhibition of $Na^+-K^+-ATPase$ activity in microsomal fraction, although it significantly inhibited at 1.0 mM. These results suggest that tBHP can inhibit phosphate uptake through a mechanism independent of $PLA_2$ activation, irreversible cell injury, and lipid peroxidation in primary cultured rabbit renal proximal tubular cells.

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Cancer Energy Metabolism: Shutting Power off Cancer Factory

  • Kim, Soo-Youl
    • Biomolecules & Therapeutics
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    • v.26 no.1
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    • pp.39-44
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    • 2018
  • In 1923, Dr. Warburg had observed that tumors acidified the Ringer solution when 13 mM glucose was added, which was identified as being due to lactate. When glucose is the only source of nutrient, it can serve for both biosynthesis and energy production. However, a series of studies revealed that the cancer cell consumes glucose for biosynthesis through fermentation, not for energy supply, under physiological conditions. Recently, a new observation was made that there is a metabolic symbiosis in which glycolytic and oxidative tumor cells mutually regulate their energy metabolism. Hypoxic cancer cells use glucose for glycolytic metabolism and release lactate which is used by oxygenated cancer cells. This study challenged the Warburg effect, because Warburg claimed that fermentation by irreversible damaging of mitochondria is a fundamental cause of cancer. However, recent studies revealed that mitochondria in cancer cell show active function of oxidative phosphorylation although TCA cycle is stalled. It was also shown that blocking cytosolic NADH production by aldehyde dehydrogenase inhibition, combined with oxidative phosphorylation inhibition, resulted in up to 80% decrease of ATP production, which resulted in a significant regression of tumor growth in the NSCLC model. This suggests a new theory that NADH production in the cytosol plays a key role of ATP production through the mitochondrial electron transport chain in cancer cells, while NADH production is mostly occupied inside mitochondria in normal cells.

Flavonoids: Potential Antiinflammatory Agents

  • Kim, Hyun-Pyo;Son, Kun-Ho;Chang, Hyun-Wook;Kang, Sam-Sik
    • Natural Product Sciences
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    • v.2 no.1
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    • pp.1-8
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    • 1996
  • Flavonoids are widely distributed polyphenol compounds in plant kingdom and known to possess varieties of biological/pharmacological activities in vitro and in vivo. A search for antiinflammatory/immunoregulatory flavonoids as potential therapeutic agents has been continued, since serious side effects of currently used nonsteroidal and steroidal antiinflammatory drugs limit their long term uses for the inflammatory disorders. In this reserch, various flavonids were isolated and tested for their in vivo antiinflammatory activity and in vitro inhibitory activity of lymphocyte proliferation. Using a mouse ear edema assay, it was found that certain flavones/flavonols possess mild antiinflammatory activity and a C-2,3-double bond might be essential. Isoflavones were less active. These flavonoids inhibited in vitro lymphocyte proliferation, relatively specific for T-cell proliferation $(IC_{50}=1-10\;{\mu}M)$ and the inhibition was reversible. We have also tested several biflavonoid derivatives, since we recently found that biflavones were phospholipase $A_2$ inhibitors. It was demonstrated that biflavones such as ochnaflavone and ginkgetin inhibited lymphocyte proliferation induced by both concanavaline A and lipopolysaccharide. The inhibition was irreversible in contrast to that of flavones/flavonols. And antiinflammatory activity of biflavonoids are discussed.

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Development of Mechanism-based Irreversible Inhibitors of S-Adenosylhomocysteine Hydrolase as Borad-spectrum Antiviral Agents

  • Lee, Kang-Man;Moon, Hyung-Ryong;Choi, Won-Jun;Park, Jae-Gyu;Shin, Dae-Hong;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.186-190
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    • 2002
  • S- Adenosylhomocysteine hydrolase $(SAH)^1$ catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine. Inhibition of this enzyme accumulates S-adenosylhomocysteine, which in turn inhibits S-adenosyl-L-methionine dependent transmethylation, resulting in no formation of the capped methylated structure at the 5'-terminus of viral mRNA. Thus, S-adenosylhomocysteine hydrolase has been an attractive target for the development of broad spectrum of antiviral agents. (omitted)

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Epoxyalkanoyls as Novel ACE Inhibitors

  • P. Choo, Hea-Young;Yoon, Hea-Ran;Park, Hwha-Soon;Kim, Dong-Hyun;Park, Jong-Sei;Kim, Dong-H.
    • Archives of Pharmacal Research
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    • v.21 no.2
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    • pp.168-173
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    • 1998
  • The epoxyalkanoyl derivatives were designed and synthesized as ACE inhibitors. Coupling of unsaturated carboxylic acids with amino acids and following epoxidation with dimethyldioxirane gave the epoxyalkanoyls with high yield. The inhibitory activity of synthesized compounds on angiotensin converting enzyme was $IC_{50}$ values of 0.06~5.5 ${\mu}M$.

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The Mitochondrial Tricarboxylate Carrier of Silver Eel: Chemical Modification by Sulfhydryl Reagents

  • Capobianco, Loredana;Impagnatiello, Tecla;Ferramosca, Alessandra;Zara, Vincenzo
    • BMB Reports
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    • v.37 no.5
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    • pp.515-521
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    • 2004
  • The tricarboxylate (or citrate) carrier was purified from eel liver mitochondria and functionally reconstituted into liposomes. Incubation of the proteoliposomes with various sulfhydryl reagents led to inhibition of the reconstituted citrate transport activity. Preincubation of the proteoliposomes with reversible SH reagents, such as mercurials and methanethiosulfonates, protected the eel liver tricarboxylate carrier against inactivation by the irreversible reagent N-(1-pyrenyl)maleimide (PM). Citrate and L-malate, two substrates of the tricarboxylate carrier, protected the protein against inactivation by sulfhydryl reagents and decreased the fluorescent PM bound to the purified protein. These results suggest that the eel liver tricarboxylate carrier requires a single population of free cysteine(s) in order to manifest catalytic activity. The reactive cysteine(s) is most probably located at or near the substrate binding site of the carrier protein.

Effect of Amino Acids on Anoxia-induced Cell Injury

  • Jung, Soon-Hee
    • Biomedical Science Letters
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    • v.7 no.3
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    • pp.127-131
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    • 2001
  • This study was undertaken to examine the effect of amino acids on anoxia-induced cell injury in rabbit renal cortical slices. In order to induce anoxic cell injury, slices were exposed to a 100% $N_2$ atmosphere and control slices were exposed to 100% $O^2$. Irreversible cell injury was estimated by measuring lactate dehydrogenase (LDH) release and alterations in renal cell function were examined by measuring p-aminohippurate (PAH) uptake. Anoxia caused the increase in LDH release in a time-dependent manner. Glycine and glutathione almost completely prevented anoxia-induced LDH release. Of amino acids tested, glycine and alanine exerted the protective effect against anoxia-induced cell injury. However, asparagine with amide side chain, leucine and valine with hydrocarbon side chain, and basic amino acids (lysine, histidine, and arginine) were not effective. Anoxia-induced inhibition of PAM uptake was prevented by glycine. ATP content was decreased by anoxia, which was not affected by glycine. Anoxia-induced depletion of glutathione was significantly prevented by glycine. These results suggest that neutral amino acids with simple structure exert the Protective effect against anoxia-induced cell injury the involvement of specific interaction of amino acids and cell structure.

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Fiber-optic biosensor for the detection of organophosphorus compounds in a contaminated water (Part II : The signal analysis and simulation) (오염수 내의 유기인 화합물의 측정을 위한 광섬유 바이오센서 (제 2 부 : 신호분석 및 수치모사))

  • Choi, Jeong-Woo;Min, Jun-Hong;Lee, Won-Hong
    • Journal of Sensor Science and Technology
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    • v.3 no.2
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    • pp.16-23
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    • 1994
  • Developed fiber-optic biosensor for the detection of organophosphorus compounds in a contaminated water needs the analysis of an enzyme kinetics and the transport phenomena in the reaction part to analyze the sensor signal and to design the sensor. The enzyme inhibition kinetics was investigated and the reactor model was proposed to design the reaction part in the proposed sensor. Since the acetylcholinesterase was inhibited by the organophosphorus compounds, experiments for enzyme inhibition reaction were performed from 0 to 2 ppm to be detected by the developed sensor, and irreversible enzyme inhibition kinetics was proposed. The reactor parts were divided into the two phases, i.e. bulk phase and immobilized enzyme layer, to analyze the flow and diffusion. Sensor signal was able to be analyzed based on the total reactor model established by linking the enzyme reaction kinetics. Based on the proposed model, the effects of loading enzyme amount and enzyme layer thickness on the magnitude of readout signal were simulated.

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