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High Throughput Screening for Natural Products to Find Biologically Active Compounds : Natural Products versus Combinatorial Chemistry

  • Sankawa, Ushio
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.11a
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    • pp.47-50
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    • 1997
  • Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

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DESIGN AND FABRICATION OF S-BAND DIPLEXER FOR LEO TT&C APPLICATION (저궤도 위성 관제용 S-대역 다이플렉서 설계 및 제작)

  • Ahn, Sang-Il;Park, Dong-Chul
    • Journal of Astronomy and Space Sciences
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    • v.24 no.4
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    • pp.397-408
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    • 2007
  • Diplexer is one of core devices needed to communicate with satellite using single ground antenna by separating uplink and downlink signal. This paper presents the design of the S-band diplexer for LEO TT&C application, especially for KOMPSAT (KOrea Multi-Purpose SATellite). To cope with requirements such as high handling power, low insertion loss, air-cavity resonator with high quality factor was considered as one of design drivers. Design was started with predicting unloaded Q and equivalent circuit from the structure of air-cavity resonator. For the convenience of adjustment, the coupling factor placed between resonators was estimated from COTSEM (Electro-Magnetic) simulator, EESOF $ADS^{TM}$, and expressed with 2-order polynomial regression. To improve the isolation between transmitting part (Tx) and receiving part (Rx), the inductive and capacitive attenuation poles were inserted between $4^{th}\;and\;6^{th}$ resonator respectively. The fabricated diplexer consists of two bandpass filters and each filter has eight resonants. From the measurement, it was shown that major requirements such as 0.5dB of insertion loss, 20dB of return loss and 100dB of isolation were fully satisfied within passband.

Effect of a Time Dependent Concrete Modulus of Elasticity on Prestress Losses in Bridge Girders

  • Singh, Brahama P.;Yazdani, Nur;Ramirez, Guillermo
    • International Journal of Concrete Structures and Materials
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    • v.7 no.3
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    • pp.183-191
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    • 2013
  • Prestress losses assumed for bridge girder design and deflection analyses are dependent on the concrete modulus of elasticity (MOE). Most design specifications, such as the American Association of State Highways and Transportation Officials (AASHTO) bridge specifications, contain a constant value for the MOE based on the unit weight of concrete and the concrete compressive strength at 28 days. It has been shown in the past that that the concrete MOE varies with the age of concrete. The purpose of this study was to evaluate the effect of a time-dependent and variable MOE on the prestress losses assumed for bridge girder design. For this purpose, three different variable MOE models from the literature were investigated: Dischinger (Der Bauingenieur 47/48(20):563-572, 1939a; Der Bauingenieur 5/6(20):53-63, 1939b; Der Bauingenieur, 21/22(20):286-437, 1939c), American Concrete Institute (ACI) 209 (Tech. Rep. ACI 209R-92, 1992) and CEB-FIP (CEB-FIP Model Code, 2010). A typical bridge layout for the Dallas, Texas, USA, area was assumed herein. A prestressed concrete beam design and analysis program from the Texas Department of Transportation (TxDOT) was utilized to determine the prestress losses. The values of the time dependent MOE and also specific prestress losses from each model were compared. The MOE predictions based on the ACI and the CEB-FIP models were close to each other; in long-term, they approach the constant AASHTO value. Dischinger's model provides for higher MOE values. The elastic shortening and the long term losses from the variable MOE models are lower than that using a constant MOE up to deck casting time. In long term, the variable MOE-based losses approach that from the constant MOE predictions. The Dischinger model would result in more conservative girder design while the ACI and the CEB-FIP models would result in designs more consistent with the AASHTO approach.

A Detection Algorithm Study of the Victim Signal for the DAA Regulation in MB-OFDM UWB System (MB-OFDM UWB 시스템에서 DAA 기술 기준 적용을 위한 피 간섭 신호 검출 방안 연구)

  • Shin, Cheol-Ho;Choi, Sang-Sung
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.20 no.12
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    • pp.1297-1307
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    • 2009
  • The purpose of this paper is to propose a detection algorithm and a tracking algorithm based on silent time using MB-OFDM UWB(Multi-Band Orthogonal Frequency Division Multiplexing Ultra Wide Band) receiver in order to satisfy DAA(Detect And Avoid) regulation of Korea to permit UWB in 3.1~4.8 GHz. In DAA regulation of Korea, if UWB device receives a signal more than -80 dBm/MHz from the victim system during UWB operation, the UWB system should avoid the collision within 2 sec. In this paper, we proposed the detection algorithm to detect the victim signal received by -80 dBm/MHz for the avoidance process that changes the operating UWB frequency to other UWB frequency and the subcarrier tracking algorithm to follow up the subcarrier positions of the victim signal for the tonenulling avoidance process that decreases the TX power of subcarriers occupied by the victim signal by -70 dBm/MHz. The performance of the detection algorithm and the tracking algorithm suggested in this paper is verified in simulation results considering various conditions.

Investigation of the Optical and Cloud Forming Properties of Pollution, Biomass Burning, and Mineral Dust Aerosol

  • Lee Yong-Seop
    • Proceedings of the Korea Air Pollution Research Association Conference
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    • 2006.04a
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    • pp.55-56
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    • 2006
  • This thesis describes the use of measured aerosol size distributions and size-resolved hygroscopic growth to examine the physical and chemical properties of several particle classes. The primary objective of this work was to investigate the optical and cloud forming properties of a range of ambient aerosol types measured in a number of different locations. The tool used for most of these analyses is a differential mobility analyzer / tandem differential mobility analyzer (DMA / TDMA) system developed in our research group. To collect the data described in two of the chapters of this thesis, an aircraft-based version of the DMA / TDMA was deployed to Japan and California. The data described in two other chapters were conveniently collected during a period when the aerosol of interest came to us. The unique aspect of this analysis is the use of these data to isolate the size distributions of distinct aerosol types in order to quantify their optical and cloud forming properties. I used collected data during the Asian Aerosol Characterization Experiment (ACE-Asia) to examine the composition and homogeneity of a complex aerosol generated in the deserts and urban regions of China and other Asian countries. An aircraft-based tandem differential mobility analyzer was used for the first time during this campaign to examine the size-resolved hygroscopic properties of particles having diameters between 40 and 586 nm. Asian Dust Above Monterey (ADAM-2003) study was designed both to evaluate the degree to which models can predict the long-range transport of Asian dust, and to examine the physical and optical properties of that aged dust upon reaching the California coast. Aerosol size distributions and hygroscopic growth are measured in College Station, TX to investigate the cloud nucleating and optical properties of a biomass burning aerosol generated from fires on the Yucatan Peninsula. Measured aerosol size distributions and size-resolved hygroscopicity and volatility were used to infer critical supersaturation distributions of the distinct particle types that were observed during this period. The predicted CCN concentrations were used in a cloud model to determine the impact of the different aerosol types on the expected cloud droplet concentration. RH-dependent aerosol extinction coefficients are calculated at a wavelength of 550 nm.

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Detection of the Fungicide Iprovalicarb Residues Using a Surface Plasmon Resonance Biosensor (표면플라즈몬공명 바이오센서를 이용한 살균제 Iprovalicarb 잔류물의 검출)

  • Kim, Woon-Ho;Cho, Han-Keun;Kyung, Kee-Sung;Kim, Gi-Young
    • Journal of Biosystems Engineering
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    • v.34 no.1
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    • pp.50-56
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    • 2009
  • Surface plasmon resonance (SPR) biosensor has been used to detect many biochemical reactions, because this label-free sensor has high sensitivity and rapid response. The reactions are monitored by refractive index changes of the SPR biosensor. Iprovalicarb is protective, curative, and eradicative systemic fungicide introduced by Bayer AG in 1999. It has potential far control of downy mildew infesting onion, cucumber, grape and melon, late blight infesting tomato and potato, and anthracnose infesting watermelon and pepper. It is strictly limited to the maximum residue limit. In this study, the applicability of a portable SPR biosensor (Spreeta, Texas instrument, TX, USA) to detect the iprovalicarb residue was examined. The sensor chip was adopted to detect the reaction of iprovalicarb to immobilized iprovalicarb-antibody. The binding of the iprovalicarb onto the biosensor surface was measured by change of the refractive index (RI). Characteristics of the sensor chip including specificity, sensitivity, stability, and reusability were analyzed. In calibration test for seven levels of iprovalicarb concentration (0.32 to 5,000 mg/L) with three replications, a Sigmoidal model with Hill function was obtained between relative RI value and the iprovalicarb concentration with R-square of 0.998. It took 30 minutes to complete a set of detecting assay with the SPR biosensor.

320-Channel Multi-Frequency Trans-Admittance Scanner(TAS) for Anomaly Detection (도전율 및 유전율이 다른 병소의 검출을 위한 320-채널 다주파수 Trans-Admittance Scanner(TAS))

  • Oh, Tong-In;Lee, Min-Hyoung;Kim, Hee-Jin;Woo, Eung-Je
    • Journal of Biomedical Engineering Research
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    • v.28 no.1
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    • pp.84-94
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    • 2007
  • In order to collect information on local distribution of conductivity and permittivity underneath a scan probe, we developed a multi-frequency trans-admittance scanner (TAS). Applying a sinusoidal voltage with variable frequency on a chosen distal part of a human body, we measure exit currents from 320 grounded electrodes placed on a chosen surface of the subject. The electrodes are packaged inside a small and light scan probe. The system includes one voltage source and 17 digital ammeters. Front-end of each ammeter is a current-to-voltage converter with virtual grounding of a chosen electrode. The rest of the ammeter is a voltmeter performing digital phase-sensitive demodulation. Using resistor loads, we calibrate the system including the scan probe to compensate frequency-dependent variability of current measurements and also inter-channel variability among multiple. We found that SNR of each ammeter is about 85dB and the minimal measurable current is 5nA. Using saline phantoms with objects made from TX-151, we verified the performance of the lesion estimation algorithm. The error rate of the depth estimation was about 19.7%. For the size estimate, the error rate was about 15.3%. The results suggest improvement in lesion estimation algorithm based on multi-frequency trans-admittance data.

Inhibitory Effects of Moutan Cortex Radicis Extracts and Paeonol on Rabbit Platelet Aggregation

  • Lee, Kyung-Sup;Oh, Ki-Wan;Bae, Ki-Hwan;Kim, Young-Ho;Lee, Mi-Yea;Cho, Mi-Ra;Jin, Yong-Ri;Yun, Yeo-Pyo
    • Journal of Food Hygiene and Safety
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    • v.19 no.3
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    • pp.167-170
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    • 2004
  • The present study was undertaken to investigate the effects of Moutan Cortex Radicis extracts and paeonol, a major component, on rabbit platelet aggregation and thromboxane (TX) $A_2$ formation. Moutan Cortex Radicis methanol and butanol layers (100 ${\mu}g/mL$) showed the weak inhibitions, and water layer (100 ${\mu}g/mL$) had no effect on the collagen-induced platelet aggregation. Whereas, hexane and EtOAc layers potently inhibited the collagen (3 ${\mu}g/mL$)-induced platelet aggregation with the $IC_{50}$ values of 10.9${\pm}$1.0 and 31.5${\pm}$0.8 ${\mu}g/mL$, respectively. Paeonol isolated from the hexane-acetone layer specifically inhibited the collagen-induced platelet aggregation with the $IC_{50}$ value of 113.1 ${\pm}$ 0.9 ${\mu}M$, whereas it had little effects on the other agonists such as AA-, thrombin-, A23187- and thapsigargin-induced platelet aggregations. Paeonol also potently inhibited the collagen-induced TXB formation in rabbit platelet in a concentration-dependent manner. These results suggest that paeonol may inhibit rabbit platelet aggregation by interfering with an essential step in collagen-induced platelet activation and $TXA_2$ formation. Paeonol may be a promising candidate for an antiplatelet agent.

Efficient RF Energy Harvesting Algorithm based on Frequency Selective Fading Map (주파수 선택적 페이딩 맵 기반 효율적 무선 에너지 하비스팅 알고리즘)

  • Park, Ji Ho;Hwang, Yu Min;Song, Yu Chan;Kim, Jin Young
    • Journal of Satellite, Information and Communications
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    • v.10 no.2
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    • pp.24-29
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    • 2015
  • Recently, with developments of various networks, devices and various services, energy efficiency has become one of the most crucial issues with respect to sustainability of mobile devices. For connecting to networks seamlessly to offer services, a scenario of RF energy harvesting which supplies energy to wireless devices with RF signals is assumed. To increase the efficiency of RF energy harvesting, this paper proposes a RF energy harvesting algorithm which is based upon a frequency selective fading map. Through the algorithm, a receiver of mobile device can get fading information at each frequency and select a frequency which has the best quality. At the end, the simulation result demonstrates its superiority by showing a 4.45dB improvement in comparison to a deep fading frequency point.

Performance of Interference Mitigation using Optical Relay and Optical Beamforming in Visible Light Communication Systems (가시광 통신 시스템에서 Optical Relay와 Optical Beamforming을 통한 간섭 완화 성능)

  • Hwang, Yu Min;Kim, Yoon Hyun;Kim, Jin Young
    • Journal of Satellite, Information and Communications
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    • v.7 no.3
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    • pp.63-68
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    • 2012
  • The VLC (visible light communication) system is communication technology using visible rays (RGB) that come out in LED device. It is energy curtailment effect and possible in ubiquitous network service applications. Also, VLC system has the above advantage about that the communication throughout the whole room is enabled by high power lighting and lighting equipment with white colored LED which are easy to install and have good outward appearance. However, the signal detection performance for the receiver near the network of transmitter boundary is severely degraded and the transmission efficiency decreased due to the influence of the interference signal from the adjacent networks. In this paper, we propose an interference mitigation method with optical relay and optical beamforming scheme in VLC systems, and evaluate the reception performance. For the system BER, the proposed system demonstrates the performance enhancement compared to the not using the optical relay and optical beamforming scheme, and SNR performance gain and higher channel capacity is achieved.