• 제목/요약/키워드: New-Ring Test

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Bioequivalence Evaluation of Lovastatin Tablets (로바스타틴 정제의 생물학적 동등성 평가)

  • Bok, Hae Sook;Kim, Myoung Min;Choi, Kyung Eob
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.107-112
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    • 1998
  • Lovastatin is a lipid lowering agent for the treatment of hypercholesterolemia and belongs to a new class of pharmacologic compounds called the 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors. By competitively inhibiting HMG CoA reductase, lovastatin disrupts the biosynthesis of cholesterol in hepatic and peripheral cells and increases the synthesis of high-density-lipoprotein HDL) receptors. Following oral administration, the lactone ring of lovastatin is hydrolysed to the active inhibitor of HMG CoA reductase, lovastatin acid. Lovastatin is known to have poor oral absorption and wide individual variation. In this study, bioequivalence test of two lovastatin formulations, the test drug ($Lovaload^{TM}$, Chong Kun Dang Pharmaceutical Co.) and the reference drug ($Mevacor^{TM}$, Chung Wae Pharmaceutical Co.) were conducted according to the guidelines of Korea Food and Drug Administration (KFDA). A total of 18 healthy male volunteers, $31.90\pm3.60$ years old and $72.17\;7.88$ kg of body weight in average, were evaluated in a randomized crossover manner with a 2-week washout period. Concentrations of lovastatin acid in plasma were measured upto 12 hours following a single oral administration of eight tablets (20 mg of lovastatin per tablet) by high-performance liquid chromatography with UV detection at 238 nm. The area under the concentration-vs-time curve from 0 to 12 hours $(AUC_{0-12h})$ was calculated by the trapezoidal summation method. The statistical analysis showed that there are no significant differences in $AUC_{0-12h),\;C_{max}\;and\;T_{max}$ between the two formulations ($6.72\%,\;1.52\%,\;and\;0.88\$, respectively). The least significant differences between the formulations at $\alpha$=0.05 were less than $20\%\;(11.65\%,\;19.73\%,\;and\;14.81\%\;for\;AUC_{0-12h},\;C_{max}\;and\;T_{max}$, respectively). The $90\%$ confidence intervals for these parameters were also within $\pm20\%\;(-1.50{\leq}{\delta}{\leq}15.00$, $-12.50{\leq}{\delta}{\leq}15.50,\;and\;-9.64{\leq}{\delta]{\leq}11.40{\leq}\;for\;\;AUC_{0-12h}$ ,$C_{max}\;and\;T_{max}$, respectively). In conclusion, the new generic product $Lovaload^{TM}$ was proven to be bioequivalent with the reference drug.

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Influence of 3-(N-methyl-N-X(Sub.)Phenylaminooxoacetyl) Group on the Herbicidal Activity of Imazapyr Derivatives (Imazapyr 유도체의 제초활성에 미치는 3-(N-methyl-N(X)-치환-Phenylaminooxoacetyl) Group의 영향)

  • Sung, N.D.;Ryu, T.S.;Chang, H.S.;Kim, D.W.
    • Applied Biological Chemistry
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    • v.37 no.6
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    • pp.516-521
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    • 1994
  • New seventeen imazapyr derivatives, 2-(4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl)-3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl)pyridine, 6 were synthesized and their pre-emergence herbicidal activity$(pI_{50})$ in vivo against Corn (Zea mays L.) and Pigweed (Amaranthus viridis L.) were studied by the pot test under paddly conditions. Quantitative structure activity relationships (QSARs) were analyzed using the physicochemical parameters of substituent(X) on the phenyl ring of 3-(N-methyl-N-X(sub.)-phenylaminooxoacetyl) group and regression analysis. The herbicidal activities were related to the steric effect of X-substituent. The effect was rationalized by paraholic function of MR and $L_1$, where the optimal values were MR=5.56 (Zea mays L.) and $L_1=3.34\;{{\AA}}$ (Amaranthus viridis L.). Among them, 2,5-difluoro substituted compound, 6i showed good herbicidal activity against Pigweed with excellent tolerance to Corn.

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Development and testing of multicomponent fuel cladding with enhanced accidental performance

  • Krejci, Jakub;Kabatova, Jitka;Manoch, Frantisek;Koci, Jan;Cvrcek, Ladislav;Malek, Jaroslav;Krum, Stanislav;Sutta, Pavel;Bublikova, Petra;Halodova, Patricie;Namburi, Hygreeva Kiran;Sevecek, Martin
    • Nuclear Engineering and Technology
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    • v.52 no.3
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    • pp.597-609
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    • 2020
  • Accident Tolerant Fuels have been widely studied since the Fukushima-Daiichi accident in 2011 as one of the options on how to further enhance the safety of nuclear power plants. Deposition of protective coatings on nuclear fuel claddings has been considered as a near-term concept that will reduce the high-temperature oxidation rate and enhance accidental tolerance of the cladding while providing additional benefits during normal operation and transients. This study focuses on experimental testing of Zr-based alloys coated with Cr-based coatings using Physical Vapour Deposition. The results of long-term corrosion tests, as well as tests simulating postulated accidents, are presented. Zr-1%Nb alloy used as nuclear fuel cladding serves as a substrate and Cr, CrN, CrxNy layers are deposited by unbalanced magnetron sputtering and reactive magnetron sputtering. The deposition procedures are optimized in order to improve coating properties. Coated as well as reference uncoated samples were experimentally tested. The presented results include standard long-term corrosion tests at 360℃ in WWER water chemistry, burst (creep) tests and mainly single and double-sided high-temperature steam oxidation tests between 1000 and 1400℃ related to postulated Loss-of-coolant accident and Design extension conditions. Coated and reference samples were characterized pre- and post-testing using mechanical testing (microhardness, ring compression test), Thermal Evolved Gas Analysis analysis (hydrogen, oxygen concentration), optical microscopy, scanning electron microscopy (EDS, WDS, EBSD) and X-ray diffraction.

Development of Determining Technique of Optimum Signal Time of Intersections On Median Exclusive Bus Lane using Bus-only Signal (중앙버스전용차로 버스전용신호 도입시 신호 최적화에 관한 연구)

  • Kim, Bo-Gyeom;Kim, Seung-Il;Kim, Yeong-Chan;Kim, Jin-Tae
    • Journal of Korean Society of Transportation
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    • v.24 no.5 s.91
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    • pp.123-133
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    • 2006
  • Seoul and many large cities in Korea have implemented Median Exclusive Bus Lane(MEB). But exclusive bus lane in the middle of the road caused new contradictions between left turn movement and through bus movement and several signal operation techniques like 'left turn Protected' and 'overlap phase' couldn't be applied in intersections on MEB. We suggest 'Bus-only Signal for median lane technique as solution of these problems This study presents optimum signal time design process and detailed algorithms for intersections where bus-only signals are installed. As a test field. we took Yang-Je intersection where Median Exclusive Bus Lane go through. and have large gap in volume of left turn in main direction. And we verified that revised optimum signal time including overlap phase can reduce average delay time of vehicle through before and after simulation.

Pharmacophore Mapping and Virtual Screening for SIRT1 Activators

  • Sakkiah, Sugunadevi;Krishnamoorthy, Navaneethakrishnan;Gajendrarao, Poornima;Thangapandian, Sundarapandian;Lee, Yun-O;Kim, Song-Mi;Suh, Jung-Keun;Kim, Hyong-Ha;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1152-1156
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    • 2009
  • Silent information regulator 2 (Sir2) or sirtuins are NAD(+)-dependent deacetylases, which hydrolyze the acetyllysine residues. In mammals, sirtuins are classified into seven different classes (SIRT1-7). SIRT1 was reported to be involved in age related disorders like obesity, metabolic syndrome, type II diabetes mellitus and Parkinson’s disease. Activation of SIRT1 is one of the promising approaches to treat these age related diseases. In this study, we have used HipHop module of CATALYST to identify a series of pharmacophore models to screen SIRT1 enhancing molecules. Three molecules from Sirtris Pharmaceuticals were selected as training set and 607 sirtuin activator molecules were used as test set. Five different hypotheses were developed and then validated using the training set and the test set. The results showed that the best pharmacophore model has four features, ring aromatic, positive ionization and two hydrogen-bond acceptors. The best hypothesis from our study, Hypo2, screened high number of active molecules from the test set. Thus, we suggest that this four feature pharmacophore model could be helpful to screen novel SIRT1 activator molecules. Hypo2-virtual screening against Maybridge database reveals seven molecules, which contains all the critical features. Moreover, two new scaffolds were identified from this study. These scaffolds may be a potent lead for the SIRT1 activation.

Pharmacophore Modeling, Virtual Screening and Molecular Docking Studies for Identification of New Inverse Agonists of Human Histamine H1 Receptor

  • Thangapandian, Sundarapandian;Krishnamoorthy, Navaneethakrishnan;John, Shalini;Sakkiah, Sugunadevi;Lazar, Prettina;Lee, Yu-No;Lee, Keun-Woo
    • Bulletin of the Korean Chemical Society
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    • v.31 no.1
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    • pp.52-58
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    • 2010
  • Human histamine H1 receptor (HHR1) is a G protein-coupled receptor and a primary target for antiallergic therapy. Here, the ligand-based three-dimensional pharmacophore models were built from a set of known HHR1 inverse agonists using HypoGen module of CATALYST software. All ten generated pharmacophore models consist of five essential features: hydrogen bond acceptor, ring aromatic, positive ionizable and two hydrophobic functions. Best model had a correlation coefficient of 0.854 for training set compounds and it was validated with an external test set with a high correlation value of 0.925. Using this model Maybridge database containing 60,000 compounds was screened for potential leads. A rigorous screening for drug-like compounds unveiled RH01692 and SPB00834, two novel molecules for HHR1 with good CATALYST fit and estimated activity values. The new lead molecules were docked into the active site of constructed HHR1 homology model based on recently crystallized squid rhodopsin as template. Both the hit compounds were found to have critical interactions with Glu177, Phe432 and other important amino acids. The interpretations of this study may effectively be deployed in designing of novel HHR1 inverse agonists.

Lane-wise Travel Speed Characteristics Analysis in Uninterrupted Flow Considering Lane-wise Speed Reversal (차로속도역전현상을 고려한 연속류 도로의 차로별 주행 속도 특성 분석)

  • Yang, Inchul;Jeon, Woo Hoon;Ki, Sung hwan;Yoon, Jungeun
    • The Journal of The Korea Institute of Intelligent Transport Systems
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    • v.15 no.6
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    • pp.116-126
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    • 2016
  • In this study, lane-wise traffic flow characteristics were analysed on uninterrupted flow using a new notion of "lane-wise travel speed reversal (LTSR)" which is defined as a phenomena that travel speed in the median lane is lower than other lanes. Mathematical formulation was also proposed to calculate the strength of LTSR. The experiment road site is Seoul Outer Ring Expressway (Jayuro-IC~Jangsoo-IC), and travel trajectories for each four lane were collected for weekdays (Mon. through Fri.) during morning peak. Comparing lane-wise travel speeds for entire test road section, no LTSR was observed, meaning that the travel speed in the median lane is the fastest, followed by 2nd, 3rd, and 4th lane as in order. Howerver, the result of microscopic analysis using 100-meter discrete road section based data shows that LTSR occurs many times. Especially the strength of LTSR is higher in congestion area and freeway merge and diverge segment. It is expected that these results could be used as a fundamental data when establishing lane-by-lane traffic operation strategy and developing lane-wise traffic information collection and dissemination technology.

Occurrence of Target Spot on Rosemary Caused by Corynespora cassiicola in Korea (Corynespora cassiicola에 의한 로즈마리 점무늬병)

  • Lee, Wang-Hyu;Han, Sang-Jun;Choi, In-Young
    • Research in Plant Disease
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    • v.19 no.1
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    • pp.55-59
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    • 2013
  • The purpose of this experiment was to investigate the development of new spot disease on the leaf and stem of rosemary (Rosmarinus officinalis) in commercial greenhouses at Jeonju and Namwon in Korea. Incidence of target spot on rosemary was higher at the end of the rainy season with high humidity. Those symptoms were black ring spots (3-5 mm in diameter) and withering on green leaves and stems. Conidiophores and conidia were formed on the infected tissue in moist chamber and conidia were shown as the cylindrical and oval types in chain, ranged from 55 to $275{\mu}m$ in length, and 7 to $14{\mu}m$ in width. Conidia with eight to ten pseudosepta were formed on the conidiapore. The optimum growth temperature of isolates was $30^{\circ}C$ on the PDA medium under the dark condition. In the pathogenesis test, the target spot and withering symptoms were appeared on the leaves and stems 3 days after inoculation showing similar symptoms compared to those of in nature. The same fungus was re-isolated from infected lesion, indicating that Corynespora cassiicola caused leaf target spot and twig blight on rosemary. The rDNA ITS nucleotide sequences of the pure cultured isolate from the diseased area on rosemary showed 100% similarity to the sequences of C. cassiicola available in the GenBank database (JQ595296, JQ595297, FJ852715 and AY238606). Therefore, we report that the target spot of leaves and stems in rosemary was caused by C. cassiicola.

Geotechnical Engineering Progress with the Incheon Bridge Project

  • Cho, Sung-Min
    • Proceedings of the Korean Geotechical Society Conference
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    • 2009.09a
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    • pp.133-144
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    • 2009
  • Incheon Bridge, 18.4 km long sea-crossing bridge, will be opened to the traffic in October 2009 and this will be the new landmark of the gearing up north-east Asia as well as the largest & longest bridge of Korea. Incheon Bridge is the integrated set of several special featured bridges including a magnificent cable-stayed girder bridge which has a main span of 800 m width to cross the navigation channel in and out of the Port of Incheon. Incheon Bridge is making an epoch of long-span bridge designs thanks to the fully application of the AASHTO LRFD (load & resistance factor design) to both the superstructures and the substructures. A state-of-the-art of the geotechnologies which were applied to the Incheon Bridge construction project is introduced. The most Large-diameter drilled shafts were penetrated into the bedrock to support the colossal superstructures. The bearing capacity and deformational characteristics of the foundations were verified through the world's largest static pile load test. 8 full-scale pilot piles were tested in both offshore site and onshore area prior to the commencement of constructions. Compressible load beyond 30,000 tonf pressed a single 3 m diameter foundation pile by means of bi-directional loading method including the Osterberg cell techniques. Detailed site investigation to characterize the subsurface properties had been carried out. Geotextile tubes, tied sheet pile walls, and trestles were utilized to overcome the very large tidal difference between ebb and flow at the foreshore site. 44 circular-cell type dolphins surround the piers near the navigation channel to protect the bridge against the collision with aberrant vessels. Each dolphin structure consists of the flat sheet piled wall and infilled aggregates to absorb the collision impact. Geo-centrifugal tests were performed to evaluate the behavior of the dolphin in the seabed and to verify the numerical model for the design. Rip-rap embankments on the seabed are expected to prevent the scouring of the foundation. Prefabricated vertical drains, sand compaction piles, deep cement mixings, horizontal natural-fiber drains, and other subsidiary methods were used to improve the soft ground for the site of abutments, toll plazas, and access roads. Light-weight backfill using EPS blocks helps to reduce the earth pressure behind the abutment on the soft ground. Some kinds of reinforced earth like as MSE using geosynthetics were utilized for the ring wall of the abutment. Soil steel bridges made of corrugated steel plates and engineered backfills were constructed for the open-cut tunnel and the culvert. Diverse experiences of advanced designs and constructions from the Incheon Bridge project have been propagated by relevant engineers and it is strongly expected that significant achievements in geotechnical engineering through this project will contribute to the national development of the longspan bridge technologies remarkably.

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Characterization of broad bean wilt virus 2 isolated from Perilla frutescens in Korea (국내 잎들깨에서 발생한 잠두위조바이러스2의 특성 구명)

  • Hyun-Sun Kim;Hee-Seong Byun;You-Ji Choi;Hyun-Yong Choi;Jang-Kyun Seo;Hong-Soo Choi;Bong-Choon Lee;Mikyeong Kim;Hae-Ryun Kwak
    • Korean Journal of Environmental Biology
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    • v.41 no.1
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    • pp.1-13
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    • 2023
  • Broad bean wilt virus 2 (BBWV2) is a species in the genus Fabavirus and family Secoviridae, which is transmitted by aphids and has a wide host range. The BBWV2 genome is composed of two single-stranded, positive-sense RNAs, RNA-1 and RNA-2. The representative symptoms of BBWV2 are mosaic, mottle, vein clearing, wilt, and stunting on leaves, and these symptoms cause economic damage to various crops. In 2019, Perilla fructescens leaves with mosaic and yellowing symptoms were found in Geumsan, South Korea. Reverse-transcription polymerase chain reaction (RT-PCR) was performed with specific primers for 10 reported viruses, including BBWV2, to identify the causal virus, and the results were positive for BBWV2. To characterize a BBWV2 isolate (BBWV2-GS-PF) from symptomatic P. fructescens, genetic analysis and pathogenicity tests were performed. The complete genomic sequences of RNA-1 and RNA-2 of BBWV2-GS-PF were phylogenetically distant to the previously reported BBWV2 isolates, with relatively low nucleotide sequence similarities of 76-80%. In the pathogenicity test, unlike most BBWV2 isolates with mild mosaic or mosaic symptoms in peppers, the BBWV2-GS-PF isolate showed typical ring spot symptoms. Considering these results, the BBWV2-GS-PF isolate from P. fructescens could be classified as a new strain of BBWV2.