• Archives of Pharmacal Research
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• v.19 no.4
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• pp.312-316
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• 1996

A series of N-Cbz${alpha}$-aminosucinimides (1), combining common moieties of various anticonvulsants such as N-CO-C-N and cyclic imide in a single molecule, were synthesized from the corresponding (R)- and (S)-N-Cbz-aspartic acid (2). And their in vivo anticonvulsant evaluations in MES and PTZ test were investigated. And also the rotorod test for neurotoxicity was investigated. All the tested compounds (1), except 1c and 1f, showed significant anticonvulsant activities in both MES and PTZ test. And the most active compound among them in MES test was (R)-N-Cbz-${alpha}$-amino-N-methylsuccinimide (1b) $(ED_50/=52.5 mg/kg)$ and (S)-N-Cbz-aminosuccinimide((1d) was most active in PTZ test $(ED_50/=78.1 mg/kg)$. And the $TD_50$ values of the tested compounds were above 117.5 mg/kg. These pharmacological data were comparable to those of currently available anticonvulsants. And also we found that the pharmacological effects were dependent on their N-substituted alkyl chains and their stereochemistry.

• Bulletin of the Korean Chemical Society
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• v.24 no.5
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• pp.605-609
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• 2003

The lower-order lithium organocyanocuprate compound, (THF)₃Li(NC)Cu($C_6$H₃-2,6-Mes₂) (1), and the bulky terphenyl Grignard reagent, Br(THF)₂Mg($C_6$H₃-2,6-Trip₂) (2), have been synthesized and structurally characterized both in the solid state by single crystal x-ray crystallography and in solution by multi-nuclear NMR and IR spectroscopy. The compound (1) was isolated as a monomeric contact ion-pair in which the C (organic ipso)-Cu-CN-Li atoms are coordinated linearly. The lithium has a tetrahedral geometry as a result of solvation by three THF molecules. The compound (1) is the first example of fully characterized monomeric lower order lithium organocyanocuprate. The bulky Grignard reagent (2) was also isolated as a monomer in which the magnesium, solvated by two THF molecules, has a distorted tetrahedral geometry. The crystals of (1) possess triclinic symmetry with the space group $P{\={1}}$, Z = 2, with a = 12.456(3) Å, b = 12.508(3) Å, c = 13.904(3) Å, α = 99.81°, β = 103.72(3)°, and γ = 119.44(3)°. The crystals (2) have a monoclinic symmetry of space group $P2_{1/C}$, Z = 4, with a = 13.071(3) Å, b = 14.967(3) Å, c = 22.070(4) Å, and β = 98.95(3)°.

• Journal of Microbiology and Biotechnology
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• v.27 no.2
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• pp.242-250
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• 2017

Anti-photoaging effects of standardized Siegesbeckia glabrescens extract (SGE) and its major active compound kirenol were investigated using Hs68 human dermal fibroblasts and hairless mice, respectively. UVB-irradiated hairless mice that received oral SGE (600 mg/kg/day) showed reduced wrinkle formation and skinfold thickness compared with the UVB-irradiated control. Furthermore, SGE treatment increased the mRNA levels of collagen synthesis genes (COL1A1, COL3A1, COL4A1, and COL7A1) and activated antioxidant enzyme (catalase), while suppressing matrix metalloproteinase (MMP-2, -3, -9, and -13) expression. In Hs68 fibroblasts, kirenol also significantly suppressed MMP expression while increasing the expression of COL1A1, COL3A1, and COL7A1. Collectively, our data demonstrate that both SGE and kirenol attenuated UVB-induced photoaging in hairless mice and fibroblasts through inhibition of the mitogen-activated protein kinases and nuclear factor kappa B pathways, suggesting that SGE has potential to serve as a natural anti-photoaging nutraceutical.

• Journal of Microbiology and Biotechnology
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• v.16 no.6
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• pp.870-879
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• 2006

The present study describes the formation of succinic acid by a nonvirulent, highly osmotolerant Klebsiella pneumoniae strain SAP (succinic acid producer), its profile of metabolites, and enzymes of the succinate production pathway. The strain produced succinate along with other metabolites such as lactate, acetate, and ethanol under aerobic as well as anaerobic growth conditions. The yield of succinate was higher in the presence of $MgCO_3$ under $N_2$ atmosphere as compared with that under $CO_2$ atmosphere. Analysis of intracellular metabolites showed the presence of a smaller PEP pool than that of pyruvate. Oxaloacetate, citrate, and $\alpha$-ketoglutarate pools were considerably larger than those of isocitrate and fumarate. In order to understand the synthesis of succinate, the enzymes involved in end-product formation were studied. Levels of phosphoenolpyruvate carboxykinase, fumarate reductase, pyruvate kinase, and acetate kinase were higher under anaerobic growth conditions. Based on the profiles of the metabolites and enzymes, it was concluded that the synthesis of succinate took place via oxaloacetate, malate, and fumarate in the strain under anaerobic growth conditions. The strain SAP showed potential for the bioconversion of fumarate to succinate under $N_2$ atmosphere in the presence of $MgCO_3$. At an initial fumarate concentration of 10 g/l, 7.1 g/l fumarate was converted to 7 g/l succinate with a molar conversion efficiency of 97.3%. The conversion efficiency and succinate yield were increased in the presence of glucose. Cells grown on fumarate contained an 18-fold higher fumarate reductase activity as compared with the activity obtained when grown on glucose.

• The Bulletin of The Korean Astronomical Society
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• v.37 no.1
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• pp.31.2-31.2
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• 2012

We present the Yonsei Evolutionary Population Synthesis (YEPS) models for spectroscopic and photometric evolutions of simple and composite stellar populations. The models are based on the most up-to-date Yonsei-Yale stellar evolutionary tracks and BaSel 3.1 flux libraries, and provide integrated spectroscopic quantities of Lick/IDS system including high-order Balmer absorption-lines. Special care has been taken to incorporate the systematic variation of horizontal branch (HB) morphology as functions of metallicity, age, alpha-element mixture, and helium abundance of simple stellar populations. Our models for normal-helium stellar populations indicate that the realistic modeling of HB and alpha-element brings about 5 Gyr and 0.1 dex differences in age and metallicity estimations, respectively, compared to those without these effects. The HB effect does not depend on the specific choice of stellar libraries and alpha-element enhancements, and this effect is non-negligible even in the metal sensitive absorption indices, such as Mg2 and Mg b. Comparison of the models to observations reveals that the HB and alpha-element effects are critical in understanding otherwise inexplicable phenomena found in globular cluster systems in the Milky Way and nearby galaxies, including the observed bimodality of the line strengths of globular clusters in massive galaxies. In addition, we found that helium-enhanced stellar populations, which are the major sources of extreme HB stars, bring about increased FUV, NUV fluxes, and thus the model colors of those filters become extremely blue. Age dating based on the YEPS model with normal-helium stellar populations reveals that the evidence for 'downsizing' of elliptical galaxies is found not only in the local field but also in Coma cluster, and that the mean age of elliptical galaxies in Coma cluster is about 1.4 Gyr younger than the mean age of those in the local field. We also find that our models with helium-enhanced subpopulations can naturally reproduce the strong UV-upturns observed in giant elliptical galaxies assuming an age similar to that of old GCs in the Milky Way.

• Korean Journal of Pharmacognosy
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• v.36 no.4 s.143
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• pp.273-277
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• 2005

In mammalian melanocytes, melanin synthesis is controlled by tyrosinase, the key enzyme in the pigment synthesis. In this study, to develop a new whitening agent, we have investigated the antioxidant and the inhibitory effect of Artemisia anomala extract on tyrosinase activity and melanigenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of butanol fraction from A. anomala was higher than that of arbutin ($97.5{\pm}0.5%$ at the concentration of 2 mg/ml). The butanol fraction was shown scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and superoxide anion radicals in a dose dependent manner. The highest inhibitory activity of melanogenesis was also butanol fraction ($25.0{\pm}3%$ at the concentration of $200\;{\mu}g/ml$). From these results, we suggest that the A. anomala extract might be used to be a potential agent for skin whitening.

• The Korean Journal of Pharmacology
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• v.20 no.1 s.34
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• pp.41-46
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• 1984

Cadmium (Cd) was administered by a series of weekly intraperitoneal injections at dose of 2mg/kg in rabbits and rats. The levels of malondialdehyde (MDA) and thromboxane $B^2(TXB_2)$ in platelet-rich plasma from Cd-poisoned animals were significantly higher than those of the control group. Furthermore, the inhibition of 6-keto-prostaglandin $F_{1{\alpha}}$, production in Cd-treated aorta ring was inversely related to the enhancement of platelet aggregation. These results suggest that Cd not only inhibits prostacyclin synthesis in the arterial endothelium, but also stimulates the platelet aggregation by enhancing thromboxane AZ production. These findings are assumed to support the evidence of an effect of Cd toxicity on the vascular wall and platelet function in raising arteriall pressure.

• Korean Journal of Materials Research
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• v.25 no.3
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• pp.144-148
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• 2015

Cubic mesocrystal $CeO_2$ was synthesized via a hydrothermal method with glutamic acid ($C_5H_9NO_4$) as a template. The XRD pattern of a calcined sample shows the face-centered cubic fluorite structure of ceria. Transmission electron microscopy (TEM) and the selected-area electron diffraction (SAED) pattern revealed that the submicron cubic mesocrystals were composed of many small crystals attached to each other with the same orientation. The UV-visible adsorption spectrum exhibited the red-shift phenomenon of mesocrystal $CeO_2$ compared to commercial $CeO_2$ particles; thus, the prepared materials show tremendous potential to degrade organic dyes under visible light illumination. With a concentration of a rhodamine B solution of 20 mg/L and a catalyst amount of 0.1 g/L, the reaction showed higher photocatalytic performance following irradiation with a xenon lamp (${\geq}380nm$). The decoloring rate can exceed 100% after 300 min.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.205-213
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• 1998

The efficacy of DA-6034, a new flavonoid derivative, was investigated in comparison with sulfasalazine in a trinitrobenzene sulfonic acid (TNBS)-induced rat colitis. Under light anaesthesia with ether, rats were subjected to intracolonic administration of 30mg TNBS in 50% ethanol (0.5ml) and were then sacrificed at 7 or 21 days after colitis induction. The TNBS control group (the saline treated colitic rat) exhibited ulceration and inflammation of the distal colon with formation of granuloma and pathologic connections. Moreover, an increase in colonic myeloperoxidase (MPO) activity (investigated as an index of leukocyte adhesion and accumulation) and an elevated colonic leukotriene $B_4$ ($LTB_4$) level were observed. The colitic rats received DA6034 (0.3-30mg/kg) or sulfasalazine (50-100mg/kg), prednisolone (0.3-3mg/kg) after the induction of colitis until they were sacrificed. Oral treatment with DA-6034 resulted in significant reductions of macroscopic colonic damage, colonic inflammation. DA6034 had a more potent effect than sulfasalazine and prednisolone on macroscopic colonic damage, while it has similar effect with prednisolone on the reduction of colonic $LTB_4$ synthesis and MPO activity. This study show, therefore, that DA-6034 is effective m attenuating the colonic lesion in an TNBS-induced colitis model. Furthermore, the results suggest that the effect of DA-6034 is partially related to its action on $LTB_4$ synthesis and MPO inhibition.

• Journal of the Korean Ceramic Society
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• v.48 no.4
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• pp.303-306
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• 2011

[ $V_2O_5$ ]doped Karrooite pigments were synthesized by the solid state method to get stabilized brown pigment in oxidation and reduction atmosphere. Optimum substitution condition and limited dopant with $V_2O_5$ for Karrooite pigment was investigated. With calcination at $1250^{\circ}C{\sim}1400^{\circ}C$, compositions were designed varying $V_2O_5$ molar ratio by increasing 0.02mole to the formula $Mg_1-xTi_2-xM_{2x}O_5$(x = 0.01~0.09 mole). Synthesized pigments were analyzed by XRD, Raman spectroscopy and UV-vis. When $V_2O_5$ was doped from 0.01 to 0.05 mole, single phase of Karrooite was observed at temperature $1300^{\circ}C$ and soaking time 4h by Raman spectroscopy. However, it was found that excess $VO_2$ peak appeared with 0.07 and 0.09 mole of $V_2O_5$ doped to $MgTi_2O_5$. This result indicated that the maximum limit of solid solution is 0.05 mole $V_2O_5$. Karrooite pigments were applied as a ceramic pigment to achieve brown colors in lime magnesia glaze and lime barium graze at both of oxidation and reduction atmosphere. CIE color coordinates are $L^*$ = 40.34, $a^*$ = 9.94, $b^*$ = 21.40 in lime magnesia glaze.