• 제목/요약/키워드: Inhibition constant

검색결과 193건 처리시간 0.023초

Chemical Inhibition of Cell Recovery after Irradiation with Sparsely and Densely Ionizing Radiation

  • Evstratova, Ekaterina S.;Kim, Jin-Hong;Lim, Young-Khi;Kim, Jin Kyu;Petin, Vladislav G.
    • 방사선산업학회지
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    • 제10권4호
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    • pp.199-204
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    • 2016
  • The dependence of cell survival on exposure dose and the duration of the liquid-holding recovery (LHR) was obtained for diploid yeast cells irradiated with ionizing radiation of different linear energy transfer (LET) and recovering from radiation damage without and with various concentrations of cisplatin - the most widely used anticancer drug. The ability of yeast cells to recover from radiation damage was less effective after cell exposure to high-LET radiation, when cells were irradiated without drug. The increase in cisplatin concentration resulted in the disappearance of this difference whereas the fraction of irreversible damage was permanently enlarged independently of radiation quality. The probability of cell recovery was shown to be constant for various conditions of irradiation and recovery. A new mechanism of cisplatin action was suggested according with which the inhibition of cell recovery after exposure to ionizing radiations was completely explained by the production of irreversible damage.

Rat Liver $\beta$-Glucuronidase; Its Purification and Inhibition Studies

  • Jeong, Han-Seung;Yang, Chul-Hak
    • Bulletin of the Korean Chemical Society
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    • 제6권5호
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    • pp.312-317
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    • 1985
  • ${\beta}$-Glucuronidase (EC 3.2.1.31) which hydrolizes D-glucuronate from ${\beta}$-D-glucuronide was purified from rat liver, using ammonium sulfate fractionation, DEAE-cellulose chromatography, Concanavalin-A Sepharose 4B chromatography and gel filtration on Sephadex G-200. This enzyme has the molecular weight of 280,000 daltons by gel filtration and 75,000 daltons by SDS-polyacrylamide gel electrophoresis. As its funtion is reverse of detoxification in the liver, the inhibition of the enzyme was tested with extracts of several food products and medicinal herbs, some are known as anti-cancer agents. Among them, Panax ginseng and Cortnellus shiiake inhibited the enzyme competitively and the $K_1$ values were $9.22 {\times}\;10^{-2}$ and 0.102 mg/ml, respectively. These inhibitors strongly bound to DEAE-cellulose. The negatively charged amino acids, L-aspartate and L-glutamate, inhibited the enzyme, and $K_1$ value of L-aspartate was 0.80 mM. The interaction between ${\beta}$-glucuronidase and p-nitrophenyl-${\beta}$-D-glucuronide was found to involve ionic forces by the effect of ionic strength on the kinetic constant, Vmax/Km. It was inferred from these findings that cationic group at the active center of the enzyme is probably involved in attacking the substrate.

Bacterial neuraminidase inhibitory linarin from Dendranthema zawadskii

  • Ju Yeon Kim;Jae Yeon Park;Yun Gon Son;Kyu Lim Kim;Jeong Yoon Kim
    • Journal of Applied Biological Chemistry
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    • 제66권
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    • pp.1-6
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    • 2023
  • Dendranthema zawadskii is a one of the popular plants as native in South Korea. In this study, linarin was isolated and purified using silica-gel, Diaion, and Sephadex LH-20 from the aerial parts of D. zawadskii. The chemical structure was completely identified through spectroscopic data including 1D, 2D nucleic magnetic resonance, and HRFABMS. Furthermore, linarin inhibited the bacterial neuraminidase (BNA) activity with 13.5 μM of IC50 dose-dependently. Through the enzyme kinetic experiments, linarin as BNA inhibitor exhibited a typical noncompetitive inhibition mode which Km was contestant and Vmax decreased as the concentration of the inhibitor increased. It was further identified that the inhibition constant was 16.0 μM. Linarin was the most abundance metabolite in the aerial part of D. zawadskii extract by UHPLC-TOF/MS analysis. Therefore, D. zawadskii and its main component are expected that it can be effectively used for the infection and inflammation caused by bacteria.

김치에서 분리한 젖산균의 미생물 생육 저해 (Microbial Inhibition of Lactic Strains isolated from Kimchi)

  • 박연희;권정주;조도현;김수일
    • Applied Biological Chemistry
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    • 제26권1호
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    • pp.35-40
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    • 1983
  • 김치에 분리한 젖산균 20주(株)의 Escherichia coli, Staphylococcus aureus 등 5종의 Test organism에 대한 생육저해실험 결과 가장 생육저해능력이 큰 A7 (Pediococcus cerevisiae)와 C4 (Leuconostoc spp.)를 선발하였다. 이 두 균주를 각각 Escherichia coli와 동시에 접종하여 배양한 결과 초기부터 Escherichia coli의 생육을 억제하였으며 약 24시간 후부터는 Escherichia coli의 균수가 급격히 감소하였다. Staphylococcus aureus와 Bacillus cereus에 대하여도 .대체로 비슷한 생육억제작용을 나타내었다. 세가지 Test organism 모두 A7과 배양할 경우 C4의 경우보다 더 큰 death rate constant를 나타내었다 이 혼합 배양액에 catalase를 첨가한 경우 생육저해현상에 영향이 없었으므로 이 두 균주의 생육억계작용은 $H_2O_2$ 생성과 관련이 없는 것으로 나타났다. A7의 배양 여액만을 Escherichia coli 배양액에 첨가한 경우에도 A7균주의 혼합 배양과 동일한 생육저해 현상을 보였으나 여액을 $80^{\circ}C$에서 30분간 열처리후 가하였을 때는 생육저해작용이 거의 나타나지 않을 뿐 아니라 여액에 trypsin 처리한 경우에도 생육저해작용은 크게 억제되었다. 이상의 결과로 A7 균주의 생육저해작용은 단백질류 생육저해물질의 생산에 의한 것이라고 추정할 수 있다.

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Inhibition of a Neutral Form of Sphingomyelinase by Alkylthioureido-l,3-propandiols, KY353X Series

  • Jung, Sang-Mi;Jeong, Eui-Man;Jo, Dong-Hwawn;Chin, Mi-Reyoung;Jun, Hyung-Jin;Kim, Yong-Hyun;Jeon, Hyung-Jun;Lee, Dong-Hun;Park, Mi-Ja;Oh, Mi-Jung;Yim, Chul-Bu;Kim, Dae-Kyong
    • Biomolecules & Therapeutics
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    • 제11권3호
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    • pp.169-173
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    • 2003
  • Alkylthioureido-1,3-propandiols (KY353X series) were synthesized and evaluated as inhibitors for neutral sphingomyelinase (N-SMase). To examine whether KY353X series inhibit N-SMase, we purified the N-SMase from bovine brain. The N-SMase was partially purified by sequential chromatographies of DEAE-Cellulose anionic exchange and phenyl-5PW hydrophobic HPLC. These seqeuntial procedures for N-SMase resulted in a 67-fold purification and excluded other isoforms of SMase. Based on in vitro assay, KY353X series inhibited N-SMase activity in time, concentration-dependent manners and completely inactivated N-SMase at 50 $\mu$M. In particular, KY3535 and KY3536 inhibited more effectively than the others. To further determine the .inhibitory pattern, a Dixon plot was constructed, to showing that the inhibition by KY3535 and KY3536 were competitive. The inhibition constant (Ki) of KY3535 and KY3536 was 1.7 $\mu$M and 2.5$\mu$M in 100 mM Tris-HCl buffer, pH 7.0, respectively.

후지 사과 Polyphenol Oxidase의 특성 및 활성억제 (Characteristics and Inhibition of Polyphenol Oxidase from Fuji Apples)

  • 최언호;정동선;조남숙;심영현
    • Applied Biological Chemistry
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    • 제30권3호
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    • pp.278-284
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    • 1987
  • 사과의 건조, 가공 중의 갈변을 방지하기 위한 기초 조사로서 후지 사과로부터 추출한 crude polyphenol oxidase의 특성과 열에 대한 저항성, 갈변 저해제의 저해 효과 등을 조사하였다. Catechol을 기질로 사용하였을 때 polyphenol oxidase의 최적 pH는 5.5, 최적온도는 $20^{\circ}C$, $K_m$ 값은 0.14M이었고, 열불활성화는 유사일차반응을 보였으며 이때 활성화에너지$(E_a)$와 Z값은 각각 23.0cal/kmol, $19.7^{\circ}C$였다. 기질에 따른 친화력은 o-diphenol, 특히 chlorogenic acid에 대하여 높았고, monophenol과 m-diphenol, p-diphenol에 대해서는 나타나지 않았다. Polyphenol oxidase에 의한 갈변은 thiourea와 potassium metabisulfite는 10mM에서, L-cysteine과 ascorbic acid, sodium diethyldithiocarbamate는 1mM에서 현저하게 저해되었다.

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Pseudomonas synxantha A3가 생성하는 siderophore A3에 관한 연구 (Biochemical studies of the siderophore A3 produced by pseudomonas synxantha A3)

  • 전홍기;강호영;고철종;백형석
    • 미생물학회지
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    • 제29권5호
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    • pp.307-313
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    • 1991
  • A yellow-green, fluorescent siderophore A3 was extracellularly produced under iron-limited growth conditions from Pseudomonas synxantha A3. The physicochemical and biological properties of siderophore A3 were examined. The approxiamte molecular weights of the Fe(III)-siderophore A3-1 complex and Fe(III)-siderophore A3-2 complex were estimated to be about 1,300 and 1,100, respectively, by Bio-gel P2 gel exclusion chromatography. The molar ratio between the siderophore and the Fe(III)was 1.08 mole. The molecular weight of the complex could be calculated with this ratio and the new values were 1,150 and 960, respectively. The binding constant(K) between thesiderophore A3 and Fe(III) that determined by displacing the iron from the Fe(III)-siderophore complex with EDTA was 4.12*10$^{18}$ at pH 5.0. Siderophore A3 appeared to have antibacterial activity on several bacterial strains, however, ferric siderophore Ae complex did not show that activity. The cytotoxicity of siderophore A3 was obtained from Human Chronic Myelogenous Leudemia K562 cells. Inhibition concentration (50%)($IC_{50}$ ) was $0.17\mu$\{g/ml}.

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광합성 미세조류인 Chlorococcum littorale을 이용한 이산화탄소의 생물학적 고정화

  • 김태호;성기돈;이진석;이준엽;오상집;이현용
    • 한국미생물·생명공학회지
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    • 제25권3호
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    • pp.235-239
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    • 1997
  • Chlorococcum littorale has been grown in high $CO_2$ concentrations to utilize $CO_2$ gas in the polluted air. The effect of incident light intensity on the specific growth rate is expressed by a photoinhibition model, showing half- saturation constant, $K_0\;as\;8\;(W/m^2)$ and inhibition constant, Ki as 35 $(W/m^2)$. The maximum specific growth rate was also estimated as 0.095 (1/day) under this condition. This strain maintained the optimum growth rate in 20% of $CO_2$ gas but 50% of input $CO_2$ gas is the maximum concentration considering the economical efficiency. The maximum Specific $CO_2$ consumption rate, $qCO_2$ was measured as 17.48 (mg $CO_2/g$ dry wt./day) in batch cultivation, 11.2 (mg $CO_2/g$ dry wt./day) in fed-batch cultivation and 10.87 (mg $CO_2/g$ dry wt./day) at 0.065 (1/day) of dilution rate in continuous cultivation. The chemical composition of the biomass obtained from this process showed 32.5% of protein, 27.5% of lipid, 16.5% of carbohydrate and ash 11.7%.

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Candida parapsilosis에 의한 Xylitol 발효시 Arabinose가 미치는 영향

  • 오덕근;김상용
    • 한국미생물·생명공학회지
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    • 제25권2호
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    • pp.197-202
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    • 1997
  • Effect of arabinose on xylitol production from xylose by Candida parapsilosis KFCC 10875 was investigated at the different concentrations of arabinose. When the arabinose was added in xylose medium, the cell growth increased and the final cell concentration was maximum at 10 g/l arabinose. The consumption rate of arabinose was greatly lower than those of xylose and arabinose. Above 10 g/l arabinose, it was not completely consumed and then remained in the medium during xylitol fermentation. Estimated cell mass obtained from arabinose increased with increasing consumed arabinose. As arabinose concentration was increased, xylitol production decreased but ethanol production increased. The inhibitory effect of ethanol, a major by-product, on xylitol production was also studied. As the ethanol concentration added increased, xylitol production decreased. When cells were inoculated in a xylose medium after removing ethanol, xylitol production was not inhibited. This results suggested that the inhibition of xylitol production resulted from ethanol which was formed by adding arabinose. It was also interesting that total products(xylitol and ethanol) yield was constant regardless of the arabinose concentration. This result suggested that the total amount of products such as xylitol and ethanol from xylose was constant regardless of the arabinose concentration and arabinose shifted the carbon flow from xylitol to ethanol.

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The Effects of Intracellular Monocarboxylates on the ATP-sensitive Potassium Channels in Rabbit Ventricular Myocytes

  • Kim, Na-Ri;Han, Jin;Kim, Eui-Yong;Ho, Won-Kyung;Earm, Yung E.
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권5호
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    • pp.581-589
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    • 1998
  • A regulating mechanism of the ATP-sensitive potassium channels $(K_{ATP}\;channels)$ is yet to fully explained. This study was carried out to investigate the effects of intracellular application of monocarboxylates (acetate, formate, lactate, and pyruvate) on $K_{ATP}$ channels in isolated rabbit ventricular myocytes. Single channel currents of $K_{ATP}$ channels were recorded using the excised inside-out or permeabilized attached (open-cell) patch-clamp technique at room temperature. Intracellular application of acetate, formate and pyruvate led to an inhibition of channel activity, whereas intracellular application of lactate increased channel activity. These effects were reversible upon washout. Analysis of single channel kinetics showed that monocarboxylates did not affect open-time constant and close-time constant. These results suggest that monocarboxylates participate in modulating $K_{ATP}$ channels activity in cardiac cells and that modulation of $K_{ATP}$ channels activity may resolve the discrepancy between the low $K_i$ in excised membrane patches and high levels of intracellular ATP concentration during myocardial ischemia or hypoxia.

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