• Title/Summary/Keyword: Kinetic study

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Effect of ${\gamma}$-mangostin through the inhibition of 5-hydroxytryptamine$_{2A}$ receptors in 5-fluoro-${\alpha}$-methyltryptamine-induced head-twitch responses of mice

  • Nattaya Chairungsrie;Furukawa, Ken-Ichi;Takeshi Tadano;Kensuke Kisara;Yasushi Ohizumi
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.170-170
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    • 1998
  • In order to discover new types of 5-hydroxytryptamine antagonists, we have devoted our attention to investigating naturally occurring compounds having anti-5HT activity in vitro. Recently, ${\gamma}$-mangostin [1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-bytenyl)-9H-xanthen-9-one] from the fruit hull of Garcinia mangostana Linn has been shown to be a selective antagonist for 5-hydroxytryptamine$_{2A}$ receptors in smooth muscle and platelets. It is of interesting that y-mangostin which does not have a nitrogen atom, possesses marked 5-$HT_{2A}$ receptor blocking activity. The present study was undertaken to investigate the effects of ${\gamma}$-mangostin on central 5-HT receptors by using animal behavioural models. Intracerebronventricular injection of ${\gamma}$-mangostin (10-40n mol/mouse) inhibited 5-fluoro-${\alpha}$-methyltryptamin (5-FMT) (45 mg kg$^{-1}$, i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (5-HT-uptake inhibitor). Neither the 5-FMT- nor the 8-hydroxy-2-( di-n-propylamino )tetralin (5-HT$_{1A}$-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by ${\gamma}$-mangostin. The locomotor activity stimulated by 5-FMT through the activation of at-adrenoceptors did not alter in the presence of ${\gamma}$-mangostin. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. ${\gamma}$-Mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation and the binding of [$^3H$]-spiperone, a specific 5-$HT_{2A}$ receptor antagonist, to mouse brain membranes. Kinetic analysis of the [$^H3$]-spiperone binding revealed that ${\gamma}$-mangostin increased the $_{d}$ value without affecting the $B_{max}$ value, indicating the mode of the competitive nature of the inhibition by ${\gamma}$-mangostin. These results suggest that ${\gamma}$-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-$HT_{2A}$ receptors not by blocking the release of 5-HT from the central neurone. ${\gamma}$-Mangostin is a promising 5-$HT_{2A}$ receptors antagonist in the central nervous system.m.

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Investigation of the processing characteristics of soybean sprouts after germination of HaePum during a long storage period with different temperature and humidity (장기 저장 중 저장 온도와 습도에 따른 해품 콩의 콩나물 가공적성 연구)

  • Lee, Yun Ju;Yoon, Won Byong
    • Journal of Applied Biological Chemistry
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    • v.63 no.1
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    • pp.1-8
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    • 2020
  • This study investigated the processing characteristics of soybean (HaePum) sprouts based on temperature (5, 15 and room temperature), period (0, 6 and 12 mon) and relative humidity (20, 40, 60, and 80%) during storage. The initial germination rate of soybean sprouts was 76.02±6.32%, which significantly reduced to 57.18±8.51%, and 0% as the storage temperature of soybean increased for a period of 12 mon. The germination rate of soybean sprouts with 30 ℃ and 80% RH decreased after 4 mon of storage to 4.94%. The yellowness of cotyledon of soybean sprouts was not significantly changed during the 12 mon period of storage at 5 ℃, whereas, soybean sprouts stored at 15 ℃ and room temperature demonstrated decreased yellowness. However, the stress of cotyledon decreased with an increase in both storage temperature and time, and the hardness of hypocotyl decreased with an increase of storage time. The stress of cotyledon affected by high temperature (30 ℃) and humidity (80%) during 4 mon was reduced to 44.39±9.38 g/㎟. The asparagine content of soybean sprouts showed a similar result with the germination rate due to the amount of hypocotyl. Therefore, lower temperatures and shorter storage times are suitable for soybean sprout processing. The first order kinetic model and Arrhenius equation (activation energy =29.56 kJ/mol) were able to predict the yield of sprout at various storage temperatures and periods.

3-Dimensional Gait analysis and the relationship between lower limb alignment and knee adduction moment in elderly healthy women (3차원적 동작 분석기를 이용한 건강한 여자 노인의 하지 정렬 상태와 슬관절 내전 모멘트의 상관 관계에 관한 연구)

  • Cho, You-Mi;Lee, Wan-Hee
    • Journal of Korean Physical Therapy Science
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    • v.10 no.1
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    • pp.90-101
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    • 2003
  • Gait analysis can provide a better understanding of how the alignment of the lower limb and foot can contribute to force observed at the knee. Anatomic and mechanical factors that affect loading in the knee pint can contribute to pathologic change seen at the knee in degenerative pint disease and should be considered in treatment plan. The purpose of this study is to present the gait analysis data and to determine whether there is any relationships between alignment of the lower limb, foot progression angle and knee pint moments in elderly healthy women with 3-dimensional motion analyzer. The results were as follows; 1. Cadence showed 114.8 steps/min, gait speed showed 1.05 m/s, time per a stride showed 1.06 sec, time per a step showed 0.53 sec, single-supporting phase was 0.41 sec, double-supporting phase was 0.24 sec, stride length was 1.04 m, Step length was 0.56 m. 2. According to the parameters of kinematics, the maximal knee flexion angle through swing phase showed left $46.82^{\circ}$, right $40.19^{\circ}$ and the maximal knee extension angle showed left $-1.32^{\circ}$, right $2.01^{\circ}$. knee varus showed left $26.90^{\circ}$, right $30.93^{\circ}$. 3. Moment, one of kinetic parameters of knee pint the maximal flexion moment showed left 0.363. Nm/kg, right 0.464 Nm/kg and maximal extension moment showed left 0.389 Nm/kg, right 0.463 Nm/kg. The maximal. adduction moment showed left 0.332 Nm/kg, right 0.379 Nm/kg and the maximal internal rotatory moment showed left 0.13 Nm/kg, right 0.140 Nm/kg. 4. On sagittal plane, the maximal power of knee joint showed left 0.571 J/kg, right 0.629 J/kg. On coronal plane, the maximal power of knee joint showed left 0.11 J/kg, right 0.12 J/kg. On transverse plane, the maximal power of knee joint showed left 0.058 J/kg, right 0.072 J/kg. 5. The subject who had varus alignment of the lower extremity had statistically higher in knee adduction moment in mid stance phase. 6. The subject who had large foot progression angle had statistically lower in knee adduction moment in late stance phase. A relationship was observed between the alignment of the lower extremity and the adduction moment of the knee joint during stance phase. Hence, we need some research to figure, out the change of adduction moment according to the sort of knee joint osteoarthritis and the normal geriatrics as well. And we also require more effective, specific therapeutic program by making use of those background of researches.

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Soil Detachment by Single and Multiple Waterdrops (우적(雨滴)에 의한 토양(土壤) 침식(侵蝕))

  • Miller, W.P.;Kim, Kye-Hoon
    • Applied Biological Chemistry
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    • v.38 no.2
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    • pp.151-156
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    • 1995
  • Single-drop splash/detachment studies and multiple-drop splash/detachment experiments were carried out to measure detachment by single and multiple drops. A raindrop tower 7.0 m in height was used to study soil splash by single drop raindrop impact over time on repacked soil samples in containers 76.2 mm in diameter. The waterdrop diameter and kinetic energy were 4.1 mm and $1.22{\times}10^{-3}$ J $drop^{-1}$, respectively. The samples consisted of five agricultural topsoils sieved to <2 mm, varying from sandy loam to clay loam in texture. The average weight of splashed soil particles after 75 drops did not show any significant difference between the five soils. The average weight of particles splashed by the first 15 drops showed that the sandy Pelham soil splashed to a greater degree than the others, and was therefore more detachable (p=0.05) than the other soils. The average weight of particles splashed by the last 15 drops also showed that the Pelham soil was the most detachable, with Cecil, Appling, Dyke, and Worsham soils being progressively less detachable. The effect of multiple drops on detachment was studied under a nozzle-type rainfall simulator at 74.9 mm $h^{-1}$ intensity for 85 min using the same soils as the single drop experiments. The total soil splash value for 85 min on Appling, Cecil, Dyke, Pelham, and Worsham soils were 6121, 6206, 4183, 5160, and 3247 g $m^{-2}$, respectively. There were no obvious relationships between soil loss measured from the different experiments.

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Study on Adsorption Features of Arsenic onto Lepidocrocite (레피도크로사이트(lepidocrocite) 표면의 비소 흡착 특성 규명)

  • Lee, Woo-Chun;Jeong, Hyeon-Su;Kim, Ju-Yong;Kim, Soon-Oh
    • Economic and Environmental Geology
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    • v.42 no.2
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    • pp.95-105
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    • 2009
  • Systematic studies are performed for arsenic adsorption on synthesized lepidocrocite. The synthesized lepidocrocite with high surface area of $94.8\;g/m^2$ has shown that the point of zero charge(PZC) is 6.57 determined by potentiometric titration, suggestive of high capacity of arsenic removal. Results show that arsenite[As(III)] uptake by synthesized lepidocrocite is greater than that of arsenate[As(V)] at pH $2{\sim}12$, indicating that the lepidocrocite has high affinity toward arsenite rather than arsenate. Adsorption of arsenate decreases with increasing pH from 2 to 12, whereas arsenite sorption increases until pH 8.0, and then decreases dramatically with increasing pH, suggesting that changes in surface charge of the lepidocrocite as a function of pH playa important role in aresinc uptake by the lepidocrocite. Upon kinetic experiments, our results demonstrate that both arsenite and arsenate sorption on the lepidocrocite increases rapidly for the first 4 h followed by little changes during the duration of the experiment, showing that adsorption plays a key role in aresenic uptake by the lepidocrocite. Our results also show that power function and elovich models are the best fit for the adsorption kinetics of arsenite and aesenate on the lepidocrocite.

Pyrolytic Reaction Pathway of Dichloromethane in Excess Hydrogen (과잉수소 반응분위기에서 Dichloromethane 열분해 반응경로에 관한 연구)

  • Won, Yang-Soo
    • Applied Chemistry for Engineering
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    • v.17 no.6
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    • pp.638-643
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    • 2006
  • Pyrolytic reaction study of dichloromethane ($CH_{2}Cl_{2}$) in excess hydrogen was performed to investigate pyrolytic reaction pathways at a pressure of 1 atm with residence times of 0.3~2.0 sec in the temperature range of $525{\sim}900^{\circ}C$. A constant feed molar ratio $CH_{2}Cl_{2}$:$H_{2}$ of 4:96 was maintained through the experiment. Reagent loss and product formation were monitored by using an on-line gas chromatograph, where batch samples were analyzed by GC/MS. Complete destruction(99%) of the parent reagent was observed at temperature near $780^{\circ}C$ with residence time over 1 sec. Major products observed were $CH_{3}Cl$, $CH_{4}$, $C_{2}H_{4}$, $C_{2}H_{6}$, and HCl. Minor products included $CHClCCl_{2}$, CHClCHCl, $CH_{2}CHCl$, and $C_{2}H_{2}$. The pyrolytic reaction pathways to describe the important features of intermediate product distributions and reagent loss, based upon thermodynamic and kinetic principles, were suggested. The results of this work provided a better understanding of pyrolytic decomposition processes which occur during the pyrolysis of $CH_{2}Cl_{2}$ and similar chlorinated methanes.

Addition Reaction of Glycidyl Methacrylate with Carbon Dioxide Using Quaternary Ammonium Salts as Catalys (4급 암모늄염 촉매에 의한 Glycidyl Methacrylate와 이산화탄소의 부가반응)

  • Yang, J.G.;Moon, J.Y.;Jung, S.M.;Park, D.W.;Lee, J.K.
    • Applied Chemistry for Engineering
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    • v.7 no.6
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    • pp.1156-1163
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    • 1996
  • This study is related to the investigation of the characteristics of quaternary ammonium salt catalyst on the addition reaction of carbon dioxide and glycidyl methacrylate(GMA) to form(2-oxo-1,3-dioxolane-4-yl)methacrylate(DOMA). Among the salts tested, the ones with higher alkyl chain length and with more nucleophilic counter anion showed a higher catalytic activity. Mixed catalysts of NaI and 18-crown-6 showed a good yield of DOMA, but when they are used alone, they showed no catalytic activity. The DOMA monomer was obtained in low polar solvents, while poly(DOMA) could be directly synthesized in aprotic dipolar solvents. Kinetic studies carried out by measuring $CO_2$ pressure in a high pressure batch reactor showed that the reaction rate was first order to the concentration of GMA and $CO_2$ respectively. The rate constant(k) was 0.56L/mol hr and Henry's constant(H') of $CO_2$ in diglyme at $80^{\circ}C$ was $6.5{\times}10^{-4}mol/L{\cdot}kPa$.

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Characteristics of Glucose Oxidase Reaction of Onion Juice (양파 착즙액과 포도당 산화효소의 반응 특성)

  • Choi, Bong-Young;Lee, Eun-Mi;Kim, Young-Ran;Kim, Hyun-Jong;Chung, Bong-Woo
    • Korean Journal of Food Science and Technology
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    • v.35 no.3
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    • pp.417-422
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    • 2003
  • The onions are considered to be a favorable functional source of beverage because they contain much sugar and various nutrients, and they are juicy vegetable. Recently, consumers have a new trend to take functional foods with health benefits. To meet this need, this study was the basic research to establish a manufacturing process of functional onion beverage by glucose oxidase. Glucose oxidase catalyzes reaction of glucose oxidation and makes generation of gluconic acid. Kinetics of the reaction was also investigated, and maximum glucose consumption rate $(V_{max})$ of $26.1{\times}10^{-2}\;g/L{\cdot}min$ and $K_m$ of 5.84 g/L were obtained. Optimum conditions were obtained when the glucose oxidase catalyzed reaction was carried out at temperature of $25^{\circ}C$, agitation rate of 450 rpm and aeration rate of 4 vvm in a 2.5 L jar fermentor. Finally, the enzyme reactor was 10-times scaled up and a similar glucose oxidation performance was achieved in the scaled-up reactor.

Quality Characteristics of Baked Rice Cake Added with Maltitol (말티톨 첨가 구운떡의 품질 특성)

  • Kim, Hee-Jung;Yoo, Seon-Mi;Han, Hye-Min;Park, Bo-Ram;Han, Gui-Jung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.7
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    • pp.1068-1074
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    • 2014
  • This study investigated the quality characteristics of baked rice cake added with maltitol syrup. The hardness, adhesiveness, cohesiveness, gumminess, and chewiness of baked rice cake significantly decreased (P<0.05) according to the level of added maltitol syrup. Hunter's color values of baked rice cake did not differ significantly according to the level of added maltitol syrup. Sensory evaluation indicated that appearance, moistness, chewiness, hardness, and overall acceptance of baked rice cake prepared with added maltitol syrup were improved compared to those of baked control rice cake. Hunter's color values and texture properties of baked rice cake added with 10% maltitol syrup were compared with those of baked control rice cake during storage at room temperature for 3 days. Hunter's color L values of baked rice cake decreased during storage, whereas a and b values increased. The rate of hardness increase in baked rice cake with maltitol syrup was lower than that in baked control rice cake during storage. The Avrami exponents (n) of baked control rice cake and baked rice cake added with 10% maltitol were 2.418 and 2.098, respectively. The time constants (1/k) of the former and latter were 43.860 and 60.976, respectively. Overall, addition of 10% maltitol syrup improved the texture, sensory properties, and retarding retrogradation of baked rice cake.

Quinacrin Induces Cytochrome c-dependent Apoptotic Signaling in Human Cervical Carcinoma Cells

  • Fasanmade, Adedigbo A.;Owuor, Edward D.;Ee, Rachel P.L.;Qato, Dima;Heller, Mark;Kong, Ah Ng Tony
    • Archives of Pharmacal Research
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    • v.24 no.2
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    • pp.126-135
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    • 2001
  • Quinacrine (QU), a phospholipase-A2 (PLA-2) inhibitor has been used clinically as a chemotherapeutic adjuvant. To understand the mechanisms leading to its chemotherapeutic effect, we have investigated QU-induced apoptotic signaling pathways in human cervical squamous carcinoma HeLa cells. In this study, we found that QU induced cytochrome c-dependent apoptotic signaling. The release of pro-apoptotic cytochrome c was QU concentration- and time-dependent, and preceded activation of caspase-9 and -3. Flow cytometric FACScan analysis using fluorescence intensities of $DiOC_6$/ demonstrated that QU-induced cytochrome c release was independent of mitochondrial permeability transition (MPT), since the concentrations of QU that induced cytochrome c release did not alter mitochondrial membrane potential (${\blacktriangle}{\Psi}_m$). Moreover, kinetic analysis of caspase activities showed that cytochrome c release led to the activation of caspase-9 and downstream death effector caspase-3, Caspase-3 inhibitor (Ac-DEVD-CHO) partially blocked QU-induced apoptosis, suggesting the importance of caspase-3 in this apoptotic signaling mechanism. Supplementation with arachidonic acid (AA) sustained caspase-3 activation induced by QU. Using inhibitors against cellular arachidonate metabolism of lipooxygenase (Nordihydroxyguaiaretic Acid, NDGA) and cyclooxygenase (5,8,11,14-Eicosatetraynoic Acid, ETYA) demonstrated that QU-induced apoptotic signaling may be dependent on its role as a PLA-2 inhibitor. Interestingly, NDCA attenuated QU-induced cytochrome c release, caspase activity as well as apoptotic cell death. The blockade of cytochrome c release by NDCA was much more effective than that attained with cyclosporin A (CsA), a MPT inhibitor. ETYA was not effective in blocking cytochrome c release, except under very high concentrations. Caspase inhibitor z-VAD blocked the release of cytochrome c suggesting that this signaling event is caspase dependent, and caspase-8 activation may be upstream of the mitochondrial events. In summary, we report that QU induced cytochrome c-dependent apoptotic signaling cascade, which may be dependent on its role as a PLA-2 inhibitor. This apoptotic mechanism induced by QU may contribute to its known chemotherapeutic effects.

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