• Title/Summary/Keyword: Activation Products

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A Study on the Kinetics and Mechanism of the Hydrolysis of 5,6-Dihydro-1,4-thiazine Derivatives (5,6-Dihydro-1,4-thiazine 유도체의 가수분해 메카니즘과 반응속도론적 연구)

  • Lee, Gwang Il;Lee, Seok U;Gwak, Cheon Geun;Jang, Byeong Man;Kim, Yeong Ju;Lee, Gi Chang
    • Journal of the Korean Chemical Society
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    • v.38 no.5
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    • pp.366-371
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    • 1994
  • The kinetics of the hydrolysis of 5,6-dihydro-1,4-thiazine derivatives was investigated by ultraviolet spectrophotometry in $H_2O$ at 25$^{\circ}C$. A rate equation which can be applied over a wide pH range was obtained. The substituent effects on the hydrolysis of 5,6-dihydro-1,4-thiazine derivatives were studied and the rate of hydrolysis was shown to be accelerated by electron donating groups. Final product of the hydrolysis was 2-(N-acetylaminoethylthio)-acetoacetanilide enol from Judging from the results of the rate equation, general base effect, activation parameters and final products, the hydrolysis of 5,6-dihydro-1,4-thiazine derivatives seemed to be initiated by the neutral $H_2O$ molecule which does not dissociate at pH below 10.0, but proceeded by the hydroxide ion at pH above 11.0, and those two reactions occurred competively at pH 10.0∼11.0 range. On the basis of these findings a plausible mechanism for the hydrolysis of 5,6-dihydro-1,4-thiazine derivative was proposed.

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Developmental Immunotoxicity in SD Rat Pups Exposed by Di(n-butyl) Phthalate through Pre and Postnatal (SD Rat에 있어서 출생 전.후에 걸친 Di(n-butyl) Phthalate 노출에 의한 발생면역독성)

  • 엄준호;정승태;이종권;박재현;권태우;김지영;오혜영;김형수
    • Toxicological Research
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    • v.18 no.4
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    • pp.401-409
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    • 2002
  • Phthalate esters have possible effects on the endocrine system. Di-n-butyl phthalate (DBP) is one of the most commonly wed phthalic acid esters (PAEs). It is extensively wed as a plasticizer in elastomers, as a solvent for printing inks and resins, and as a textile lubricating agent. It is also present in the formulations of various cosmetic products. DBP has been identified as a reproductive toxicant in several animal species and also know as a endocrine disruptor. The objective of this study was to investigate the effect of DBP on developmental immune Junction wing rat pups as experimental animals. Timed-bred pregnant SD rats were orally dosed with 0, 250, 500, or 750 mg DBP/kg body weight once a day from gestational day (GD) 5 to 18 and postpartum day (PD) 3 to 18. On PD22, the dams and their pups were euthanized and examined for alteration in parameters associated to immune function. The results showed no significant changes in body weight, thymus weight, thymus and spleen cellularities, the polyclonal activation respones of splenocyte with ConA and LPS, and also the distribution of arterial blood cells and thymocyto subsets in both rat dam and pups. However DBP exposure on rat dam resulted in increases of liver weights of dam and their pups except 750 mg DBP/kg, and body and spleen weights in pups except 750 mg DBP/kg. On the other hands, distribution rates of CD8+ T cells at 500 mg DBP/kg and B cells at 750 mg DBP/kg among splenocyte subsets were significantly increased in rat pups, unlike dams. Reasons of these distribution alterations of CD8+ T cells and B cells in rat pups are under study.

Effect of Job's Tear(Yul-Moo) Extracts on Mouse Spleen and $IL-1{\beta},\;IL-6,\;TNF-{\alpha}$ Cytokine Production by Peritoneal Macrophages (4주 동안의 율무 추출물 투여가 사이토카인 $IL-1{\beta},\;IL-6,\;TNF-{\alpha}$ 생성과 비장세포 증식에 미치는 영향)

  • Ryu Hye-Sook;Kim Hyun-Sook
    • The Korean Journal of Food And Nutrition
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    • v.19 no.2
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    • pp.201-206
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    • 2006
  • Numerous investigators have studied various activities of natural products and have found that they have not only nutritional effects, but also beneficial properties to cure various diseases and to maintain good health. Job's Tear(Yul-Moo) is a grass crop that has long been used in traditional medicine and as a nourishing food. Although its mechanism of action remains unclear, Job's Tear has been reported to exhibit anti-inflammatory, stomachic, anti-allergic, and anti-spastic effects and has been used in China for the treatment of warts, rheumatism, and neuralgia. Previous results in our laboratory demonstrated that the ethanol extract and the water extract of Job's Tear exerted an immune regulatory function on mice cells in vitro. The present study was performed to investigate the ex vivo effect of Job's Tear on immune function. Seven to eight weeks old mice(Balb/c) were fed chow diet ad libitum and water extract of Job's Tear was administered orally every other day for four weeks at two different concentrations(50 and 500mg/kg B.W.). Splenocytes proliferation with mitogen stimulation with Con A and LPS was enhanced at 50 mg/kg B.W. of Job's Tear compared to those of the control group. The results of this ex vivo study showed that proliferation of splenocytes and macrophage activation were seen in the mice orally administrated 50 mg/kg B.W. of Job's Tear water extracts. In conclusion, this study suggests that Job's Tear extracts may enhance immune function by regulating splenocyte proliferation and the cytokine prodution capacity of activated macrophages in mice.

Characterizations and Quantitative Estimation of Alkali-Activated Binder Paste from Microstructures

  • Kar, Arkamitra;Ray, Indrajit;Halabe, Udaya B.;Unnikrishnan, Avinash;Dawson-Andoh, Ben
    • International Journal of Concrete Structures and Materials
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    • v.8 no.3
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    • pp.213-228
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    • 2014
  • Alkali-activated binder (AAB) is recently being considered as a sustainable alternative to portland cement (PC) due to its low carbon dioxide emission and diversion of industrial wastes and by-products such as fly ash and slag from landfills. In order to comprehend the behavior of AAB, detailed knowledge on relations between microstructure and mechanical properties are important. To address the issue, a new approach to characterize hardened pastes of AAB containing fly ash as well as those containing fly ash and slag was adopted using scanning electron microscopy (SEM) and energy dispersive X-ray spectra microanalyses. The volume stoichiometries of the alkali activation reactions were used to estimate the quantities of the sodium aluminosilicate (N-A-S-H) and calcium silicate hydrate (CSH) produced by these reactions. The 3D plots of Si/Al, Na/Al and Ca/Si atom ratios given by the microanalyses were compared with the estimated quantities of CSH(S) to successfully determine the unique chemical compositions of the N-A-S-H and CSH(S) for ten different AAB at three different curing temperatures using a constrained nonlinear least squares optimization formulation by general algebraic modeling system. The results show that the theoretical and experimental quantities of N-A-S-H and CSH(S) were in close agreement with each other. The $R^2$ values were 0.99 for both alkali-activated fly ash and alkali-activated slag binders.

Expression and Biochemical Characterization of the Bacillus thuringiensis Cry4B ${\alpha}1$-${\alpha}5$ Pore-forming Fragment

  • Puntheeranurak, Theeraporn;Leetacheewa, Somphob;Katzenmeier, Gerd;Krittanai, Chartchai;Panyim, Sakol;Angsuthanasombat, Chanan
    • BMB Reports
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    • v.34 no.4
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    • pp.293-298
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    • 2001
  • Tryptic activation of the 130-kDa Bacillus thuringiensis Cry4B $\delta$-endotoxin produced protease-resistant products of ca. 47 kDa and ca. 21 kDa. The 21-kDa fragment was identified as the N-terminal five-helix bundle (${\alpha}1-{\alpha}5$,) which is a potential candidate for membrane insertion and pore formation. In this study, we constructed the recombinant clone over-expressing this putative pore-forming (PPF) fragment as inclusion bodies in Escherichia coli. The partially purified inclusions were composed of a 23-kDa protein, which cross-reacted with Cry4B antibodies, and whose N-terminus was identical to that of the 130-kDa protein. Dissimilar to protoxin inclusions, the PPF inclusions were only soluble when the carbonate buffer, pH 9.0, was supplemented with 6 M urea. After renaturation via a stepwise dialysis, the refolded PPF protein appeared to exist as an oligomer and was structurally stable upon trypsin treatment. Unlike the 130kDa protoxin, the refolded protein was able to release entrapped glucose from liposomes, and showed comparable activity to the full-length activated toxin, although it lacks larvicidal activity These results, therefore, support the notion that the PPF fragment that consists of ${\alpha}1-{\alpha}5$ of the activated Cry4B toxin is involved in membrane pore-formation.

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Obesity and Obese-related Chronic Low-grade Inflammation in Promotion of Colorectal Cancer Development

  • Pietrzyk, Lukasz;Torres, Anna;Maciejewski, Ryszard;Torres, Kamil
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.10
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    • pp.4161-4168
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    • 2015
  • Colorectal cancer (CRC) is a worldwide health problem, being the third most commonly detected cancer in males and the second in females. Rising CRC incidence trends are mainly regarded as a part of the rapid 'Westernization' of life-style and are associated with calorically excessive high-fat/low-fibre diet, consumption of refined products, lack of physical activity, and obesity. Most recent epidemiological and clinical investigations have consistently evidenced a significant relationship between obesity-driven inflammation in particular steps of colorectal cancer development, including initiation, promotion, progression, and metastasis. Inflammation in obesity occurs by several mechanisms. Roles of imbalanced metabolism (MetS), distinct immune cells, cytokines, and other immune mediators have been suggested in the inflammatory processes. Critical mechanisms are accounted to proinflammatory cytokines (e.g. IL-1, IL-6, IL-8) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$). These molecules are secreted by macrophages and are considered as major agents in the transition between acute and chronic inflammation and inflammation-related CRC. The second factor promoting the CRC development in obese individuals is altered adipokine concentrations (leptin and adiponectin). The role of leptin and adiponectin in cancer cell proliferation, invasion, and metastasis is attributable to the activation of several signal transduction pathways (JAK/STAT, mitogen-activated protein kinase (MAPK), phosphatidylinositol 3 kinase (PI3K), mTOR, and 5'AMPK signaling pathways) and multiple dysregulation (COX-2 downregulation, mRNA expression).

Characteristics of Basalt Materials Derived from Recycling Steel Industry Slags (철강산업 슬래그를 이용하여 제조한 바잘트 소재의 특성)

  • Jung, Woo-Gwang;Back, Gu-Seul;Yoon, Mi-Jung;Lee, Jee-Wook
    • Korean Journal of Materials Research
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    • v.27 no.5
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    • pp.281-288
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    • 2017
  • In this study, Fe-Ni slag, converter slag and dephosphorization slag generated from the steel industry, and fly ash or bottom ash from a power plant, were mixed at an appropriate mixing ratio and melted in a melting furnace in a mass-production process for glass ceramics. Then, glass-ceramic products, having a basalt composition with $SiO_2$, $Al_2O_3$, CaO, MgO, and $Fe_2O_3$ components, were fabricated through casting and heat treatment process. Comparison was made of the samples before and after the modification of the process conditions. Glass-ceramic samples before and after the process modification were similar in chemical composition, but $Al_2O_3$ and $Na_2O$ contents were slightly higher in the samples before the modification. Before and after the process modification, it was confirmed that the sample had a melting temperature below $1250^{\circ}C$, and that pyroxene and diopside are the primary phases of the product. The crystallization temperature in the sample after modification was found to be higher than that in the sample before modification. The activation energy for crystallization was evaluated and found to be 467 kJ/mol for the sample before the process modification, and 337 kJ/mol for the sample after the process modification. The degree of crystallinity was evaluated and found to be 82 % before the process change and 87 % after the process change. Mechanical properties such as compressive strength and bending strength were evaluated and found to be excellent for the sample after process modification. In conclusion, the samples after the process modification were evaluated and found to have superior characteristics compared to those before the modification.

Soft corals collected from Jeju Island inhibits the α-MSH-induced melanogenesis in B16F10 cells through activation of ERK

  • Sanjeewa, K. K. Asanka;Park, Young-jin;Fernando, I. P. Shanura;Ann, Yong-Seok;Ko, Chang-Ik;Wang, Lei;Jeon, You-Jin;Lee, WonWoo
    • Fisheries and Aquatic Sciences
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    • v.21 no.9
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    • pp.21.1-21.8
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    • 2018
  • In the present study, we first evaluated the melanin inhibitory effect of four crude 70% ethanol extracts separated from soft corals abundantly growing along the seawaters of Jeju Island, South Korea, including Dendronephthya castanea (DC), Dendronephthya gigantea (DG), Dendronephthya puetteri (DP), and Dendronephthya spinulosa (DS). Among the four ethanol extracts, the ethanol extract of DP (DPE) did not possess any cytotoxic effect on B16F10 cells. However, all other three extracts showed a cytotoxic effect. Also, DPE reduced the melanin content and the cellular tyrosinase activity without cytotoxicity, compared to the ${\alpha}-MSH$-stimulated B16F10 cells. Specifically, DPE downregulated the expression levels of tyrosinase and microphthalmia-associated transcription factor by activating the ERK signaling cascade in ${\alpha}-MSH$-stimulated B16F10 cells. Interestingly, the melanin inhibitory effect of DPE was abolished by the co-treatment of PD98059, an ERK inhibitor. According to these results, we suggest that DPE has whitening capacity with the melanin inhibitory effects by activating ERK signaling and could be used as a potential natural melanin inhibitor for cosmeceutical products.

TNF-induced genes and Proteins

  • 이태호
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.11a
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    • pp.17-20
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    • 1993
  • As a step toward a more complete understanding of the molecular actions of TNF, we prepared a cDNA library from TNF-treated human FS-4 fibroblasts and used differential hybridization to identify cDNA clones corresponding to mRNAs enriched in TNF-treated eells. In Quiescent FS-4 cells n induces an increase in the level of some mRNAs within 20 to 30 min. Some of these immediate-early response mRNAs are elevated only transiently for about 30 to 120 min, e. g., c-fos and c-myc (Lin and Vilcek,1987) or the transcription factor IRF-1 (Fujita et al.1989). Such immediate-early gene products may be important for the activation of other genes, but their transient induction suggests that they are not the actual effector molecules responsible for the phenotypic changes induced by TNF. We chose a 3-h incubation with W because we were seeking cDNAs corresponding to messages that are more stably elevated after TNF treatment. Indeed, the results shown in Figure 8 and 9 indicate that all of the mRNAs corresponding to the eight TSG cDNAs isolated remained significantly elevated after 16h of continuous treatment with TNF, and their kinetics of induction were clearly different from those of the immediate-early response mRNAs such as c-fos, c-myc or IRF-1. Nevertheless, only the induction of TSG-21 (collagenase) and TSG-27 (stromelysin) nNAs was completely inhibited by cycloheximide and the induction of TSG-37 (metallothionein-II) was reduced in the presence of this inhibitor of protein synthesis. Induction of the other five TSG mRNAs by TNF was completelyresistant to cycloheximide, suggest ins that no protein intermediate is needed for the upregulation of these mRNAs.

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Estimation of Radioactive Inventory for a major component of Reactor in Decommissioning (해체시 원자로 주요 구성품에 대한 방사능 재고량 평가)

  • Hak-Soo Kim;Ki-Doo Kang;Kyoung-Doek Kim;Chan-Woo Jeong
    • Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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    • v.2 no.1
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    • pp.69-75
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    • 2004
  • DORT and ORIGEN2 code were used for calculation of neutron flux and inventory in reactor pressure vessel(RPV) of Kori unit-1, To calculate neutron flux using DORT code, the reactor was divided into 94 mesh from the center of core to RPV and from 0 to 45 degree along the azimuth. The cross-sections of main nuclides were recalculated using neutron flux in the RPV region. The results showed that 95% of the total activity in RPV came from the nuclides of $^{55}$ Fe, $^{60}$ Co, $^{59}$ Ni and $^{63}$ Ni. And the total activity with cooling of more than 50 years after decommissioning was no more than 0.2% of at the time of shutdown. Considering the weight of RPV is 210 tons, the initial total activity of RPV reached 5.25${\times}$10$^{6}$ GBq. To verify results of ORIGEN2 calculation, comparison between calculated and measured value at RPV of Kori unit-1 was peformed. The comparison results showed a good agreement.

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