• 제목/요약/키워드: Inhibition kinetics

검색결과 154건 처리시간 0.033초

Application of hybrid material, modified sericite and pine needle extract, for blue-green algae removal in the lake

  • Choi, Hee-Jeong
    • Environmental Engineering Research
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    • 제23권4호
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    • pp.364-373
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    • 2018
  • The present study assessed the efficient removal of nutrients and Chlorophyll-a (Chl-a) by using methyl esterified sericite (MES) and pine needle extracts (PNE), a low cost and abundant green hybrid material from nature. For this purpose, the optimal conditions were investigated, such as the pH, temperature, MES and PNE ratio, and MES-PNE dose. In addition, a Microcystis aeruginosa control using MES-PNE was also analyzed with various inhibition models. The removal of the nutrient and Chl-a onto MES-PNE was optimized for over 95% removal as follows: 2-2.5 for the MES-PNE ratio, 7-8 pH and a $22-25^{\circ}C$ temperature. In this respect, approximately 1.52-2.20 g/L of MES-PNE was required to remove each 1 g of dry weight/L of Chl-a. Total phosphorus (TP) has a greater influence on the increase in Chl-a than total nitrogen (TN) according to the correlation between TN, TP and Chl-a. Moreover, the Luong model was the best model for fitting the biodegradation kinetics data from Chl-a on MES-PNE from lake water. The novel hybrid material MES-PNE was very effective at removing TN, TP and Chl-a from the lake and can be applied in the field.

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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Blockade of Kv1.5 channels by the antidepressant drug sertraline

  • Lee, Hyang Mi;Hahn, Sang June;Choi, Bok Hee
    • The Korean Journal of Physiology and Pharmacology
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    • 제20권2호
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    • pp.193-200
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    • 2016
  • Sertraline, a selective serotonin reuptake inhibitor (SSRI), has been reported to lead to cardiac toxicity even at therapeutic doses including sudden cardiac death and ventricular arrhythmia. And in a SSRI-independent manner, sertraline has been known to inhibit various voltage-dependent channels, which play an important role in regulation of cardiovascular system. In the present study, we investigated the action of sertraline on Kv1.5, which is one of cardiac ion channels. The effect of sertraline on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Sertraline reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an $IC_{50}$ value and a Hill coefficient of $0.71{\mu}M$ and 1.29, respectively. Sertraline accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -20 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to +10 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance ${\delta}$ of 0.16. Sertraline slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of sertraline, were superimposed. Inhibition of Kv1.5 by sertraline was use-dependent. The present results suggest that sertraline acts on Kv1.5 currents as an open-channel blocker.

Blockade of Kv1.5 by paroxetine, an antidepressant drug

  • Lee, Hyang Mi;Hahn, Sang June;Choi, Bok Hee
    • The Korean Journal of Physiology and Pharmacology
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    • 제20권1호
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    • pp.75-82
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    • 2016
  • Paroxetine, a selective serotonin reuptake inhibitor (SSRI), has been reported to have an effect on several ion channels including human ether-a-go-go-related gene in a SSRI-independent manner. These results suggest that paroxetine may cause side effects on cardiac system. In this study, we investigated the effect of paroxetine on Kv1.5, which is one of cardiac ion channels. The action of paroxetine on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Paroxetine reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an $IC_{50}$ value and a Hill coefficient of $4.11{\mu}M$ and 0.98, respectively. Paroxetine accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -30 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to 0 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance ${\delta}$ of 0.32. The binding ($k_{+1}$) and unbinding ($k_{-1}$) rate constants for paroxetine-induced block of Kv1.5 were $4.9{\mu}M^{-1}s^{-1}$ and $16.1s^{-1}$, respectively. The theoretical $K_D$ value derived by $k_{-1}/k_{+1}$ yielded $3.3{\mu}M$. Paroxetine slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of paroxetine, were superimposed. Inhibition of Kv1.5 by paroxetine was use-dependent. The present results suggest that paroxetine acts on Kv1.5 currents as an open-channel blocker.

시규제초제 LGC-40863의 벼와 피에 대한 Acetolactate synthase 저해 활성 (In vitro Acetolactate Synthase Inhibition of LGC-40863 in Rice and Barnyardgrass)

  • 배영태;이재환;구석진
    • 한국잡초학회지
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    • 제17권1호
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    • pp.66-70
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    • 1997
  • (주)LG화학에서 개발중엔 LGC-40863은 벼에 대해 높은 안전성을 보이며 피 등 여러 잡초를 방제하는 신규제초제이다. LGC-40863은 관련 제초제나 식물에서의 효과 발현 증상으로 부터 acetolactate synthase(ALS)를 저해하는 것으로 추정된다. 본 연구에서는 LGC-40863의 ALS에 대한 영향을 알아보기 위하여 벼와 피로부터 추출한 ALS를 사용하여 $I_{50}$값과 효소반응속도를 조사하였다. LGC-40863의 $I_{50}$값은 14(벼), 16mM(피)였고, 대조약제로 사용한 imazapyr와 chlorsulfuron의 $I_{50}$값은 각각 12-15mM, 0.03-0.04mM였으므로 LGC-40863의 $I_{50}$값은 imazapyr와 유사하고 chlorsulfuron에 비해서는 약 400배 정도 높았다. 그리고 세 가지 약재 모두 벼와 피 간의 감수성 차이는 크지 않았다. 효소반응속도 면에서 살펴보면, LGC-40863은 벼와 피 모두 pyruvate에 대해 noncompetitive inhibition을 나타내었으며, chlorsulfuron과 imazapyr는 벼에서 각각 noncompetitive와 uncompetitive inhibition을 하는 것으로 나타났으므로 LGC-40863은 chlorsulfuron과 저해유형이 비슷하였다.

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Symbolic-numeric Estimation of Parameters in Biochemical Models by Quantifier Elimination

  • Orii, Shigeo;Anai, Hirokazu;Horimoto, Katsuhisa
    • 한국생물정보학회:학술대회논문집
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    • 한국생물정보시스템생물학회 2005년도 BIOINFO 2005
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    • pp.272-277
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    • 2005
  • We introduce a new approach to optimize the parameters in biological kinetic models by quantifier elimination (QE), in combination with numerical simulation methods. The optimization method was applied to a model for the inhibition kinetics of HIV proteinase with ten parameters and nine variables, and attained the goodness of fit to 300 points of observed data with the same magnitude as that obtained by the previous optimization methods, remarkably by using only one or two points of data. Furthermore, the utilization of QE demonstrated the feasibility of the present method for elucidating the behavior of the parameters in the analyzed model. The present symbolic-numeric method is therefore a powerful approach to reveal the fundamental mechanisms of kinetic models, in addition to being a computational engine.

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Alcaligenes eutrophus 균주의 성장과 Ploy-${\beta}$-hydroxybutyrate 생합성에 대한 속도론 (Kinetics for the Growth of Alcaligenes eutrophus and the Biosynthesis of Poly-${\beta}$-hydroxybutyrate)

  • 이용우;유영제
    • 한국미생물·생명공학회지
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    • 제19권2호
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    • pp.186-192
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    • 1991
  • It is very important to have a good kinetic model which considers the effects of both ammonium and glucose for the control and optimization of the poly-${\beta}$-hydroxybutyrate (PHB) fermentation. A kinetic model for the growth of Alcaligenes eutrophus and the biosynthesis of PHB under both ammonium and glucose limitation was proposed. Growth rate of residual biomass was expressed as a function of concentrations of residual biomass, glucose and ammonium having glucose inhibition. PHB production rate was expressed as a function of concentrations of residual biomass, glucose, ammonium and PHB content having ammonium and product inhibitions. Novel approaches were made to estimate the parameters in the model equations which considered two limiting substrates. Model parameters were evaluated by graphical and simplex methods. The proposed kinetic model fitted the data very well.

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Tyrosinase Inhibitor from the Flowers of Impatiens balsamina

  • Lim, Young-Hee;Kim, In-Hwan;Seo, Jung-Ju;Kim, Jeong-Keun
    • Journal of Microbiology and Biotechnology
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    • 제16권12호
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    • pp.1977-1983
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    • 2006
  • Kaempferol was isolated and identified from the methanol extract of the flowers of Impatiens balsamina. Kaempferol showed inhibitory activity against mushroom tyrosinase with an $ID_{50}$ of 0.042 mM. Inhibition kinetics, as determined using a Lineweaver-Burk plot, showed kaempferol to be a competitive inhibitor of mushroom tyrosinase with a $K_i$ value of 0.011 mM. The lag phase of tyrosine hydroxylation catalyzed by mushroom tyrosinase clearly increased on increasing the concentration of kaempferol. In addition to its tyrosinase inhibiting activity, kaempferol strongly inhibited melanin production by Streptomyces bikiniensis, in a dose-dependent manner, without inhibiting cell growth. For comparative purposes, the tyrosinase inhibitory activity of kaempferol was also assayed versus quercetin, a positive standard.

Pethidine induced changes in ovarian follicular kinetics and biochemical parameters in albino rats

  • Patil, Somanath Reddy;Patil, Saraswati B;Malashetty, Vijaykumar B
    • Advances in Traditional Medicine
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    • 제6권4호
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    • pp.300-305
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    • 2006
  • Pethidine at the dose level of 0.5 mg and 0.75 mg/100 g body weight administered for 20 days to the cycling albino rats caused decrease in the ovarian weight and its protein content. The ovarian folliculogenesis in treated rats is hampered; as a result the follicles which are at the different stages of growth underwent regression. Therefore, the number of healthy follicles is reduced and atretic follicles increased. The elevated levels of ovarian cholesterol and decreased level of glycogen in the pethidine treated rats indicates the inhibition brought in steroidogenesis, which is dependent on pituitary gonadotrophins.

The Inhibitory Effect of New Hydroxamic Acid Derivatives on Melanogenesis

  • Baek, Heung-Soo;Rho, Ho-Sik;Yoo, Jae-Won;Ahn, Soo-Mi;Lee, Jin-Young;Lee, Jeong-A;Kim, Min-Kee;Kim, Duck-Hee;Chang, Ih-Seop
    • Bulletin of the Korean Chemical Society
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    • 제29권1호
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    • pp.43-46
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    • 2008
  • The aim of present study was to examine the inhibitory effects of hydroxamic acid derivatives on the melanogenesis. We found that hydroxamic acid moiety was important for anti-melanogenic activity. Compounds 1a and 1b strongly inhibited melanin synthesis via deactivation of tyrosinase. Hydroxamic acid has metal ion chelating ability which is similar to that kojic acid, however, anti-tyrosinase mechanism of compounds 1a and 1b was different from that of kojic acid. They showed noncompetitive inhibition kinetics