• Journal of the Korean Chemical Society
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• v.54 no.1
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• pp.77-87
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• 2010

Hospital-acquired methicillin-resistant Staphylococcus aureus (MRSA) has been an increasing problem worldwide since the initial reports over 40 years ago. To examine new drug leads with potential antibacterial activities, Various N'-[(-3-substituted-4-oxo-1,3-thiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4a-4.i) and N'-[-(3,4-disubstituted)-1,3-thiazolidin-2ylidene)]-4-hydroxybenzohydrazide from (5.a-5.i) to (10.a-10.i) were synthesized using appropriate synthetic route. The entire test compounds (4.a-4.i) and from (5.a-5.i) to (10.a-10.i) were assayed in vitro against s. aureus strain. The minimum inhibitory concentration (MIC) was determined for test compounds and for reference standards. The test compounds showed significant antibacterial activity against the strains used, when tested in vitro. In general, p-hydroxybenzohydrazide ring and substituted thiazoline ring are essential for antimicrobial activity. Among the compounds tested, compounds 6.f, 7.g, 9.f and 10.f, 10 i were found to be most potent. The test compounds were found nontoxic upto the dose level of 2000 ${\mu}g$/mL. The intact compounds were then subjected for 3D-QSAR studies. 3D-QSAR study based on the principal of alignment of pharmacophoric features by Schrodinger PHASE module. The 3D-QSAR study allowed us to confirm the preferential binding mode of p-hydroxybenzohydrazide inside the active site.

• Asian-Australasian Journal of Animal Sciences
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• v.33 no.6
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• pp.992-1001
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• 2020

Objective: This study was conducted to investigate the effects of hot-melt extruded ZnO nano-particles (HME-ZnO) as an alternative for P-ZnO on growth performance, nutrient digestibility, Zn bioavailability, intestinal microbiota, and intestinal morphology of weanling pigs. Methods: A total of 450 piglets (Landrace×Yorkshire×Duroc) were randomly allotted to five treatments based on initial body weight and sex. The experimental diets were fed in a meal form as phase 1 from d 0 to 14 and phase 2 from d 15 to 28. Treatments were the control diet without ZnO supplementation, the diet containing 2,500 ppm Zn as ZnO, and three diets containing 500, 1,000, or 2,500 ppm Zn as HME-ZnO. Results: The overall result showed a higher (p<0.01) average daily gain in weanling pigs fed ZnO-supplemented diets in comparison to the control diet. There was a decrease (p<0.01) in fecal score in the ZnO-supplemented diets. Dietary supplementation of ZnO improved (p<0.05) crude protein digestibility. The weanling pigs fed the P-ZnO diet had a lower (p<0.01) Zn digestibility in the feces than HME-ZnO supplemented treatments. Weanling pigs fed diets supplemented with ZnO had greater (p<0.05) Lactobacillus spp. populations and lower Clostridium spp. (p<0.05) and Coliforms (p<0.01) populations in the ileum. Weanling pigs fed diets supplemented with increasing concentrations of HME-ZnO linearly decreased Clostridium spp. (p<0.05) and Coliforms (p<0.01) in the ileum. Lower (p<0.05) Clostridium spp. and Coliforms counts in the colon were observed in pigs fed with ZnO-supplemented diets. Weanling pigs fed diets supplemented with ZnO showed a greater (p<0.01) villus height in the duodenum. Conclusion: Dietary supplementation of HME-ZnO and P-ZnO showed a potential to improve the digestibility of protein, intestinal Coliform and Clostridium, villus height in duodenum and ileum. Moreover, HME-ZnO showed a higher Zn digestibility compared with P-ZnO.

• Asian-Australasian Journal of Animal Sciences
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• v.29 no.10
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• pp.1470-1476
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• 2016

Octacosanol, which has prominent physiological activities and functions, has been recognized as a potential growth promoter in animals. A total of 392 1-d-old male Arbor Acres broiler chicks with similar body weight were randomly distributed into four dietary groups of seven replicates with 14 birds each supplemented with 0, 12, 24, or 36 mg octacosanol (extracted from rice bran, purity >92%)/kg feed. The feeding trial lasted for six weeks and was divided into the starter (day 1 to 21) and the grower (day 22 to 42) phases. The results showed that the feed conversion ratio (FCR) was significantly improved in broilers fed a diet containing 24 mg/kg octacosanol compared with those fed the control diet in the overall phase (day 1 to 42, p = 0.042). The average daily gain and FCR both showed linear effects in response to dietary supplementation of octacosanol during the overall phase (p = 0.031 and 0.018, respectively). Broilers fed with 24 or 36 mg/kg octacosanol diet showed a higher eviscerated yield, which increased by 5.88% and 4.26% respectively, than those fed the control diet (p = 0.030). The breast muscle yield of broilers fed with 24 mg/kg octacosanol diet increased significantly by 12.15% compared with those fed the control diet (p = 0.047). Eviscerated and breast muscle yield increased linearly with the increase in dietary octacosanol supplementation (p = 0.013 and 0.021, respectively). Broilers fed with 24 or 36 mg/kg octacosanol diet had a greater (p = 0.021) $pH_{45min}$ value in the breast muscle, which was maintained linearly in response to dietary octacosanol supplementation (p = 0.003). There was a significant decrease (p = 0.007) in drip loss value between the octacosanol-added and the control groups. The drip loss showed linear (p = 0.004) and quadratic (p = 0.041) responses with dietary supplementation of octacosanol. These studies indicate that octacosanol is a potentially effective and safe feed additive which may improve feed efficiency and meat quality, and increase eviscerated and breast muscle yield, in broiler chicks. Dietary supplementation of octacosanol at 24 mg/kg diet is regarded as the recommended dosage in the broilers' diet.

• Proceedings of the Korean Vacuum Society Conference
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• 2015.08a
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• pp.157-157
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• 2015

Recently, the growing interest in organic microelectronic devices including OLEDs has led to an increasing amount of research into their many potential applications in the area of flexible electronic devices based on plastic substrates. However, these organic devices require a gas barrier coating to prevent the permeation of water and oxygen because organic materials are highly susceptible to water and oxygen. In particular, high efficiency OLEDs require an extremely low water vapor transition rate (WVTR) of $1{\times}10^{-6}g/m^2day$. The Key factor in high quality inorganic gas barrier formation for achieving the very low WVTR required ($1{\times}10^{-6}g/m^2day$) is the suppression of defect sites and gas diffusion pathways between grain boundaries. In this study NBAS process was introduced to deposit enhanced film density single gas barrier layer with a low WVTR. Fig. 1. shows a schematic illustration of the NBAS apparatus. The NBAS process was used for the $Al_2O_3$ nano-crystal structure films deposition, as shown in Fig. 1. The NBAS system is based on the conventional RF magnetron sputtering and it has the electron cyclotron resonance (ECR) plasma source and metal reflector. $Ar^+$ ion in the ECR plasma can be accelerated into the plasma sheath between the plasma and metal reflector, which are then neutralized mainly by Auger neutralization. The neutral beam energy is controlled by the metal reflector bias. The controllable neutral beam energy can continuously change crystalline structures from an amorphous phase to nanocrystal phase of various grain sizes. The $Al_2O_3$ films can be high film density by controllable Auger neutral beam energy. we developed $Al_2O_3$ high dense barrier layer using NBAS process. We can verified that NBAS process effect can lead to formation of high density nano-crystal structure barrier layer. As a result, Fig. 2. shows that the NBAS processed $Al_2O_3$ high dense barrier layer shows excellent WVTR property as a under $2{\times}10^{-5}g/m^2day$ in the single barrier layer of 100nm thickness. Therefore, the NBAS processed $Al_2O_3$ high dense barrier layer is very suitable in the high efficiency OLED application.

• Journal of the Korean GEO-environmental Society
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• v.11 no.1
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• pp.45-51
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• 2010

Cadmium (Cd) adsorption by the activated carbon containing hydroxyapatite (HAP) was investigated. Cd adsorption with different HAP mass ranged from 10% to 30%. With more HAP, more Cd was adsorbed. These results suggest that the higher HAP dose causes an increase of the ion exchange potential in HAP sorbent. Kinetics and equilibrium studies were investigated in series of batch adsorption experiments. Langmuir and Freundlich isotherm models were fit to the equilibrium data and Cd adsorption on HAP sorbent were found to follow the Freundlich isotherm model well in the initial adsorbate concentration range. The simple kinetic model, the pseudo first order kinetic model and the pseudo second order kinetic model, were used to investigate the adsorption. The adsorption reaction of Cd followed the pseudo second order kinetic model, and the adsorption pseudo second order kinetic constants ($k_2$) increased with increasing initial HAP amounts onto activated carbon. Also, intraparticle diffusion model was used to investigate the adsorption mechanism between adsorbate and adsorbent in the aqueous phase. Surface adsorption reaction and intraparticle diffusion occur simultaneously Cd adsorption mechanism from aqueous phase in this study.

• Environmental Mutagens and Carcinogens
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• v.24 no.2
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• pp.51-66
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• 2004

Retinoids, better known as vitamin A, have been reported to inhibit the growth of several breast cancer cell lines in culture and to reduce breast tumor growth in animal models. Furthermore, retinoids can augment the action of other breast cancer cell growth inhibitors both in vitro and in vivo. Clinically, interest has increased in the potential use of retinoids for the prevention and treatment of human breast cancer. We have examine the effect of all-trans retinoic acid(tRA) and 9-cis retinoic acid(9-cis RA) on human breast cancer cell(MCF-10A, T47-D, MCF-7) proliferation using MTT assay and cell cycle analysis(FACS). Overexpression of cyclin D1 protein is observed in the majority of breast cancers, suggesting that dysregulated expression of cyclin D1 might be a critical event in breast cancer carcinogenesis. We investigated whether tRA and 9-cis RA might affect expression of cyclin D1 on human breast cancer cells(MCF-10A, T47-D, MCF-7) using RT-PCR and west-ern bolt. In MCF-10A cells, either tRA or 9-cis RA treatment did not affect the cell proliferation. In T47-D cells and MCF-7 cells, either tRA or 9-cis RA treatment showed the inhibition of the cell proliferation over control cells and also inhibit the estrogen stimulated cell proliferation when it was given together with estrogen. The effect of retinoids was dose- and time- dependent. T47-D cells treated with 1.0 $\muM$ tRA undergo G0/G1-phase arrest by Day 5. MCF-7 cells treated with 1.0 $\muM$ tRA undergo S-phase arrest by Day 5. All-trans retinoic acid(tRA) and 9-cis retinoic acid(9-cis RA) inhibited the cyelin D1 mRNA and protein expression levels of human MCF-7 and T47-D breast carcinoma cells in vitro. The data indicate that retinoids can reduce cyclin D1 expression levels in a variety of breast cell lines in vitro and result in inhibition of cell proliferation. tRA-mediated growth inhibition and cyclin D1 expression inhibition is more potent than 9-cis RA mediated that. tRA-mediated inhibition effect is more potent on T47-D cells than on MCF-7 cells. Our data suggest that retinoids activity is different according to property of cell lines. Future chemoprevention of breast cancer studies using retinoids will be necessary to determine the mechanism of the retinoids-mediated growth inhibition.

• Korean Journal of Food Science and Technology
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• v.25 no.2
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• pp.148-153
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• 1993

Composition and structure of synthetic glucitol fatty acid polyesters (GPE)-a potential fat substitute-were investigated. Also degree of substitution (D.S) of GPE was determined according to the relative ester distribution within it to evaluate the feasibility of GPE using as a fat substitute. The GPE was separated into single ester group by a normal-phase HPLC and D.S of it was identified to be 6. Absorption band at $1747\;cm^{-1}$ in the IR spectrum of GPE indicated that there were ester bonds within GPE molecules. which link fatty acid moiety to glucitol. Disappearance of the hydroxyl proton signals of glucitol in the H-NMR spectrum of GPE implied that most of hydroxyl groups in glucitol participated in the formation of ester bonds with fatty acids. In addition the D.S estimated from the quantitative proton integration of GPE coincided well with the D.S of GPE determined by hydroxyl value measurement. In conclusion, the GPE synthesized in this study was found to be a glucitol fatty acid hexaester so that it is expected to be used as a fat substitute in the near future.

• BMB Reports
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• v.30 no.5
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• pp.303-307
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• 1997

Grb2, which is composed of a Src homology 2 (SH2) domain and two Src homology 3 (SH3) domains, is known to serve as an adaptor protein in signaling for Ras activation. Thus, a blocker of the Grb2 interactions with other proteins can be a potential candidate for an anticancer drug. In this study, we have developed a high throughput screening method for SH3 domain binding ligands and blockers. Firstly, we made and purified the glutathione S-transferase (GST)-fusion proteins with the Grb2 SH2 and SH3 domains, and the entire Grb2. This method measures the binding of a biotin-labeled oligopeptide, derived from a Grb2/SH3 binding motif in the hSos, to the GST-fusion proteins, which are precoated as glutathione S-transferase fusion protein on a solid phase. When $1\;{\mu}g$ of each fusion protein was used to coat the wells, both N- and C- terminal SH3 the domains as well as the whole of Grb2 were able to interact with the biotin-conjugated ligand peptide, while the SH2 domain and GST alone showed no binding affinity. Although N- and C- terminal SH3 domains showed an increase of binding to the ligand peptide in proportion to the amount of peptide, the GST fusion protein with Grb2 demonstrated much higher binding affinity. GST-Grb2 coating on the solid phase showed a saturation curve; 66 and 84% of the maximal binding was observed at 100 and 300 ng/$100\;{\mu}l$, respectively. This binding assay system was peptide sequence-specific, showing a dose-dependent inhibition with the unlabeled peptide of SH3 binding motif. Several other peptides, such as SH2 domain binding motifs and PTB domain binding motif, were ineffective to inhibit the binding to the biotin-conjugated ligand peptide. These results suggest that our method may be useful to screen for new anticancer drug candidates which can block the signaling pathways mediated by SH3 domain binding.

• Korean Journal of Environmental Agriculture
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• v.25 no.4
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• pp.331-338
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• 2006

Coal combustion fly ash, which has a high available Si content and alkaline pH, was selected as a potential source of soil amendment in this study. Two field experiments were carried out to evaluate the possibility of heavy metal accumulation in silt loam (Pyeongtaeg series) and loamy sand (Nagdong series) of rice (Oryza sativa) paddy soils to which 0, 40, 80, and $120Mg\;ha^{-1}$ of fly ash were added. Rice yields increased significantly with fly ash application and the highest rice yields were achieved following the addition of around $90Mg\;ha^{-1}$ fly ash. Fly ash increased the soil pH but did not increase heavy metal uptakes of rice and heavy metal concentration in soils, due to very low concentration of heavy metals in the selected fly ash. Labile fraction of heavy metals (exchangeable + acidic fraction) was scarcely contained and most of them were stable and unavailable form (oxidizable and residual fraction). In conclusion fly ash could be a good supplement to an inorganic soil amendments without heavy metal contamination in paddy soils.

• Clinical and Experimental Pediatrics
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• v.48 no.5
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• pp.495-499
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• 2005

Purpose : Interleukin-4(IL-4) is a critical component of the Th2 cytokine pathway and contributes to severity of respiratory syncytial virus(RSV) bronchiolitis. Previous studies observed an association between severe RSV bronchiolitis in Korean children with a common haplotype of the IL4 promoter. This study was performed to investigate functional differences of the variant IL4 promoter haplotypes. Methods : Genomic DNA was obtained from 20 children from 6 to 48 months of age in the Department of Pediatrics, Seoul National University Bundang Hospital. The IL4 promoter spanning an 1.2 kb region was amplified and haplotype was determined by cloning and the PHASE reconstruction. Transcriptional activity of Jurkat T cells which were transfected with each IL4 haplotype were analyzed by use of luciferase assay. Results : Three haplotypes of the IL4 promoter have been identified with the frequency of GCC(7 percent), TCC(17 percent), and TTT(76 percent). The TTT haplotype demonstrated the highest luciferase values in both unstimulated and PMA-stimulated Jurkat T cells. Increases in transcriptional activity compared to GCC have been shown in TTT(5.3 fold higher) followed by TCC(4.2 fold higher) in unstimulated Jurkat T cells. Conclusion : We provided evidence that increased transcriptional activity of the TTT haplotype of the IL4 promoter, which has previously been over-represented in Korean children with severe RSV bronchiolitis. Therefore, IL-4 could play a potential role in the pathogenesis of RSV infection, possibly via an altered transcriptional activity of the different IL4 haplotypes.