• Title/Summary/Keyword: Inhibition constant

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The Kinetic Investigation of D-Hydroxyisovalerate Dehydrogenase from Fusarium sambucinum

  • Lee, Chan;Goerisch, Helmut;Zocher, Rainer
    • BMB Reports
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    • v.33 no.3
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    • pp.228-233
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    • 2000
  • The steady-state investigation of the mechanism of Dhydroxyisovalerate dehydrogenase was performed in order to understand this type of kinetic patterns. The initial velocity was measured with various amounts of both substrates, NADPH and 2-ketoisovalerate. Double reciprocal plots gave patterns that conversed on or near the abscissa. Binding studies indicated that NADPH bound first to the enzyme. The product $NADP^+$ was found to be a competitive inhibitor with respect to NADPH at a constant concentration of 2-ketoisovalerate. However, it showed noncompetitive inhibition against 2-ketoisovalerate at a fixed amount of NADPH. Another product, D-hydroxyisovalerate, was a non-competitive inhibitor versus NADPH and 2-ketoisovalerate at constant levels of 2-ketoisovalerate and NADPH, respectively. These results were comparable with an ordered bi-bi mechanism, in which NADPH bound first to the enzyme, followed by the binding of 2- ketoisovalerate. $NADP^+$ is the last product to be released. The ordered reaction manner of D-hydroxyisovalerate dehydrogenase from 2-ketoisovalerate to D-hydroxyisovalerate allows the accurate regulation of valine metabolism and it may lead to the regulation of total biosynthesis of enniatins in the Fusarium species.

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Singlet Oxygen Quenching by Deoxygadusol and Related Mycosporine-Like Amino Acids from Phytoplankton Prorocentrum micans

  • Suh, Hwa-Jin;Lee, Hyun-Woo;Jung. Jin
    • Journal of Photoscience
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    • v.11 no.32
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    • pp.77-81
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    • 2004
  • Deoxygadusol (DO) and structurally related mycosporine-like amino acids, i.e. mycosporine glycine (MO) and mycosporine taurine (MT), were isolated from phytoplankton Prorocentrum micans and studied for the reactivity toward singlet oxygen. These water-soluble compounds with a cyclohexenone chromophore were all shown to be highly effective in quenching singlet oxygen ($^1$ $O_2$), with the efficiencies being significantly larger compared with histidine, a well-known $^1$ $O_2$ quencher. The $^1$ $O_2$ reaction rate constant ( $k_{Q}$) of DG was determined to be 5.4 ${\times}$ 10$^{7}$ $M^{-1}$ $s^{-1}$ by a steady state method based on competitive inhibition of rubrene oxidation. The feasibility of this method was confirmed by estimating the $k_{Q}$ values for MG and two other quenchers, furfuryl alcohol and 1,4-diazabicyclo [2,2,2]octane, and comparing with those values determined by the time-resolved $^1$ $O_2$ decay method in the previous work.ork.

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Production of Poly-$\beta$-hydroxybutyrate from Methanol by Fed-batch Cultivation of methylobacterium sp. GL-10 (Methylobacterium sp. GL-10의 유가식 배양에 의한 Methanol로 부터 Poly-$\beta$-hydroxybutyrate의 생산)

  • 이호재;이용현
    • KSBB Journal
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    • v.6 no.1
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    • pp.35-43
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    • 1991
  • The production of poly-$\beta$-hydroxybutyrate(PHB) from methanol by batch and fed-batch cultivations of Methylobacterium sp. GL-10 was studied. PHB accumulation was stimulated by the nutrients deficiency including, NH4+, SO42-, and K+. The nitrogen deficiency was the most critical factor for PHB accumulation. In batch cultivation, the maximum cell concentration and PHB content were 1.86g/l and 0.62g/l, respectively, with 1.0%(v/v) of methanol and 0.5g/1 of ammonium sulfate. The mass doubling time of Methylobacterum sp. GL-10 was in the range of 4-5 hrs. The cell growth and PHB accumulation were severely inhibited at the methanol concentration over than 2% (v/v). To overcome methanol Inhibition, constant feeding and intermittent feedillg fed-batch cultivations were adopted, using C/N molar ratio as a control factor. In constant feeding fed-batch process, cell concentration was increased up to 2.67g/1, and PHB yield was enhanced from 0.33 of batch culture to 0.53. The relatively low cell concentration was caused by methanol accumulated in culture broth at late growth phase. To prevent methanol accumulation and to maximize PHB production, DO-state intermittent fed-batch cultivation was attempted. The cell and PHB concentration was reached up to 4.55g/1 and 1.80g/1, respectively. It was possible to maintain methanol concentration low and also to feed nutrient of desired C/N molar ratio.

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Effect of Modified Starches on Caking Inhibition in Ramen Soup

  • Wee, Hye-Won;Choi, Young-Jin;Chung, Myong-Soo
    • Food Science and Biotechnology
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    • v.16 no.4
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    • pp.646-649
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    • 2007
  • The effect of the addition of 2 kinds of chemically modified starches (the anti-caking agents; tapioca starch and com starch) on caking of ramen soup was observed using a low-resolution proton-pulsed nuclear magnetic resonance (NMR) technique. After storing ramen soup samples with diverse compositions of modified starch at 20-40% relative humidity for 4 weeks, changes in the spin-spin relaxation time constant ($T_2$) were measured as a function of temperature. $T_2-Temperature$ curves for ramen soup containing modified starches showed that the caking initiation temperature (glass transition temperature) was increased by $5^{\circ}C$ following the addition of only 0.5% modified cornstarch. The results indicate that the modified com starch used in this study would be an effective anti-caking agent for ramen soup, thus prolonging the shelf life of the product.

High Temperature Creep Behavior in Al-Mg(Zn)-Fe Alloys

  • Bae, Chang-Hwan;Lee, Ju-Hee;Han, Chang-Suk
    • Korean Journal of Materials Research
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    • v.20 no.1
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    • pp.37-41
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    • 2010
  • Creep tests were conducted under a condition of constant stress on two aluminum-based alloys containing particles: Al-5% Mg-0.25% Fe and Al-5% Zn-0.22% Fe. The role of grain boundary sliding was examined in the plane of the surface using a square grid printed on the surface by carbon deposition and perpendicular to the surface using two-beam interferometry. Estimates of the contribution of grain boundary sliding to the total strain, $\varepsilon_{gbs}/\varepsilon_t$ reveal two trends; (i) the sliding contribution is consistently higher in the Al-Mg-Fe alloy, and (ii) the sliding contribution is essentially independent of strain in the Al-Mg-Fe alloy, but it shows a significant decrease with increasing strain in the Al-Zn-Fe alloy. Sliding is inhibited by the presence of particles and its contributions to the total strain are low. This inhibition is attributed to the interaction between the grain boundary dislocations responsible for sliding and particles in the boundaries.

Pharmacokinetic Changes of Tolbutamide After Oral Administration to Rabbits with Alloxan-Induced Diabetes Mellitus (알록산으로 유도된 당뇨병 가토에 톨부타마이드 경구투여시 약물동태변화)

  • Choi, Byung-Chul;Lee, Jin-Hwan;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
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    • v.30 no.2
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    • pp.107-112
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    • 2000
  • The changes in pharmacokinetic parameters of tolbutamide, such as the area under the plasma concentration-time curve from time zero to time infinity (AUC) and elimination rate constant (Kel) were evaluated after oral administration of the drug to rabbits with acute and chronic alloxan-induced diabetes mellitus (AIDRs). After oral administration, the plasma concentrations of tolbutamide were significantly higher between 9 and 12 hr in chronic AIDRs compared with these in control rabbits. Therefore, the AUC was significantly greater in chronic AIDRs $(3,490{\pm}649\;versus\;5,020{\pm}1,030{\mu}gml{\cdot}hr)$. This could be due to inhibition of tolbutamide metabolism by liver in AIDRs since tolbutamide is essentially completely metabolized in liver. Impaired liver and kidney function in AIDRs were based on blood chemistry and tissue microscopy. The absorption rate constant and Kel were significantly slower in chronic AIDRs compared with those in control rabbits.

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Toxic action of N-dimethylphosphinothioyl carbofuran by oxidative activation process (산화적 활성화 과정을 통한 N-dimethoxyphosphinothioyl carbofuran의 독성발현)

  • Yang, Kyew-Wan;Lee, Seog-Jong;Kim, Song-Mun;Han, Dae-Sung;Hur, Jang-Hyun
    • The Korean Journal of Pesticide Science
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    • v.2 no.2
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    • pp.10-15
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    • 1998
  • The bimolecular inhibition rate constants of carbofuran and N-dimethylphosphinothioyl carbofuran(PSC) to acetylcholinesterase(AChE) were $7.7{\times}10^{5}\;M^{-1}{\cdot}min^{-1}$ and $1.2{\times}10^{3}\;M^{-1}{\cdot}min^{-1}$, respectively. These results showed that PSC required a bioactivation process for its toxic action because it didn't inhibit the target enzyme effectively. The potency of PSC as an inhibitor of AChE increased when PSC and AChE were incubated with microsomes fortified with NADPH compared with microsome alone. Piperonyl butoxide(PBO) addition to these coupled systems greatly reduced the inhibition of the target enzyme by blocking the bioactivation process. In vivo inhibition study of mouse brain AChE, $I_{50}$ value for AChE was 28 mg/kg for PSC and the value increased to 57 mg/kg when PBO was pretreated. This result showed that cytochrome $P_{450}$ would also play a role in the bioactivation process of PSC in vivo. And conversioin of carbofuran from PSC was 55 % in a chemical oxidation system using meta-chloroperoxybenzoic acid. The oxidative activation of PSC to carbofuran was shown to be essential for showing its toxicological action and cytochrome $P_{450}$ was identified as an important enzyme which participated in this process.

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Quantitative Structure Activity Relationship (QSAR) Analyses on the Farnesyl Protein Transferase Inhibition Activity of Hetero Ring Substituted Chalcone Derivatives by the Hansch and Free-Wilson Method (Hansch와 Free-Wilson 방법에 의한 헤테로 고리 치환 chalcone 유도체들의 farnesyl protein transferase 저해활성에 대한 정량적 구조 활성 관계(QSAR) 의 분석)

  • Yu, Seong-Jae;Myung, Pyung-Keun;Kwon, Byung-Mok;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.43 no.2
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    • pp.95-99
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    • 2000
  • A series of hetero ring (X) substitued chalcone derivatives with farnesyl protein transferase (FPTase) inhibition activities $(pI_{50})$ values determined in vitro is analyzed by modified Free-Wilson (F-W) and Hansch method for quantitative structure activity relationship (QSARs). On the basis of F-W analysis on the FPTase inhibitory activity of a training set of the compounds, none of the (X)-substituents were not contribute the activity. But the net charge of ${\alpha}$ carbon atom is contribute the activity than that of ${\beta}$ carbon atom. And the relative orders of the (Y)-substituents on the activity are ortho>meta>para-substituents. According to Hansch approach, the activities would depend largely on the optimal, $(R_{opt.}=-0.35)$ resonance effect with ortho substituted $(I_o>0)$ electron donating group (R<0) and STERIMOL parameter, $B_1$ constant. The inhibition activity between hetro ring substituents have been a proportioned with each others and none substituent(H), 45 showed the highest FPTase inhibition $(pI_{50}=4.30)$ activity.

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Inhibition of acetylcholinesterase activity by impurities in technical grades and purified flupyrazofos (Flupyrazofos 원제 및 정제품의 불순물 조성과 Acetylcholinesterase에 대한 저해 비교)

  • You, Kyoung-Youl;Cho, Boo-Yeon;Park, Dong-Sik;Hur, Jang-Hyun
    • The Korean Journal of Pesticide Science
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    • v.9 no.1
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    • pp.97-101
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    • 2005
  • Flupyrazofos (O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothioate) is an organophosphorus insecticide with a pyrazole moiety which is newly developed and commercialized by SUNGBO chemical company and Korean Research Institute of Chemical Technology for effectively control against diamond back moth. This study was conducted to determine the composition and quantity of impurities in technical 1 (94.5%), technical 2 (97.6%) and purified (99.2%) flupyrazofos using GLC/MSD. Bimolecular inhibition rate constant($k_i$) with acethylcholinesterase (in vitro) and $I_{50}$ with mouse brain acetylcholinesterase (in vivo) were measured for comparing inhibitory patterns of two technicals and purified flupyrazofos. Impurities of flupyrazofos were identified as O,O,O-triethylthio-phosphoric acid (TEA), 1-phenyl-3-trifluoromethyl-5-ethoxy pyrazole(PTMEP), O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphoric acid ester(flupyrazofos oxen), O,S-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothionate (S-ethyl flupyrazofos). In in vitro, technical 1 showed the fastest inhibition on AChE activity among them. And technical 1 and 2 showed 40% higher in vivo inhibition against mouse brian AChE than purified flupyrazofos did. These results could be caused by the impurities such as flupyrazofos oxen and S-methyl flupyrazofos contained in technical grades of flupyrazofos.

Effect of environmental and nutritional conditions on $H_2$ production from glucose by the chemoheterotropic facultative bacterium, Citrobacter sp. Y19

  • Oh, You-Kwan;Seol, Eun-Hee;Lee, Young-Kyun;Park, Sung-Hoon
    • 한국생물공학회:학술대회논문집
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    • 2001.11a
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    • pp.598-601
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    • 2001
  • Citrobacter sp. Y19 was studied for $H_2$ production from glucose in batch culture. Important conditions studied include phosphate concentration, temperature, glucose concentration, and gas-phase replacement. Optimal $H_2$ production was observed at 140 - 180 mM of phosphate and $36^{\circ}C$. When glucose concentration increased from 0.1 to 5% (w/v), $H_2$ production increased up to 2% and remained constant thereafter. Intermittent purging of the reaction bottle with Ar gas stimulated the $H_2$ production by alleviating the inhibition by $H_2$. The maximum productivity was observed to be 113.2 ml $H_2$/h-1.

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