• Title/Summary/Keyword: TOPO

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Binding Mode Studies of Indenoisoquinoline Analogues into Human Topoisomerase I-DNA Complex Using Flexible Docking (Human Topoisomerase I-DNA 절개가능 복합체에 대한 Indenoisoquinoline 유도체들의 결합양상 연구)

  • Park, In-Seon;Kim, Bo-Yeon;Kim, Choon-Mi;Choi, Sun
    • YAKHAK HOEJI
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    • v.53 no.4
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    • pp.228-234
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    • 2009
  • Topoisomerase I (Topo I) participates in the DNA replication, transcription, and repair. Binding of Topo I inhibitor to the Topo I-DNA cleavage complex forms stabilized ternary complex which blocks DNA religation and ultimately causes cell death. Camptothecin (CPT) and its derivatives have been among the most effective anticancer drugs by inhibition of topo I. However, efforts to synthesize non-CPT drugs have been actively going on because the CPT derivatives have several limitations such as poor solubility, short half-life, and side effects. As an indenoisoquinoline, NSC314622 is not as potent as CPT, but its chemical stability and slower reversibility of the cleavage complex made it a good lead compound. Recently, a series of indenoisoquinoline analogues were synthesized with substituted dimethoxy or methylenedioxy on the aromatic ring and alkylamino on the lactam nitrogen. Some of them showed quite good Topo I inhibitory activity. Using the computer docking program, Surflex-Dock, indenoisoquinoline analogues were docked into the human Topo I-DNA cleavable complex. The docking results showed that the compounds with activity better than NSC314622 intercalated between the -1 and +1 base pairs at the cleavage site, but those with little or no activities did not appear to intercalate. These results could be useful to design new Topo I inhibitors improved than CPT.

Determination of Tb(III) in aqueous solution by fluorescence spectrometry (형광분광법에 의한 수용액 중의 Tb(III) 정량)

  • Lee, Sang Hak;Bae, Zun Ung;Chung, Hae Young;Choi, Sang Seob
    • Analytical Science and Technology
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    • v.10 no.4
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    • pp.274-281
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    • 1997
  • Methods to determine terbium(III) ion in aqueous solution by measuring the enhanced fluorescence intensity of terbium(III)-terephthalic acid(TPA) complex ion have been studied. The optimum analytical conditions for pH, excitation wavelength and concentration of TPA were found to be 6.0, 260nm and $4.0{\times}10^{-4}M$, respectively. The fluorescence intensity of the terbium(III) complex ion was further increased with addition of trioctylphosphine oxide (TOPO). In this case Triton X-100 was used to dissolve TOPO in aqueous solution. When TOPO was used, the optimum analytical conditions for pH, excitation wavelength, and concentrations of TPA, TOPO and Triton X-100 were found to be 4.5, 285nm. $4.0{\times}10^{-4}M$, $5.0{\times}10^{-5}M$, and 0.05%, respectively. Under the optimum experimental conditions, calibration curve for Tb(III) was linear over the range from $4.0{\times}10^{-8}M$ to $4.0{\times}10^{-5}M$ and the detection limit was $4.0{\times}10^{-8}M$. When TOPO was used, the concentration range of linear response, and the detection limit were $4.0{\times}10^{-9}M$ to $2.0{\times}10^{-6}M$, and $4.0{\times}10^{-9}M$, respectively. Effects of interferences from various cations for the determination of terbium(III) ion were also investigated.

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The activity - binding affinity relationship of topoisomerase I inhibitors by flexible docking with FlexiDock

  • Kim, Ji-Hyun;Park, In-Hee;Kim, Choon-Mi
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.159.1-159.1
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    • 2003
  • Human Topoisomerase I (topo I) helps the control of DNA supercoiling in cells by assisting breaking and religation of DNA strand. It is essential for cellular metabolism and survival, hence, a good target for a novel class of anticancer drugs. As topo I inhibitor binds to the DNA-topo I complex, the religation of DNA strand is suppressed which results in the death of the target cell. Seven compounds of H-Imidazo[4, 5-g]phthalazing-4, 9-dione derivatives with $IC_50$ in the range of 0.001 and 6.27 $\mu$M in 5 different cancer cells and four compounds of 7-chloro-6-quinazoline-5, 8-dione derivatives with positive and negative topo I inhibition activities were studied. (omitted)

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Solvent Extraction of Lithium Ion in Aqueous Solution Using TTA and TOPO (TTA와 TOPO를 이용한 수용액 중의 리튬이온 용매추출)

  • Lee, Jeon-Kyu;Jeong, Sang-Gu;Koo, Su-Jin;Kim, Si-Young;Ju, Chang-Sik
    • Korean Chemical Engineering Research
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    • v.51 no.1
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    • pp.53-57
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    • 2013
  • For the purpose of development of the extraction process of lithium ion from concentrated water eliminated from desalination process, an experimental research on the solvent extraction of lithium ion from aqueous solutions was performed. The effects of operating parameters, such as concentration of extractant, ratio of extracting solution/aqueous solution, pH of aqueous solution, were examined. The effect of sodium chloride, the major component of sea water, was also examined. Lithium ion in aqueous solutions of pH=10.2~10.6 adjusted by ammonia solution was most effectively extracted by extracting solution composed of 0.02 M TTA and 0.04 M TOPO in kerosine. The addition of sodium chloride in lithium aqueous solution significantly interfered the extraction of lithium ion.

Determination of Eu(III) by Fluorescence Spectrometry (형광분광법에 의한 Eu(Ⅲ)의 정량)

  • Lee, Sang Hak;Han, Jong Hwan;Choi, Sang Seob
    • Journal of the Korean Chemical Society
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    • v.42 no.3
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    • pp.285-291
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    • 1998
  • Methods to determine EU(Ⅲ) ion in aqueous solution by fluorescence spectrometry based upon the ligand sensitized fluorescence of Eu(Ⅲ)-terephthalic acid (TPA) complex ion have been studied. The effects of excitation wavelength, pH, concentration of TPA and emission wavelength on the fluorescence intensity were investigated. The fluorescence intensity of the Eu(Ⅲ) complex ion was further increased with addition of trioctylphosphine oxide (TOPO). In this case Triton X-100 was used to dissolve TOPO in aqueous solution. The calibration curve for Eu(Ⅲ) was linear over the range from $1.0{\times}10^{-6}M\;to\;4.0{\times}10^{-4}M$ and the detection limit was $1.0{\times}10^{-6}M$ under the experimental conditions of 256 nm, 5.6, $3.5{\times}10^{-4}$M$ and 615 nm for excitation wavelength, pH, concentration of TPA and emission wavelength, respectively. When TOPO was added to the Eu(Ⅲ)-TPA system, the concentration range of linear response and the detection limit were $1.0 {\times}10^{-9}M\;to\;1.0{\times}10^{-4}M,\;1.0{\times}10^{-7}M,$ respectively under the experimental conditions of 284 nm, 4.4 and $1.0{\times} 10^{-4}M$ for excitation wavelength, pH and concentration of TOPO, respectively. Effects of interferences from various cations for the determination of Eu(Ⅲ) ion were also investigated.

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Biochemical Characterization of Adriamycin-Resistance in PC-14 Human Lung Adenocarcinoma Cell Line

  • Yi, Jae-Youn;Hong, Weon-Seon;Son, Young-Sook
    • BMB Reports
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    • v.34 no.1
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    • pp.66-72
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    • 2001
  • To investigate the mechanism of adriamycin (ADM) resistance in the ADM resistant subline PC-14/ADM, we examined the expressions of p-glycoprotein (P-gp), topoisomerase I (Topo I) and II (Topo II), glutathione-S-transferases (GSTs), tissue transglutaminase (t-TG), epidermal growth factor receptor (EGFR), and E-cadherin and the activity of superoxide dismutase (SOD) in PC-14 and PC-14/ADM cells. There was no change in the cellular levels of P-gp, Topo I, Topo II, and the two isoforms of GSTs. However, SOD activity in PC-14/ADM cells was 2.38 fold higher than that in PC-14 cells. A marked induction of the t-TG expression was also observed in PC-14/ADM cells. In addition to those changes, expressions of EGFR and E-cadherin were down regulated in PC-14/ADM cells. Therefore, molecular modifications such as an increase in SOD activity, induction of the t-TG expression, and down regulation of EGFR and E-cadherin expressions may play important roles in PC-14/ADM cells during the development of ADM resistance.

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Studies on Equilibria and Analytical Applications of Synergistic Solvent Extraction(II). Determination of Trace Lithium in Sea Water using TTA and TOPO

  • Kim, Yeong Sang;Choe, Jong Mun;Lee, Chi U
    • Bulletin of the Korean Chemical Society
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    • v.21 no.9
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    • pp.855-859
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    • 2000
  • An application of synergistic solvent extraction for the etermination of trace lithium in sea water has been studied by forming an adduct complex of thenoyltrifluoroacetone (TTA) and trioctylphosphine oxide (TOPO) in a solvent. The interference by major constituents in sea water was eliminated by phosphate precipitation. Ex-perimental conditions such as solution pH, concentrations of TTA and TOPO etc. were optimized in synthetic sea water with similar compositionto its natural counterpart. To eliminate the interference, 1.38g of ammoni-um dihydrogen phosphate and 2.5 mL of ammonia water were added into 100 mL of thediluted solution at $60^{\circ}C$ to form the phosphate precipitates of Ca2+ and Mg2+ ions. After the pH of this filtrate was adjusted to 8.0, 10.0 mL of m-xylene containing 0.1 M TTA and 0.05 M TOPO was added to the solution in a separatory funnel, and the solution was shaken vigorously for 20 minutes. The solvent was separated from the aqueous solution, and 20 uL of m-xylene solution was injected into a gaphite tube to measure the absorbance by GF-AAS. The detection limit was 0.42 ng/mL. Lithium was determined within the range of 146 to 221 ng/mLin Korean coast-al sea waters, and the recoveries in the spiked samples were 94 to 106%.

Thermal Curing Property of Silicone Encapsulant Containing Quantum Dot Surrounded by Various Types of Ligands

  • Lee, Chae Sung;Kim, BeomJong;Jeon, Seongun;Han, Cheul Jong;Hong, Sung-Kyu
    • Bulletin of the Korean Chemical Society
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    • v.34 no.12
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    • pp.3787-3789
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    • 2013
  • In this study, the silicone thermal curing degree of the silicone-encapsulated quantum dot light emission diode was measured using the various types of chemical ligands around quantum dot. It was confirmed that the trioctyl phosphin oxide (TOPO) ligand around the quantum dot was responsible for dispersion of the quantum dot in silicone encapsulant and decline of the thermal curing degree of the silicone encapsulant. Also, it was confirmed that the thermal curing degree of silicone encapsulants containing the steric acid (SA) and the dodecanoic acid (DA) ligands were higher than the one of TOPO ligand.

A Study on the Religious Costume in Korea - Buddhist and Taoist Costume - (한국(韓國) 종교복식(宗敎服飾)에 관(關)한 연구(硏究) - 불교(佛敎)와 도교복식(道敎服飾)을 중심(中心)으로 -)

  • Im, Yeong-Ja
    • Journal of the Korean Society of Costume
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    • v.14
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    • pp.63-73
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    • 1990
  • The thought of three religious, Confucianism, Buddhism, and Taoism, had been the mainaxis of Korean spirit of the past. This study is centered on Buddhist and Taoist costume. There have been a lot of studies on Korean costume from many viewpoints. However, there have been few approaches to the inner !"ide of it. That is to say, the research on spiritual back-ground or religious correlation has not done yet. And especially, we are wholly lacking the studies on Taoist costume. In this dissertation, I investigate how they had come to wear Buddhist costume and how it trans, on the basis of related documentary records and existing remains. I also inquiry Taoist costume which was worn at Taoist ceremony in our country, with the help of Korean books and documents and of the sources of Packwoonkwan in China. In the case of Topobyunjeung in Korean costume, in particular, we can catch the source of it only after studying the religious side of Taoist costume and Buddhist costume. As revealed in the theory of Topobyunjeung in Ojuyunmoonja-ngsango by Lee, Kyu Kyung, even old masters and great Confucianists could not know whether Topo, the ordinary clothes of the Sadaeboo, originated from Taoist costume or Buddhist costume. There have been many opinions about the origin, but even now it is true that no one has made it clear. Therefore in this dissertatio I demonstrate mainly how Topo and Hakchangeui appeared in Korean costume through Taoist costume. It is said that Taoists, Buddhists, and literary men wore Topo, Chickchul, and Chickshin in Song dynasty of China. Topo was a clerical robe of Taoists and was also an ordinary clothes. Chick-chul was a clerical robe of Buddhists, and Chick-shin was worn by Zen priests in Won dynaty. Over the Po, Buddhist wore a large robe, namely Kasa, and Taoist wore Packhakchang like Wooeui, when they attended at the religious ceremony. And they regarded such manner of dressing as ceremonial full-dress attire. The style of Topo in China was Saryunggyogeo. The is th say that they put the black Yeon along Sajoo, which are Young, Soogoo, Keum, and Keo, and that they wore Sajodae around their waists so as to let the band down in front of them. Our existing type of Topo is that of Chickryung-gyoin. The characteristics of the type are its Koreum hung on the dress, no Yeon along Sajoo, and Soopok at the back of the dress. And when they put on the dress, they wear Saejodae around their waists. These characteristics considered, we can find the source of Topo from the Po of Chickshin among Buddhist costume. Other types of Topo are those that were transformed elegantly according to our national manners and customs in our country. So-called Wooeui in Chiness Taoism is Hakchang. Originally it was made by weaving for of cranes or other feathered birds. Its remarkable feature is the wide sleeves. Later they called such a robe with wide sleeves Hakchang. Our hakchangeui has Yeon along Sajoo and a belt around waist. We can guess that the features of Topo and wide-sleeved Hakchang mingled and turned into Hakchangeui. Or it might also be that Topa worn by Taoist was regarded as Hakchang and Topa which has Yeon along Sajoo was regarded as Hakchangeui in our country. Such type of Hakchang worn by Taoists was well shown in the Buddhist and Taoist paintings among "The Pictures of Hills, Waters, and Folks" in the latter half of the 16th century. In China Hakchang with a belt around waist could not be seen. Comparing our style of Hakchangeui with the Chinese style, we can recognize the former was similar to that of Chinese Topa. From this, we gather that Topa was regarded as Hakchang, Wooeui worn by Taoists, Ascetics and True Men in Korea. Furthermore I also gather that our Hakchangeui, which has Tongjeong, Koreurn and a belt around waist, was a transformed style in our own country. From the above, we can realize that in costume the three religions, Confucianism, Buddhism, and Taoism, cannot be treated separately although they are different each other in the essential thought. We have to recognize that Korean Costume was established under the closely connected correlation among the religions and that it was transfigured and accepted according to the cultural characteristics. This study is significant in that it is the first attempt to understand Korean costume through the religous approach, which has never been made in our Korean costume studies. We are demanded even more wide and profound investigation on the religious side of costume throughout the general field of costume studies.

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Application of a Grid-Based Rainfall-Runoff Model Using SRTM DEM (SRTM DEM을 이용한 격자기반 강우-유출모의)

  • Jung, In-Kyun;Park, Jong-Yoon;Park, Min-Ji;Shin, Hyung-Jin;Jeong, Hyeon-Gyo;Kim, Seong-Joon
    • Journal of the Korean Association of Geographic Information Studies
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    • v.13 no.4
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    • pp.157-169
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    • 2010
  • In this study, the applicability of SRTM(The Shuttle Radar Topography Mission) DEM(Digital Elevation Model) which is one of the remotely sensed shuttle's radar digital elevation was tested for use as the input data in a grid-based rainfall-runoff model. The SRTM DEM and digital topographic map derived DEM(TOPO DEM) were building with 500m spatial resolution for the Chungju-Dam watershed which located in the middle east of South Korea, and stream-burning method was applied to delineate the proper flow direction for model application. Similar topographical characteristics were shown as a result of comparing elevation, flow-direction, hydrological slope, number of watershed cell, and profile between SRTM DEM and TOPO DEM. Two DEMs were tested by using a grid-based rainfall-runoff model named KIMSTORM with 6 storm events. The results also showed no significant differences in average values of relative error for both peak runoff(0.91 %) and total runoff volume(0.29 %). The results showed that the SRTM DEM has applicability like TOPO DEM for use in a grid-based rainfall-runoff modeling.