• Title/Summary/Keyword: Compound-127

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Anti-tumor effect of new compound, 127, through the induction of apoptosis (새로운 화합물 c-127의 세포고사 유도에 의한 항암효과)

  • Baek, Ki Hwan;Han, A Lum;Shin, Sae Ron;Jin, Chun Mae;Yoon, Young Wook;Yu, Seung Taek;Kim, Jong Duk;Choi, Du Young
    • Clinical and Experimental Pediatrics
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    • v.52 no.6
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    • pp.696-700
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    • 2009
  • Purpose : We screened more than 350 compounds with an endoperoxide ring structure in search of an anti-leukemic drug and found that compound 127 (c-127) could induce significant cytotoxicity in HL-60 cells. In this study, we investigated the molecular mechanisms of compound 127-induced antitumor activity on HL-60 cells. Methods : HL-60 cells were cultured in Rosewell Park Memorial Institute 1640 and cell viability was measured by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide], a tetrazole assay. Apoptosis was assessed by a DNA fragmentation test. Apoptotic machineries were determined by Western blot analysis. Results : C-127 could induce a cytotoxic effect at 24 h and apoptosis at 6 h, which was demonstrated with MTT assay and DNA fragmentation test, respectively. The apoptotic effect of this drug was caused by the activation of the intracellular caspase-8,3 activation, the cleavage of pro-apoptotic Bid, and the increase of c-Jun expression accompanied with JNK (Jun N-terminal kinases) phosphorylation. On the contrary, it increased the expression of anti-apoptotic Bcl-2 levels, leading to the induction of the induction of anti-apoptotic effect. Taken together, the present study demonstrated that c-127 was a potent inducer of cytotoxicity on HL-60 cells through apoptotic mechanisms, which included the activation of caspase family, the regulation of Bcl-2 family, and the activation of JNK signaling pathway. Conclusion : Our results suggest that c-127 has a strong antitumor activity through the regulation of various apoptotic machineries on HL-60 cells. The compound may be utilized as an effective and potentially therapeutic drug in leukemia.

Compound-A inhibited the Asthmatic Responses in the Conscious Guinea Pigs

  • Lee, Ji-Yun;Lee, Jin-Hee;Kim, Youn-Joung;Sim, Sang-Soo;Kim, Chang-Jong
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.127.1-127.1
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    • 2003
  • Effect of Compound-A, a phenylpropanoid isolated from Arctium lappa fruit, on the early- (EAR) and late-phase asthmatic responses (LAR) of guinea pigs were studied in vivo. Guinea pigs were sensitized by injection of 100 mg of ovalbumin (OA). Twenty-one days after sensitization, animals were challenged with exposure to aerosolized 1 % OA for five minutes in double-chambered plethysmograph box with jet nubulizer. Immediately and twenty-four hours after challenge, EAR and LAR ashmatic responses were determined the tidal volume (TV), respiration rate (RR) and specific airway resistance (sRaw), and then animals anethetized and taken the bronchoalveolar lavage fluid (BALF) by lavage the lung with HEPES buffer through cannulation into trachea. (omitted)

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Study on antioxidant and anti-inflammatory activity of compound K extract produced by Saccharomyces servazzii(GB-07) strain derived from traditional soy (전통장류 유래 GB-07균주에 의해 생산된 Compound K 함유 발효인삼의 항산화 및 항염증 활성 연구)

  • Shin, Dong-Gue;Seo, Jeong-Hun;Cho, Shang-Min;Choi, Hak-Joo
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.9
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    • pp.127-135
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    • 2017
  • Ginseng, whichhas long been used for its medicinal properties, has recently been investigated by scientific research to identify its components and evaluate its efficacy. Recently, two components of ginseng, Rg3 and compound K, have been attracting attention and various functional materials containing these materials have been developed and investigated. In this study, compound K wasproduced using yeast (Saccharomyces servazzii, GB-07) and To be used for industrialization. The antioxidant and anti-inflammatory activity of compound K (containing 20 g/g) ginseng fermented extract was investigated. In the fermented ginseng extract, the free radical DPPH was scavenged in a concentration-dependent manner and the production of ROS was inhibited in macrophages(RAW 264.7 cell). Moreover, the LPS-induced inflammatory cytokines $IL-1{\beta}$, IL-6 and $TNF-{\alpha}$ were suppressed. These results suggest the possibility of industrialization viathe development of products containing compound K through future process development and various efficacy tests.

INTERFACIAL REACTIONS BETWEEN SN-58MASS%BI EUTECTIC SOLDER AND (CU, ELECTROLESS NI-P/CU)SUBSTRATE

  • Yoon, Jeong-Won;Lee, hang-Bae;Park, Guang-Jin;Shin, Young-Eui;Jung, Seung-Boo
    • Proceedings of the KWS Conference
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    • 2002.10a
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    • pp.487-492
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    • 2002
  • The growth kinetics of intermetallic compound layers formed between eutectic Sn-58Bi solder and (Cu, electroless Ni-P/Cu) substrate were investigated at temperature between 70 and 120 C for 1 to 60 days. The layer growth of intermetallic compound in the couple of the Sn-58Bi/Cu and Sn-58Bi/electroless Ni-P system satisfied the parabolic law at given temperature range. As a whole, because the values of time exponent (n) have approximately 0.5, the layer growth of the intermetallic compound was mainly controlled by volume diffusion over the temperature range studied. The apparent activation energies of Cu$_{6}$Sn$_{5}$ and Ni$_3$Sn$_4$ intermetallic compound in the couple of the Sn-58Bi/Cu and Sn-58Bi/electroless Ni-P were 127.9 and 81.6 kJ/mol, respectively.ely.

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Suppression of Anaphylactic Reaction in Murine by Siegesbeckia pubescens

  • Kim, Hyung-Min;Kim, Chang-Young;Kwon, Mun-Hyun;Shin, Tae-Yong;Lee, Eon-Jeong
    • Archives of Pharmacal Research
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    • v.20 no.2
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    • pp.122-127
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    • 1997
  • The aqueous extract of Siegesbeckia pubescens (SPAE) inhibited compound 48/80-induced systemic anaphylaxis 100% with the dose of 1.0, 0.5 mg/g body weight (BW) at 1 h before or 5 min, 10 min after intraperitoneal injection of compound 48/80. The passive cutaneous anaphylaxis (PCA) reaction also inhibited to 78.5% by oral administration of SPAE(1.0 mg/g BW). When SPAE pretreated on mice at concentrations ranging from 0.0001 to 1.0 mg/g BW, the serum histamine levels were reduced in a dose-dependent manner. Moreover, SPAE ($100-800{\mu}g/ml) dose-dependently inhibited the histamine release from peritoneal mast cells (RPMC) by compound 48/80 $(5{\mu}g/ml)$. Analysis by microscopic appearance observation revealed that SPAE $(500{\mu}g/ml) stabilized the RPMC membrane. Therefore, these findings indicate that SPAE inhibits anaphylactic reactions through stabilization of mast cell membrane.

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The Relative Importance of Indoor and Outdoor Sources for Determining Indoor Pollution Concentrations in Homes in Seoul, South Korea

  • Lee, Jae Young;Kim, Kyunghwan;Ryu, Sung Hee;Kim, Chang Hyeok;Bae, Gwi-Nam
    • Asian Journal of Atmospheric Environment
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    • v.12 no.2
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    • pp.127-138
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    • 2018
  • This study measured indoor and outdoor levels of hydrocarbon volatile organic compounds (VOCs), such as benzene, toluene, ethylbenzene, and xylene isomers (collectively referred to as BTEX), as well as 13 carbonyl compounds, at 20 homes in Seoul, South Korea. Along with the sampling of BTEX and carbonyls, indoor concentrations of the air pollutants nitrogen oxide (NO) and carbon dioxide ($CO_2$) were also measured at each home. These measurements were used to understand the characteristics of BTEX and carbonyls by calculating the various ratios and correlation coefficients between measured contaminant levels. We found that carbonyls were mostly originated from indoor sources, while BTEX were originated from both indoor and outdoor sources. A high correlation between indoor levels of NO and BTEX indicated that traffic emissions were also an important sources of BTEX.

Studies on the Nutritional Physiology of Soybean 6. Variatio of Potassium at the Various Position of Leaf on the Main Stem (대두의 영양생리학적 연구 6. 엽위별 가리의 변이)

  • 이순희
    • Journal of Plant Biology
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    • v.17 no.3
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    • pp.127-136
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    • 1974
  • The effect of potassium metabolism on the soybean leaves was studied with comparison of other elements during the successive growing period. The results were as follows; 1. The percentage of potassium content showed remarkable increase not only in the first compound leaf at a stage which was growing vigorously and producing new leaves, but also in the fifth compound leaf at a stage which was taking a active metabolism of nitrogen and carbohydrate but not producing new leaves. However, the percentage of potassium content was decreased in the second compound leaf than in the first one. Such a result could be regarded as a potassium removal from mature leaves into immature and flowing out from stoma through respiration. During the pod-development the percentage of potassium content in the soybean leaf was decreased. 2. If nitrogen, phosphorus and potassium were added excessively in the nutrient solution, the percentage of potassium content in the soybean leaf had increased. The effects of these elements showed a remakable increase in the excessive plot of nitrogen than in that of phosphorus. At early stage the redtarded effect of phosphorus on the growth of soybean could be covered by potassium, however, at late stage it could not. The growth of soybean plant was much more inhibited by potassium, compared with nitrogen and phosphorus. New leaves could not be produced in the potassium deficient soybean plant after the third compound leaf. The normal growth of soybean plant could not be observed if only one element was excessively added to the culture solution, compared with the deficiency of other two elements.

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Computational Study on Spirocyclic Compounds as Energetic Materials (I)

  • Seok, Won K.
    • Bulletin of the Korean Chemical Society
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    • v.35 no.4
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    • pp.989-993
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    • 2014
  • The molecular structures of 2,6-diaza-1,3,5,7-tetraoxaspiro[3,3]heptane (1) and its dinitro derivative, 2,6-dinitro-2,6-diaza-1,3,5,7-tetraoxaspiro[3,3]heptane (2), were fully optimized without symmetry constraints at $HF/6-31G^*$ level of theory. A bisected conformation with respect to the ring is preferred with a $C_2$ symmetric structure. The density of each molecule in the crystalline state was estimated to 1.12 and 2.36 $g/cm^3$ using PM3/VSTO-3G calculations from the molecular volume. The heat of formation was calculated for two compounds at the CBS-4M level of theory. The detonation parameters were computed using the EXPLO5 software: D = 6282 m/s, $P_{C-J}$ = 127 kbar for compound 1, D = 7871 m/s, $P_{C-J}$ = 307 kbar for compound 2, and D = 6975 m/s, $P_{C-J}$ = 170 kbar for 60% compound 2 with 40% TNT. Specific impulse of compound 1 in aluminized formulation when used as monopropellants was very similar to that of the conventional ammonium perchlorate in the same formulation of aluminum.

Environment for Translation Domain Adaptation and Continuous Improvement of English-Korean Machine Translation System

  • Kim, Sung-Dong;Kim, Namyun
    • International Journal of Internet, Broadcasting and Communication
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    • v.12 no.2
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    • pp.127-136
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    • 2020
  • This paper presents an environment for rule-based English-Korean machine translation system, which supports the translation domain adaptation and the continuous translation quality improvement. For the purposes, corpus is essential, from which necessary information for translation will be acquired. The environment consists of a corpus construction part and a translation knowledge extraction part. The corpus construction part crawls news articles from some newspaper sites. The extraction part builds the translation knowledge such as newly-created words, compound words, collocation information, distributional word representations, and so on. For the translation domain adaption, the corpus for the domain should be built and the translation knowledge should be constructed from the corpus. For the continuous improvement, corpus needs to be continuously expanded and the translation knowledge should be enhanced from the expanded corpus. The proposed web-based environment is expected to facilitate the tasks of domain adaptation and translation system improvement.

Design and Synthesis of New 4-Alkylthio Monocyclic β-Lactams

  • Lee, Sang Hyup
    • Bulletin of the Korean Chemical Society
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    • v.34 no.1
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    • pp.121-127
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    • 2013
  • New types of monocyclic ${\beta}$-lactams constitute an important class of compounds due to their unique structures and natures. Here, the design and synthesis of new 4-alkylthio monocyclic ${\beta}$-lactams 2a and 3a are reported. Significantly, compounds 2a and 3a, while keeping a monocyclic system, were designed to contain all of the substructures provided by the cleavage of C(2)-C(3) bond in penicillins. Efficient synthetic pathways for compounds 2a and 3a were established based on two different strategies. Compound 2a was synthesized from raw materials, using 4-acetoxyazetidin-2-one as a key intermediate, through a ten-step synthetic sequence in 3% overall yield. Compound 3a was synthesized from potassium salt of penicillin G (17), using the degraded product 20 as a key intermediate, through a six-step synthetic sequence in 11% overall yield. 4-Alkylthioazetidin-2-one derivatives, introduced in this study, could serve as valuable intermediates for the development of new monocyclic ${\beta}$-lactams.