• Title/Summary/Keyword: GP5

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Various Partial Charge Schemes on 3D-QSAR Models for P-gp Inhibiting Adamantyl Derivatives

  • Gadhe, Changdev G.;Madhavan, Thirumurthy;Kothandan, Gugan;Lee, Tae-Bum;Lee, Kyeong;Cho, Seung-Joo
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1604-1612
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    • 2011
  • We developed three-dimensional quantitative structure activity relationship (3D-QASR) models for 17 adamantyl derivatives as P-glycoprotein (P-gp) inhibitors. Eighteen different partial charge calculation methods were tested to check the feasibility of the 3D-QSAR models. Best predictive comparative molecular field analysis (CoMFA) model was obtained with the Austin Model 1-Bond Charge Correction (AM1-BCC) atomic charge. The 3D-QSAR models were derived with CoMFA and comparative molecular similarity indices analysis (CoMSIA). The final CoMFA model ($q^2$ = 0.764, $r^2$ = 0.988) was calculated with an AM1-BCC charge and electrostatic parameter, whereas the CoMSIA model ($q^2$ = 0.655, $r^2$ = 0.964) was derived with an AM1-BCC charge and combined steric, electrostatic, hydrophobic and HB-acceptor parameters. Leave-five-out (LFO) cross-validation was also performed, which yielded good correlation coefficient for both CoMFA (0.801) and CoMSIA (0.656) models. Robustness of the developed models was checked further with 1000 run bootstrapping analyses, which gave an acceptable correlation coefficient for CoMFA (BS-$r^2$ = 0.997, BS-SD = 0.003) and CoMSIA (BS-$r^2$ = 0.996, BS-SD = 0.018).

Reversion of Multidrug Resistance by SKI-II in SGC7901/DDP Cells and Exploration of Underlying Mechanisms

  • Zhu, Zu-An;Zhu, Zheng-Qiu;Cai, Hong-Xing;Liu, Ying
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.2
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    • pp.625-631
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    • 2012
  • In order to investigate whether SKI-II could reverse drug resistance and its possible mechanisms, we treated SGC7901/DDP cells with SKI-II or SKI-II in combination with DDP. Then cell growth, apoptosis, micromorphological changes, and expression of SphK1, P-gp, NF-${\kappa}B$, Bcl-2 and Bax were assessed by MTT assay, flow cytometry, electron microscopy, immunocytochemistry and Western blot assay respectively. SGC7901/DDP cells were insensitive to cisplatin 2.5mg/L, but when pretreated with SKI-II, their proliferation was inhibited by cisplatin 2.5mg/L significantly, the inhibition rate increasing with time and dose. The apoptosis rate was also significantly elevated. Expression of SphK1 and P-gp was decreased significantly, Pearson correlation analysis showing significant correlation between the two (r=0.595, P<0.01). Expression of NF-${\kappa}B$ and Bcl-2 was decreased significantly,while that of Bax was increased, compared to the control group. There were significant correlations between SphK1 and NF-${\kappa}B$(r=0.723, P<0.01), NF-${\kappa}B$ and Bcl-2(r=0.768, P<0.01). All these data indicated that SKI-II could reverse drug resistance of SGC7901/DDP to cisplatin by down-regulating expression of P-gp and up-regulating apoptosis through down-regulation of SphK1. The increased apoptotic sensitivity of SGC7901/DDP to cisplatin was due to the decreasing proportion of Bcl-2/Bax via down-regulating NF-${\kappa}B$.

Application of CCD Image by Direct Georeferencing (Direct Georeferencing에 의한 CCD 영상의 적용기법)

  • Song Youn Kyung;Park Woon Yong;Park Hong Gi
    • Journal of the Korean Society of Surveying, Geodesy, Photogrammetry and Cartography
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    • v.23 no.1
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    • pp.77-88
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    • 2005
  • Direct Georeferencing (DG) is based on the direct measurement of the projection centers and rotation angle of sensor through loading the GPS and INS in aircraft. The methods can offer us to acquire the exterior orientation parameters with only minimum GCPs, even the ground control process could be completely skipped. In this study, a CCD camera is simultaneously used in GPS/INS, and acquired CCD image through Direct Georeferencing produce digital orthoimage. In this process, methods of combining sensor and digital orthoimage are examined and estimated. For the comparison of the positioning accuracy digital orthoimage through Direct Georeferencing, GCPs determined by GPS surveying are used. Two digital orthoimage are produced; one with a few GCP and the other without them. The produced maps can be used to correct or revised 1:1,000 or 1:5,000 scale maps accordingly.

방사선(放射線) 조사후(照射後)의 N:GP(S) mouse 비장세포(脾臟細胞) 증식(增殖)에 미치는 보중익기탕(補中益氣湯)과 사육탕(四六湯)의 효과

  • Lee, Neung-Gi;Choe, Seung-Hun
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.2 no.1
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    • pp.91-100
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    • 1996
  • Radiotherapy is an irreplaceable method of cancer treatment but, it has various side effects, especially damage to the hemopoietic system. A lot of radioprotectors have been found but they also have toxic effects. Many kinds of crude drugs(Oriental Chinese medicine)with low toxicity have been reported to promote the recovery from radiation damage. Recently, the trial to combine radiotherapy with herbal treatment of cancer patients shows a desirable result, an enhancement in recovery of the blood system.. This study was performed to determine whether prescriptions to support the healthy energy and strengthen the body resistence, Buzhongyiqi-tang and Siliu-tang, promote the recovery of splenocytes of N:GP(s) mice from radiation damage. We investigated the proliferative effect of Buzhongyiqi-tang, Siliu-tang and EIB(ethanol insoluble fraction of Buzhongyiqi-tang) on N:GP(S)mice splenocytes before or after ${\gamma}$-irradiation. We also investigated the morphology of splenocytes cultured with these herbs. Buzhongyiqi-tang and Siliu-tang promoted the proliferation of splenocytes in a concentration of 0.1 mg/ml compared with normal control(p<0.001). After 1-5Gy of ${\gamma}$-irradiation they also showed the effect of recovery of hemopoietic cells, especially in Buzhongyiqi-tang(4Gy:p<0.005; 5Gy:p<0.05). In addition, EIB(ethanol insoluble fraction of Buzhongyiqi-tang) showed the highest proliferative effect of all agents suggesting that more effective fractions could be found from crude herbs or prescriptions. These results suggest that it is possible to make use of Buzhongyiqi-tang, Siliu-tang or EIB as radio-protective agents.

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Spectral Irradiance and Underwater Transmission Characteristics of a Combined High-Luminance Light-Emitting Diodes as the Light Source for Fishing Lamps (복수 조합에 의한 고휘도 발광 다이오드의 분광분포와 수중투과특성)

  • Choi, Sok-Jin
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.42 no.6
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    • pp.703-710
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    • 2009
  • The spectral irradiance and underwater transmission characteristics of a combined high-luminance light-emitting diode (LED) lights have been studied to evaluate suitable light sources for fishing lamps of the next generation. The wavelengths at which the irradiance was maximum were changed from 473, 501, 525, and 465 nm for blue, peacock blue, green, and white LED light to 475, 504 and 528 nm for [$F_{WB}$], [$F_{PB}$] and [$F_{GB}$] combined LED lights, respectively. If the irradiance characteristics at 400-700 nm wavelengths are set as 100%, the irradiance rates at 450-499 nm and 500-549 nm were decreased from 82.4% and 56% for blue, peacock blue LED light to 60.0%, 38.5% for [$F_{WB}$], [$F_{WP}$] combined LED lights. The underwater transmission characteristics of the combined LED lights were superior in the order [$F_{WB}$], [$F_{BP}$], [$F_{GB}$] in optical water type I; [$F_{WB}$], [$F_{PB}$], [$F_{GP}$] in optical water type II-III; and [$F_{GP}$], [$F_{WP}$], [$F_{PB}$] in optical water type 1. Setting the 10m depth underwater transmission characteristics of the combined LED lights in optical water type I at 100%, the transmission of water types II, III and 1 drops to 29.5%, 8.0% and 2.2%. Based on the distribution of spectral irradiance and underwater transmission characteristics calculated in optical water types II-III, where was the jigging ground for fishing lamps, the [$F_{WB}]$ and [$F_{GP}$] combined LED lights can be used as a suitable light sources for fishing lamps of the next generation.

Effects of Two Herbal Extracts and Virginiamycin Supplementation on Growth Performance, Intestinal Microflora Population and Fatty Acid Composition in Broiler Chickens

  • Ramiah, Suriya Kumari;Zulkifli, Idrus;Rahim, Nordiana Asyikin Abdul;Ebrahimi, Mahdi;Meng, Goh Yong
    • Asian-Australasian Journal of Animal Sciences
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    • v.27 no.3
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    • pp.375-382
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    • 2014
  • The competency of garlic and pennywort to improve broiler chicken growth and influence intestinal microbial communities and fatty acid composition of breast meat were studied. Two hundred forty, "day-old" chicks were randomly allocated to 4 treatment groups consisting of 6 replications of 10 chicks in each pen. The groups were assigned to receive treatment diets as follows: i) basal diet (control), ii) basal diet plus 0.5% garlic powder (GP), iii) basal diet plus 0.5% pennywort powder (PW) and iv) 0.002% virginiamycin (VM). Birds were killed at day 42 and intestinal samples were collected to assess for Lactobacillus and Escherichia coli. The pectoralis profundus from chicken breast samples was obtained from 10 birds from each treatment group on day 42 and frozen at $-20^{\circ}C$ for further analyses. Fatty acid profile of breast muscles was determined using gas liquid chromatography. Feed intake and weight gain of broilers fed with GP, PW, and VM were significantly higher (p<0.05) compared to control. Feeding chicks GP, PW, and VM significantly reduced Escherichia coli count (p<0.05) while Lactobacillus spp count were significantly higher (p<0.05) in the gut when compared to control group on day 42. Supplemented diet containing pennywort increased the C18:3n-3 fatty acid composition of chickens' breast muscle. Garlic and pennywort may be useful in modulating broiler guts as they control the enteropathogens that help to utilize feed efficiently. This subsequently enhances the growth performances of broiler chickens.

A Rapid Preconcentration Method Using Modified GP-MSE for Sensitive Determination of Trace Semivolatile Organic Pollutants in the Gas Phase of Ambient Air

  • He, Miao;Xu, Qingjuan;Yang, Cui;Piao, Xiangfan;Kannan, Narayanan;Li, Donghao
    • Bulletin of the Korean Chemical Society
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    • v.35 no.10
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    • pp.2995-3000
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    • 2014
  • A sensitive concentration method utilising modified gas-purge microsyringe extraction (GP-MSE) was developed. Concentration (reduction in volume) to a microlitre volume was achieved. PAHs were utilised as semivolatile analytes to optimise the various parameters that affect the concentration efficiency. The injection rate and temperature were the key factors that affected the concentration efficiency. An efficient concentration (75.0-96.1%) of PAHs was obtained under the optimised conditions. The method exhibited good reproducibility (RSD values that ranged from 1.5 to 9.0%). The GP-MSE concentration method enhances the volume reduction (concentration factor), leading to a low method detection limit ($0.5-15ngL^{-1}$). Furthermore, this method offers the advantage of small-volume sampling, enabling even the detection of diurnal hourly changes in the concentration of PAHs in ambient air. Utilising this method in combination with GC-MS, the diurnal hourly flux of PAHs from the gas phase of ambient air was measured. Indeed, the proposed technique is a simple, fast, low-cost and environmentally friendly.

3D modelling shape embodiment and efficiency analysis of reservoir that using RTK-GPS and E/S (RTK-GPS와 E/S를 이용한 저수지의 3D 모델링 형상 구현과 효율성 분석)

  • 김용석;박운용;홍순헌;박창하
    • Proceedings of the Korean Society of Surveying, Geodesy, Photogrammetry, and Cartography Conference
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    • 2004.04a
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    • pp.151-156
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    • 2004
  • 현재 전국에 산재해 있는 많은 소규모의 저수지들은 현재까지 관리 상태나 실지 내용적에 대한 정확한 자료가 모두 구비되어있지 못한 실정이다. 본 연구에서는 행정구역상 저수지가 많이 분포되어있는 영남권의 경주시 73개 소규모 저수지 가운데 23개소를 선정하여 실험을 하였다. RKT-GPS를 이용하여 5초마다 데이터를 취득하였고, E/S를 이용하여 1초 간격으로 수심에 대한 값과 TS를 이용하여 현황 측량을 실시하였다. 이렇게 취득된 자료를 가지고 3D 모델링을 하여본 결과 15개소(약 65%)의 저수지가 양호한 상태였음을 알 수 있었고, 과거자료와의 비교ㆍ분석을 통하여 현재 저수지 상태에 대한 정확한 내용적을 알 수 있었다. 또한 23개소 저수지의 만수면적과 유효저수량을 분석한 결과 만수면적은 20.63%, 유효저수량은 3.34 %만큼 줄어들었음을 알 수 있었다. 이를 통하여 현재 저수지 상태에 대한 분석과 관리 방향에 대한 방법에 대하여 기여하고자 한다.

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Precision Analysis of Fixing Methods Use in the GPS Continuous Station (GPS 상시관측소 활용에 있어 고정방법이 절대위치에 미치는 정밀도 분석)

  • 정영동;강상구;박보연
    • Proceedings of the Korean Association of Geographic Inforamtion Studies Conference
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    • 2003.04a
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    • pp.88-93
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    • 2003
  • 국토공간정보의 기반인 수치지도 제작을 위해서는 위치에 대한 정확한 정보가 요구되며 이러한 정보는 GPS를 이용한 방법이 대표시 되고 있다. 우리나라도 GPS를 이용한 위치결정 방법의 효율성과 정확성을 확보하기 위해 전 국토에 걸쳐 24시간 위성데이터를 취득할 수 있는 70여개의 GPS 상시관측소를 설치 운영하고 있다. 따라서 본 연구는 GPS 상시관측소 데이터의 효과적인 활용 방안을 모색하기 위해 행정자치부와 국리지리원에서 설치 운영하며 호남권에 위치한 5곳의 상시관측소를 대상으로 각기 고정위치를 달리하여 기선해석과 망조정을 수행하여 고정위치에 따른 3차원 절대좌표의 정밀도를 분석하였다. 현재 행정자치부의 3곳의 상시관측소 절대위치는 고시되지 않아 국립지리원 고시 성과를 기준으로 고시성과와 계산성과의 3차원 절대 좌표를 비교하였다.

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Design of a Rule Based Controller using Genetic Programming and Its Application to Fuzzy Logic Controller (유전 프로그래밍을 이용한 규칙 기반 제어기의 설계와 퍼지로직 제어기로의 응용)

  • 정일권;이주장
    • Journal of Institute of Control, Robotics and Systems
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    • v.4 no.5
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    • pp.624-629
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    • 1998
  • Evolutionary computation techniques can solve search problems using simulated evolution based on the ‘survival of the fittest’. Recently, the genetic programming (GP) which evolves computer programs using the genetic algorithm was introduced. In this paper, the genetic programming technique is used in order to design a rule based controller consisting of condition-action rules for an unknown system. No a priori knowledge about the structure of the controller is needed. Representation of a solution, functions and terminals in GP are analyzed, and a method of constructing a fuzzy logic controller using the obtained rule based controller is described. A simulation example using a nonlinear system shows the validity and efficiency of the proposed method.

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