• Title/Summary/Keyword: ${\beta}$-ME

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INFLUENCE OF 17-$\alpha$-ESTRADIOL ON CATECHOLAMINE SECRETION FROM THE PERFUSED RAT ADRENAL GLAND

  • Lim, Dong-Yoon;Lee, Jong-Jin-;Ko, Suk-Tai
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.297-297
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    • 1994
  • It has been known that adrenal corticosteroids influence the expression of adrenomedullary catecholamine-synthetizing enzymes and also suppress the emission of axonal-like processes in cultured chromaffin cells. In the present study, it was attempted ta investigate the effect of 17${\alpha}$-estradiol on catecholamine(CA) secretion evoked by acetylcholine(ACh), DMPP, McN-A-343, excess K$\^$+/ and Bay-K-8644 from the isolated perfused rat adrenal gland. The perfusion of 17${\alpha}$-estradiol (10$\^$-6/ 10$\^$-4/M) me an adrenal vein for 20min produced relatively dose-dependent inhibition in CA secretion evoked by ACh (5.5 ${\times}$ 10$\^$-3/M), DMPP (10$\^$-4/M for 2min), McN-A-343 (10$\^$-4/M for 4min) and Bay-K-8644 (10$\^$-5/M for 4min), while did not affect the CA secretory effect of high K$\^$+/(5.6 x 10$\^$-2/M). Also, in the presence of 17${\beta}$-estradiol, CA secretion of ACh, DMPP and McN-A-343 without any effect on excess K$\^$+/-evoked CA secretion. However, in adrenal glands preloaded with 17${\alpha}$-estradiol (10$\^$-5/M) plus tamoxifen (10$\^$-5/M), which is known to be a selective antagonist of estrogen receptors (for 20min), CA secretory responses evoked by ACh, DMPP and McN-A-343 were considerably recovered as compared to that of 17${\alpha}$-estradiol only, but excess K$\^$+/-induced CA secretion was not affected.

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Kinetic Study on Aminolysis of Phenyl 2-Pyridyl Carbonate in Acetonitrile: Effect of Intramolecular H-bonding Interaction on Reactivity and Reaction Mechanism

  • Song, Ji-Hyun;Lee, Jae-In;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.35 no.7
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    • pp.2081-2085
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    • 2014
  • Second-order rate constants ($k_N$) have been measured spectrophotometrically for the reactions of phenyl 2- pyridyl carbonate (6) with a series of cyclic secondary amines in MeCN at $25.0{\pm}0.1^{\circ}C$. The Br${\o}$nsted-type plot for the reaction of 6 is linear with ${\beta}_{nuc}$ = 0.54, which is typical for reactions reported previously to proceed through a concerted mechanism. Substrate 6 is over $10^3$ times more reactive than 2-pyridyl benzoate (5), although the reactions of 6 and 5 proceed through the same mechanism. A combination of steric hindrance, inductive effect and resonance contribution is responsible for the kinetic results. The reactions of 6 and 5 proceed through a cyclic transition state (TS) in which H-bonding interactions increase the nucleofugality of the leaving group (i.e., 2-pyridiniumoxide). The enhanced nucleofugality forces the reactions of 6 and 5 to proceed through a concerted mechanism. In contrast, the corresponding reaction of 4-nitrophenyl 2-pyridyl carbonate (7) proceeds through a stepwise mechanism with quantitative liberation of 4-nitrophenoxide ion as the leaving group, indicating that replacement of the 4-nitrophenoxy group in 7 by the PhO group in 6 changes the reaction mechanism (i.e., from a stepwise mechanism to a concerted pathway) as well as the leaving group (i.e., from 4-nitrophenoxide to 2-pyridiniumoxide). The strong electron-withdrawing ability of the 4-nitrophenoxy group in 7 inhibits formation of a H-bonded cyclic TS. The presence or absence of a H-bonded cyclic TS governs the reaction mechanism (i.e., a concerted or stepwise mechanism) as well as the leaving group (i.e., 2-pyridiniumoxide or 4-nitrophenoxide).

Studies of Valve Lifer for Automotive Heavy Duty Diesel Engine by Ceramic Materials II. Development of SiC Valve Lifter by Injection Molding Method (Ceramic 재질을 이용한 자동차용 대형 디젤엔진 Valve Lifter 연구 II. 사출성형에 의한 탄화규소질 Valve Lifter 개발)

  • 윤호욱;한인섭;임연수;정윤중
    • Journal of the Korean Ceramic Society
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    • v.35 no.2
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    • pp.172-179
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    • 1998
  • Valve lifter namely tappet is supported by lifter hole which is located upper side of camshaft in cylinder block transforms rotatic mvement of camshaft into linear movement and helps to open and shut the en-gine valve as an engine parts. The face of valve lifter which is continuously contacting with camshaft brings about abnormal wears such as unfair wear and early wear because it is severely loaded in the valve train system. These wears act as a defect like over-clearance and cause imperfect combustion of fuel during the valve lifting in the combustion chamber. Consequently this imperfect combustion makes the engine out-put decrease and has cause on air pollution. To prevent these wears therefore The valve lifter cast in me-tal developed into SiC ceramics valve lifter which has an excellence in wear and impact resistance As a results the optimum process conditions like injection condition mixture ratio and debonding process could be established. After sintering fine-sinered dual microstructure in which prior ${\alpha}$-SiC matches well with new SiC(${\beta}$-SiC) produced by reaction among the ${\alpha}$-SiC carbon and silicon was obtained. Based on the study it is verified that mechanical properties of SiC valve lifter are excellent in Vickers hardness 1100-1200 bending strength (300-350 Pa) fracture toughness(1.5-1.7 Mpa$.$m1/2) Through engine dynamo test-ing SiC valve lifter and metal valve lifter are examined and compared into abnormal phenomena such as early fracture unfair and early wear. It is hoped that this research will serve as an important springboard for the future study of heavy duty diesel engine parts developed by ceramics which has a good wear resis-tance relaibility and lightability.

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Plasma Phosphoproteome and Differential Plasma Phosphoproteins with Opisthorchis Viverrini-Related Cholangiocarcinoma

  • Kotawong, Kanawut;Thitapakorn, Veerachai;Roytrakul, Sittiruk;Phaonakrop, Narumon;Viyanant, Vithoon;Na-Bangchang, Kesara
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.3
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    • pp.1011-1018
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    • 2015
  • This study was conducted to investigate the plasma phosphoproteome and differential plasma phosphoproteins in cases of of Opisthorchis viverrini (OV)-related cholangiocarcinoma (CCA). Plasma phosphoproteomes from CCA patients (10) and non-CCA subjects (5 each for healthy subjects and OV infection) were investigated using gel-based and solution-based LC-MS/MS. Phosphoproteins in plasma samples were enriched and analyzed by LC-MS/MS. STRAP, PANTHER, iPath, and MeV programs were applied for the identification of their functions, signaling and metabolic pathways; and for the discrimination of potential biomarkers in CCA patients and non-CCA subjects, respectively. A total of 90 and 60 plasma phosphoproteins were identified by gel-based and solution-based LC-MS/MS, respectively. Most of the phosphoproteins were cytosol proteins which play roles in several cellular processes, signaling pathways, and metabolic pathways (STRAP, PANTHER, and iPath analysis). The absence of serine/arginine repetitive matrix protein 3 (A6NNA2), tubulin tyrosine ligase-like family, member 6, and biorientation of chromosomes in cell division protein 1-like (Q8NFC6) in plasma phosphoprotein were identified as potential biomarkers for the differentiation of healthy subjects from patients with CCA and OV infection. To differentiate CCA from OV infection, the absence of both serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit beta isoform and coiled-coil domain-containing protein 126 precursor (Q96EE4) were then applied. A combination of 5 phosphoproteins may new alternative choices for CCA diagnosis.

Chemical Constituents of the Root of Dystaenia takeshimana and Their Anti-Inflammatory Activity

  • Kim, Ju-Sun;Kim, Jin-Cheul;Shim, Sang-Hee;Lee, Eun-Ju;Jin, Wen-Yi;Bae, Ki-Hwan;Son, Kun-Ho;Kim, Hyun-Pyo;Kang, Sam-Sik;Chang, Hyeun-Wook
    • Archives of Pharmacal Research
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    • v.29 no.8
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    • pp.617-623
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    • 2006
  • In our ongoing search for bioactive compounds originating from the endemic species in Korea, we found that the hexane and EtOAc fractions of the MeOH extract from the root of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5- lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2\;(PGD_2)$ and leukotriene $C_4\;(LTC_4)$ in mouse bone marrow-derived mast cells. By activity-guided fractionation, five coumarins, viz. psoralen (2), xanthotoxin (3), scopoletin (4), umbelliferone (5), and (+)-marmesin (6), together with ${\beta}-sitosterol$ (1), were isolated from the hexane fraction, and two phenethyl alcohol derivatives, viz. 2-methoxy-2-(4'-hydroxyphenyl)ethanol (7) and 2-hydroxy-2-(4'-hydroxyphenyl)ethanol (8), three flavonoids, viz. apigenin (9), luteolin (10), and cynaroside (11), as well as daucosterol (12) were isolated from the EtOAc fraction using silica gel column chromatography. In addition, D-mannitol (13) was isolated from the BuOH fraction by recrystallization. Two of the coumarins, scopoletin (4) and (+)- marmesin (6), the two phenethyl alcohol derivatives (7, 8) and the three flavonoids (9-11) were isolated for the first time from this plant. Among the compounds isolated from this plant, the five coumarins as well as the three flavonoids showed COX-2/5-LOX dual inhibitory activity. These results suggest that the anti-inflammatory activity of D. takeshimana might in part occur via the inhibition of the generation of eicosanoids.

Flagellin-Stimulated Production of Interferon-β Promotes Anti-Flagellin IgG2c and IgA Responses

  • Kang, Wondae;Park, Areum;Huh, Ji-Won;You, Gihoon;Jung, Da-Jung;Song, Manki;Lee, Heung Kyu;Kim, You-Me
    • Molecules and Cells
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    • v.43 no.3
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    • pp.251-263
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    • 2020
  • Flagellin, a major structural protein of the flagellum found in all motile bacteria, activates the TLR5- or NLRC4 inflammasome-dependent signaling pathway to induce innate immune responses. Flagellin can also serve as a specific antigen for the adaptive immune system and stimulate anti-flagellin antibody responses. Failure to recognize commensal-derived flagellin in TLR5-deficient mice leads to the reduction in anti-flagellin IgA antibodies at steady state and causes microbial dysbiosis and mucosal barrier breach by flagellated bacteria to promote chronic intestinal inflammation. Despite the important role of anti-flagellin antibodies in maintaining the intestinal homeostasis, regulatory mechanisms underlying the flagellin-specific antibody responses are not well understood. In this study, we show that flagellin induces interferon-β (IFN-β) production and subsequently activates type I IFN receptor signaling in a TLR5- and MyD88-dependent manner in vitro and in vivo. Internalization of TLR5 from the plasma membrane to the acidic environment of endolysosomes was required for the production of IFN-β, but not for other pro-inflammatory cytokines. In addition, we found that anti-flagellin IgG2c and IgA responses were severely impaired in interferon-alpha receptor 1 (IFNAR1)-deficient mice, suggesting that IFN-β produced by the flagellin stimulation regulates anti-flagellin antibody class switching. Our findings shed a new light on the regulation of flagellin-mediated immune activation and may help find new strategies to promote the intestinal health and develop mucosal vaccines.

Photoluminescence Studies of ZnO Nanorods Grown by Vapor Phase Transport (기상이동법으로 성장한 산화아연 나노막대의 포토루미네슨스 분석)

  • Kim, Soaram;Cho, Min Young;Nam, Giwoong;Kim, Min Su;Kim, Do Yeob;Yim, Kwang Gug;Leem, Jae-Young
    • Korean Journal of Metals and Materials
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    • v.49 no.10
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    • pp.818-822
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    • 2011
  • ZnO nanorods were grown on Au-coated Si substrates by vapor phase transport (VPT) at the growth temperature of $600^{\circ}C$ using a mixture of zinc oxide and graphite powders as source material. Au thin films with the thickness of 5 nm were deposited by ion sputtering. Temperature-dependent photoluminescence (PL) was carried out to investigate the optical properties of the ZnO nanorods. Five peaks at 3.363, 3.327, 3.296, 3.228, and 3.143 eV, corresponding to the free exciton (FX), neutral donor bound exciton ($D^{\circ}X$), first order longitudinal optical phonon replica of free exciton (FX-1LO), FX-2LO, and FX-3LO emissions, were obtained at low-temperature (10 K). The intensity of these peaks decreased and their position was red shifted with the increase in the temperature. The FX emission peak energy of the ZnO nanorods exhibited an anomalous behavior (red-blue-red shift) with the increase in temperature. This is also known as an "S-shaped" emission shift. The thermal activation energy for the exciton with increasing temperature in the ZnO nanorods is found to be about 26.6 meV; the values of Varshni's empirical equation fitting parameters are = $5{\times}10^{-4}eV/K$, ${\beta}=350K$, and $E_g(0)=3.364eV$.

Stability of $^{188}Re$ Labeled Antibody for Radioimmunotherapy and the Effect of Stabilizing Agents (방사면역치료용 $^{188}Re$ 표지 항체의 안정성과 안정제의 효과)

  • Chang, Young-Soo;Kim, Bo-Kwang;Jeong, Jae-Min;Chung, June-Key;Lee, Seung-Jin;Lee, Dong-Soo;Lee, Myung-Chul
    • The Korean Journal of Nuclear Medicine
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    • v.36 no.3
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    • pp.195-202
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    • 2002
  • Purpose: For clinical application of beta-emitter labeled antibody, high specific activity is imporiant. Carrier-free $^{188}Re$ from $^{188}W/^{188}Re$ generator is an ideal radionuclide for this purpose. However, low stability of $^{188}Re$ labeled antibody, especially in high specific activity, due to radiolytic decomposition by high energy (2.1 MeV) beta ray was problem. We studied the stability of $^{188}Re$ labeled antibody, and stabilizing effect of several stabilizers. Materials and Methods: Pre-reduced monoclonal antibody (CEA79.4) was labeled with $^{188}Re$ by incubating with generator-eluted $^{188}Re-perrhenate$ in the presence of stannous tartrate for 2 hr at room temperature. Radiochemical purity of each preparation was determined by chromatography. Human serum albumin was added to the labeled antibodies (2%). Stability of $^{188}Re-CEA79.4$ was investigated in the presence of ascorbic acid, ethanol, of Tween 80 as stabilizing agents. Results: Labeling efficiencies were $88{\pm}4%\;(n=12)$. Specific activities of $1.25{\sim}4.77MBq/{\mu}g$ were obtained. If stored after purging with $N_2$, all the preparations were stable for 10 hr. However, stability decreased in the presence of air. Perrhenate and $^{188}Re-tartrate$ was major impurity in declined preparation. colloid-formation was not a significant problem in all cases. Addition of ascorbic acid stabilized the labeled antibodies either under $N_2$ or under air by reducing the formation of perrhenate. Conclusion: High specific activity $^{188}Re$ labeled antibody is unstable, especially, in the presence of oxygen. Addition of ascorbic acid increased the stability.

Inhibition of Adipocyte Differentiation through G1 Arrest by Extract of Sophora tonkinensis Gapnep in 3T3-L1 Preadipocytes (산두근 추출물의 세포주기 정지를 통한 3T3-L1 지방전구세포의 분화 억제)

  • Jeong, Hyun-Young;Hyun, Sook-Kyung;Choi, Yung-Hyun;Kim, Byung-Woo;Kwon, Hyun-Ju
    • Journal of Life Science
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    • v.21 no.9
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    • pp.1346-1353
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    • 2011
  • Sophora tonkinensis Gapnep has been used as a traditional herbal medicine in oriental regions since ancient times. In this study, the effect and mechanism of the MeOH extract of Sophora tonkinensis Gapnep (STME) on adipocite differentiation and adipogenesis in 3T3-L1 preadipocites were investigated. Treatment with STME in the concentration range of 0-200 ${\mu}g$/ml significantly inhibited the differentiation of 3T3-L1 preadipocites in a dose-dependent manner, as determined by a decrease in intracellular lipid droplets and lipid contents measured by Oil Red O staining. In association with the inhibitory effect of lipid accumulation, the expressions of the proteins concerned with adipogenesis in 3T3-L1 preadipocites were also investigated. Treatment with STME reduced the expressions of peroxisome proliferator-activated receptor ${\gamma}$ (PPAR${\gamma}$), cytidine-cytidine-adenosine-adenosine-thymine (CCAAT)/enhancer-binding proteins ${\alpha}$ and ${\beta}$ (C/EBP${\alpha}$ and C/EBP${\beta}$) and sterol regulatory element binding protein (SREBP), which are adipocyte specific markers. In flow cytometry analysis, the inhibitory effect of differentiation was caused by G1 arrest and following mitotic clonal expansion cease. Therefore, we also investigated the alteration of G1 phase arrest-related proteins. As a result, the expression of p21 protein was significantly increased, while the expressions of Cdk2, E2F-1 and phospho-Rb were reduced in a dose-dependent manner in STME treated 3T3-L1 cells. According to these results, STME might inhibit differentiation through G1 arrest in 3T3-L1 preadipocytes adipogenesis, and further studies, which are in progress, have to be completed to identify the active compounds.

Evaluation for Rock Cleavage Using Distribution of Microcrack Lengths and Spacings (3) (미세균열의 길이 및 간격 분포를 이용한 결의 평가(3))

  • Park, Deok-Won;Park, Eui-Seob;Jung, Yong-Bok;Lee, Tae-Jong;Song, Yoon-Ho
    • The Journal of the Petrological Society of Korea
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    • v.28 no.1
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    • pp.1-13
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    • 2019
  • The characteristics of the rock cleavage of Jurassic Geochang granite were analysed using the parameters from the length and spacing-cumulative frequency diagrams. The evaluation for three planes and three rock cleavages was performed using the 25 parameters such as (1~2) slope angle(${\alpha}^{\circ}$and ${\beta}^{\circ}$), (3) intersection angle(${\alpha}-{\beta}^{\circ}$), (4) exponent difference(${\lambda}_S-{\lambda}_L$), (5~12) length of line(oa, ob, ol, os, ss', ll' and sl') and (13~15) length ratio(ol/os, ss'/ll' and ll'/sl'), (16) mean length((ss'+ll')/2), (17~23) area (${\Delta}oaa^{\prime}$, ${\Delta}obb^{\prime}$, ${\Delta}obb^{\prime}$, ${\Delta}oaa_a^{\prime}$, ${\Delta}obb_a^{\prime}$, ${\Delta}ll^{\prime}s^{\prime}$, ${\Delta}ss^{\prime}l^{\prime}$ and ⏢$ll^{\prime}ss^{\prime}$) and (24~25) area difference(${\Delta}obb^{\prime}-{\Delta}oaa^{\prime}$ and ${\Delta}obb_a^{\prime}-{\Delta}oaa_a^{\prime}$). Firstly, the values of the 11 parameters(group I: No. 1, 3~4, 7, 9~10, 13, 15~16, 20 and 25), the 3 parameters(group II: No. 5, 8 and 17) and the 2 parameters(group III: No. 12 and 22) are in orders of H(hardway) < G(grain) < R(rift), R < G < H and G < H < R, respectively. On the contrary, the values of parameters belonging to the above three groups show reverse orders for three planes. Secondly, the generalized chart for three planes and three rock cleavages were made. From the related chart, the distribution types formed by the two diagrams related to lengths and spacings were derived. The diagrams related to spacings show upward curvature in the chart of rift plane(G1 & H1, R') and hardway(H1 & H2, H). On the contrary, the diagrams related to lengths show downward curvature. These two diagrams take the form of a convex lens in the upper section. Besides, the two diagrams cross each other in the lower section. The overall shape formed by the above two diagrams between three planes($H^{\prime}{\rightarrow}G^{\prime}{\rightarrow}R^{\prime}$) and three rock cleavages($R{\rightarrow}G{\rightarrow}H$) display in reverse order. Lastly, these types of correlation analysis is useful for discriminating three quarrying planes.