• 약학회지
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• 제40권3호
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• pp.279-292
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• 1996

To assess their stability as a prodrug of 5-fluorouracil (5-FU), four N-acyloxycarbonyl derivatives (1-(N-tert-butyloxycarbonyl)glycyloxymethyl-5-FU :BGFU, 1-(N-tert-butyloxycar bonyl)-leucyloxymethyl-5-FU:BLFU, 1-(N-tert-carbobenzyloxymethyl) glycyloxymethyl-5-FU:CGFU and 1-(N-tert-carbobenzlyoxymethyl)leucyloxymethyl-5-FU:CLFU) possessing differently protected amino acids, and two acetic acid derivatives (5FU-1-acetylpentane:FUAP and 5-FU-1-acetylhexane:FUAH) were synthesized and their physicochemical properties, hydrolysis kinetics, acute toxicity and antitumor activity were evaluated. The lipid-water partition coefficients of six 5-FU prodrugs were higher than that of 5-FU and their aqueous solubilities were in the following rank order; BGFU>FUAP>CGFU>BLFU>CLFU${\simeq}$FUAH. The hydrolysis of N-acyloxycarboyl derivatives, greater at higher pH, was enhanced in presence of liver homogenate or human plasma. Meanwhile, acetic acid ester derivatives, very stable, were hydrolyzed by liver homogenate. Absorption rate constants were 0.181, 0.121, 0.111, 0.168, 0.168, 0.116 and 0.125 $hr^{-1}$ for 5-FU, BGFU, BLFU, CGFU, CLFU, FUAP and FUAH, respectively. The cytotoxicity of N-acyloxycarbonyl derivatives was 4 to 5 times lower than that of 5-FU, but that of acetic acid ester derivatives was negligeble. The $LD_{50}$ values were 204, 325.97 (133.59, amount as 5-FU), 708.16 (262.13), 663.50 (211.77), 382.33 (192.54) and 272.33 (130.09) mg/kg for 5-FU, BGFU, CGFU, CLFU, FUAP and FUAH, respectively. While N-acyloxycarbonyl derivatives showed enhanced antitumor activity and therapeutic ratio (3.30, 3.06, 4.19, 3.11 and 1.81 for BGFU, BLFU, CGFU, CLFU and 5-FU, respectively), FUAH and FUAP showed a smaller therapeutic ratio (0.79 and 0.83).

• Journal of Microbiology and Biotechnology
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• 제25권8호
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• pp.1299-1306
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• 2015

This study aims to investigate the mechanism of action of the cinnamon bark essential oil (CB), when used singly and also in combination with piperacillin, for its antimicrobial and synergistic activity against beta-lactamase TEM-1 plasmid-conferred Escherichia coli J53 R1. Viable count of bacteria for this combination of essential oil and antibiotic showed a complete killing profile at 20 h and further confirmed its synergistic effect by reducing the bacteria cell numbers. Analysis on the stability of treated cultures for cell membrane permeability by CB when tested against sodium dodecyl sulfate revealed that the bacterial cell membrane was disrupted by the essential oil. Scanning electron microscopy observation and bacterial surface charge measurement also revealed that CB causes irreversible membrane damage and reduces the bacterial surface charge. In addition, bioluminescence expression of Escherichia coli [pSB1075] and E. coli [pSB401] by CB showed reduction, indicating the possibility of the presence of quorum sensing (QS) inhibitors. Gas-chromatography and mass spectrometry of the essential oil of Cinnamomum verum showed that trans-cinnamaldehyde (72.81%), benzyl alcohol (12.5%), and eugenol (6.57%) were the major components in the essential oil. From this study, CB has the potential to reverse E. coli J53 R1 resistance to piperacillin through two pathways; modification in the permeability of the outer membrane or bacterial QS inhibition.

• International Journal of Automotive Technology
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• 제6권2호
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• pp.149-159
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• 2005

A full nonlinear finite element P185/70Rl4 passenger car radial-ply tire model was developed and run on a 1.7-meter-diameter spinning test drum/cleat model at a constant speed of 50 km/h in order to investigate the tire transient response characteristics, i.e. the tire in-plane free vibration modes transmissibility. The virtual tire/drum finite element model was constructed and tested using the nonlinear finite element analysis software, PAM-SHOCK, a nonlinear finite element analysis code. The tire model was constructed in extreme detail with three-dimensional solid, layered membrane, and beam finite elements, incorporating over 18,000 nodes and 24 different types of materials. The reaction forces of the tire axle in vertical (Z axis) and longitudinal (X axis) directions were recorded when the tire rolled over a cleat on the drum, and then the FFT algorithm was applied to examine the transient response information in the frequency domain. The result showed that this PI 85/70Rl4 tire has clear peaks of 84 and 45 Hz transmissibility in the vertical and longitudinal directions. This result was validated against more than 10 previous studies by either theoretical or experimental approaches and showed excellent agreement. The tire's post-impact response was also investigated to verify the numerical convergence and computational stability of this FEA tire model and simulation strategy, the extraordinarily stable scenario was confirmed. The tire in-plane free vibration modes transmissibility was successfully detected. This approach was never before attempted in investigations of tire in-plane free vibration modes transmission phenomena; this work is believed to be the first of its kind.

• 한국응용과학기술학회지
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• 제31권3호
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• pp.367-374
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• 2014

In this study, skin permeation enhancement was confirmed by designing it to have a structure and composition similarity to the intercellular lipids that improve miscibility with skin by cross-linked lipids poloxamer. The cross-linked lipids poloxamer was synthesized and analyzed by 1H NMR that structure dose had conjugated pluronic with ceramide3. Active component is released by modification of liquid crystal structure because PPO part, large-scale molecule block of pluronic, has hydrophobic nature at skin temperature of $35^{\circ}C$. Conjugated pluronic with ceramide3 was synthesized using Pluronic F127 and p-NPC (4-nitrophenyl chloroformate) at room temperature yielded 89%. Pluronic(Ceramide 3-conjugated Pluronic) was synthesized by reaction of p-NP-Pluronic with Ceramide3 and DMAP. The yield was 51%. This cross-linked lipids poloxamer was blended and dissolved at isotropic state with skin surface lipids, phospholipid, ceramide, cholesterol and anhydrous additive solvent. Next step was preceded by ${\alpha}$-Transition at low temperature for making the structure of Meso-Phase Lamella, and non-hydrous skin analogue liquid crystal using thermo-sensitivity smart sensor, lamellar liquid crystal structure through aging time. For confirmation of conjugation thermo-sensitivity smart sensor and non-hydrous skin analogue liquid crystal, structural observation and stability test were performed using XRD(Xray Diffraction), DSC(Differential Scanning Calorimetry), PM (Polarized Microscope) And C-SEM (Cryo-Scanning Electron Microscope). Thermo-sensitivity observation by Franz cell revealed that synthesized smart sensor shown skin permeation effect over 75% than normal liquid crystal. Furthermore, normal non-hydrous skin analogue liquid crystal that not applied smart sensor shown similar results below $35^{\circ}C$ of skin temperature, but its effects has increased more than 30% above $35^{\circ}C$.

• 공업화학
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• 제22권2호
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• pp.155-160
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• 2011

동물성유지는 식물성유지에 비해 산화안정성이 뛰어나며, 높은 발열량과 세탄가를 보여 불완전 연소율이 낮다는 장점을 가지고 있으나 포화지방산의 함량이 높고, 원료유지에 불순물 함량이 높아 정제과정이 필요하다는 단점을 가지고 있다. 본 연구에서는 동물성 유지로 폐돈지를 선정하여 초음파에너지를 이용한 전이에스테르화반응의 최적조건을 설정하고자 하였다. 또한 기존공정의 가열 및 교반을 대체할 수 있는 초음파에너지 효과를 확인함으로써 새로운 바이오디젤 제조공정을 제시하고자 하였다. 기존가열방식을 이용한 폐돈지의 전이에스테르화 반응은 $55^{\circ}C$에서 메탄올과 돈지의 반응몰비 12에서 1 h 반응한 경우 가장 우수한 전환특성을 나타내었다. 전이에스테르화 반응에 초음파에너지를 조사할 경우 최적 초음파 조사세기 500 W에서 반응시간을 30 min으로 크게 단축할 수 있었다. 또한 제조된 바이오디젤의 성능평가 결과 점도는 $0{\sim}70^{\circ}C$ 범위에서 1.3~4.0 cP, 발열량은 40.3 MJ/kg으로 바이오디젤 성능기준을 만족하였다.

• 한국진공학회:학술대회논문집
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• 한국진공학회 1998년도 제14회 학술발표회 논문개요집
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• pp.17-17
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• 1998

Synchrotron radiation is produced when charged particles moving with relativistic velocities a are accelerated - for example, deflected by the bending magnets which guide the electron or p positrons in circular accelerators or storage rings. By using special focusing magnetic lattices i in the particle accelerators it is possible to make the dimensions of the particle beam very small with a hi맹 charge density which results in a light source with high b디lIiance. Synchrotron light h has important properties which make it ideal for a wide range of investigations in surface s science. The fact that the spectrum of electromagnetic radiation emitted in a bending magnet e extends in a continuum from the 얹r infra red region to hard x-rays means that it is id않I for a v variety of spectroscopic studies. Since there are no convenient lasers, or other really bright l light sources, in the vacuum ultraviolet and soft x-ray re.밍ons the development of synchrotron r radiation has enabled enormous advances to be made in this di펌C비t spectr따 re밍on. P Polarization-dependent measurements, for ex없nple ellipsometry or circular dichroism studies a are possible because the radiation has a well-defined polarization - linear in the plane of orbit w with additional right-circular, or left-circular, components for emission an생es above, or below, t the horizontal, respectively. Since the synchrotron light is emitted from a bunch of charge c circulating in a ring the light is emitted with a well-defined time structure with a short flash of l light every time a bunch passes an exit port. The time structure depends on the size of the ring a and the number and sequence of filling of the bunches. A pulsed light source enables time¬r resolved studies to be performed which provide direct information on the lifetimes and decay m modes of excited states and in addition opens up the possibility of using time of flight t techniques for spectroscopic studies. The fact that synchrotron radiation is produced in a clean u ultrahi야 vacuum environment is of gr않t importance for surce science studies. The current t비rd generation synchrotron light sources provide exceptionally high baliance and stability a and open up possibilities for experiments which would have been inconceivable only a short time ago.

• 한국식품저장유통학회지
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• 제31권3호
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• pp.394-407
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• 2024

The poultry industry faces disposal difficulty in waste, but recent advancements in material science and sustainability have enabled the innovative transformation of waste into valuable resources. In this study, eggshell (EC) was added as a bio-filler to gum Arabic (GA) to fabricate a GA-EC bio-composite film. Bio-composites containing 0.5 g (GA-EC_0.5) and 1.0 g (GA-EC_1.0) EC dispersed in 30 mL of 15% GA solution were fabricated and characterized using standard analytical techniques. The GA-EC_0.5 composites showed significantly higher moisture content, transparency, water solubility, and water vapor permeability but lower tensile strength and thermal stability than GA-EC_1.0. Following a post-harvest wrapping of tomato fruits with the GA-EC composite films and storage at 25±2℃ for 20 days, significant (p>0.05) reductions in weight loss, pH, lycopene content, and activities of polyphenol oxidase and pectin methylesterase compared to unwrapped fruits were recorded. Adding EC to GA has enabled the fabrication of composite films with improved mechanical, barrier, and thermal properties with potential application in the post-harvest storage of tomato fruits.

• 생명과학회지
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• 제15권1호
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• pp.118-123
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• 2005

B. stearothermophilus 유래의 CGTase 유전자(cgtS)를 보유하고 있는 재조합 plasmid pCGTS (4.8 kb)을 효모 표면 발현용 vector인 pYDl (GAL1 promoter)에 subcloning 하였다. 구축된 재조합 plasmid, pYDCGT (7.2 kb)는 S. cerevisiae EBY100에 형질전환하였고, tryptophan이 결여된 SD 배지에서 1차 선별된 형질전환체들을 YPGS배지에서 배양 후 활성 염색을 통하여 CD가 생 성 됨을 확인하였다. 배양시간과 효소반응시간에 따른 반응 산물을 TLC로 분석 한 결과, 배양 12시간째부터 효소활성이 나타났고, 반응 10분 이후부터 CD가 생성되어 시간이 지남에 따라 CD 생성양이 증가하는 것을 확인하였다. 회분 배양한 결과 $25^{\circ}C$와 $30^{\circ}C$에서 CGTase의 최대 활성이 각각 21.3 unit/1 와 16.5 unit/1로 나타났고, plasmid 안정성은 각각 $86\%$와 $82\%$로 나타나 배양온도에 상관없이 plasmid는 비교적 안정하게 유지되었다.

• Asian-Australasian Journal of Animal Sciences
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• 제15권2호
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• pp.266-273
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• 2002

A total of 225 day-old broiler chicks (43.08 g initial body weight) were allotted to three dietary treatments for a 6-week feeding trial. The treatments were 1) Control (defatted rice bran; DFRB), 2) fresh rice bran (FRB) and 3) rancid rice bran (RRB). Rice brans were intentionally spoiled by two degrees of rancidity by the values of free fatty acids (FFA): 7.6% (FRB) and 16.3% (RRB). Diets were prepared on an isonutrient basis, and defatted or rancid rice brans were included 5 and 10% for starter (0-3 week) and finisher (3-6 week), respectively. At the end of the feeding trial, six chicks per treatment were sacrificed, and thigh meats were ground and stored at $1^{\circ}C$ for thiobarbituric acid reactive substances (TBARS) and peroxide value (POV) analyses. For a digestibility, 48 growing chicks (4 weeks old) were employed in cages (3 replicates/treatment, 2 birds/cage) according to the experimental design: FRB, RRB, pelleted and extruded rice bran. Some of the FRB were pelleted ($70^{\circ}C$) or extruded ($110^{\circ}C$). There was no significant difference in growth performance during the starter period, but chicks fed a diet containing DFRB grew faster (p<0.05) with increased feed intake (p<0.05) than those fed diets containing rice brans, FRB or RRB, during the finisher period. Feed conversion ratio in the RRB was inferior (p<0.05) to the DFRB. Between rice bran groups, weight gain was higher (pco.os) in FRB than in RRB during finisher period. There was a similar trend in growth performance of chicks for the overall period (0-6 week) as the finisher period. Dry matter and energy digestibilities were higher (p<0.05) in extruded than in RRB group. Protein digestibility was improved (p<0.05) when rice bran was extruded, but not pelleted. The chicken meats from RRB showed higher (p<0.05) TBARS than those from FRB during storage for 4 weeks at $1^{\circ}C$. In conclusion, it would appear that feeding rancid rice bran gave negative effects on growth performance and lipid stability of meat in broiler chicks.

• Animal Bioscience
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• 제34권6호
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• pp.993-1005
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• 2021

Objective: Zearalenone (ZEA) has estrogen-like effects. Our previous study has shown that ZEA (0.5 to 1.5 mg/kg) could induce abnormal uterine proliferation through transforming growth factor signaling pathway. To further study the other regulatory networks of uterine hypertrophy caused by ZEA, the potential mechanism of ZEA on porcine endometrial epithelial cells (PECs) was explored by the Illumina Hiseq 2000 sequencing system. Methods: The PECs were treated with ZEA at 0 (ZEA0), 5 (ZEA5), 20 (ZEA20), and 80 (ZEA80) µmol/L for 24 h. The collected cells were subjected to cell cycle, RNA-seq, real-time quantitative polymerase chain reaction, immunofluorescence, and western blot analysis. Results: The proportion of cells in the S and G2 phases decreased (p<0.05), but the proportion of cells in the G1 phase increased (p<0.05) in the ZEA80 treatment. Data analysis revealed that the expression of Wnt pathway-related genes, estrogen-related genes, and mitogen-activated protein kinase pathway-related genes increased (p<0.05), but the expression of genetic stability genes decreased (p<0.05) with increasing ZEA concentrations. The relative mRNA and protein expression of WNT1, β-catenin, glycogen synthase kinase 3β (GSK-3β) were increased (p<0.05) with ZEA increasing, while the relative mRNA and protein expression of cyclin D1 (CCND1) was decreased (p<0.05). Moreover, our immunofluorescence results indicate that β-catenin accumulated around the nucleus from the cell membrane and cytoplasm with increasing ZEA concentrations. Conclusion: In summary, ZEA can activate the Wnt/β-catenin signaling pathway by up-regulating WNT1 and β-catenin expression, to promote the proliferation and development of PECs. At the same time, the up-regulation of GSK-3β and down-regulation of CCND1, as well as the mRNA expression of other pathway related genes indicated that other potential effects of ZEA on the uterine development need further study.