• Title/Summary/Keyword: non-polar

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Screening of ${\beta}$-Catenin/TCF Transcription Factor Inhibitors in Medicinal Herb Extracts

  • Choe, Ye-Dang;Na, Byung-Jo;Park, Se-Yeon
    • The Journal of Korean Medicine
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    • v.32 no.3
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    • pp.35-43
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    • 2011
  • Objectives: This study was performed to screen target-specific inhibitors of ${\beta}$-catenin/TCF signaling whose functional activation plays an important role in early events in carcinogenesis. Methods: To investigate the activation or suppression of ${\beta}$-catenin/TCF transcription, we established a transiently transfected cell line with a constitutively active ${\beta}$-catenin mutant gene whose product is not degraded. This cell line was also co-transfected with luciferase reporter gene constructs containing either an optimized (TOPflash) or mutant (FOPflash) TCF-binding element. We investigated cytotoxic effects using a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium salt (MTS) assay. To find effective inhibitors of ${\beta}$-catenin/TCF signaling from medicinal herbs, the crude extracts of 99 types of medicinal herbs were screened using a luciferase assay system in HEK-293 and SH-SY5y cells. Results: At a concentration of $50{\mu}g$/ml, extracts of Angelica koreanae radix, Cannabis sativa semen, Ephedrae intermedia Schrenk radix, and Vitis rotundifolia fruit showed the following inhibitory effects on ${\beta}$-catenin/TCF signaling: $40{\pm}5.6%$, $23{\pm}6.1%$, $8{\pm}5.1%$, and $22{\pm}9.8%$ in ${\beta}$-catenin-activated HEK-293 cells and $9{\pm}4.7%$, $39{\pm}8.1%$, $39{\pm}6.4%$, and $42{\pm}10.1%$ in ${\beta}$-catenin-activated SH-SY5y cells, respectively. Crude extracts of E. radix were isolated by silica gel column chromatography, and two non-polar fractions of these extracts showed inhibitory effects on ${\beta}$-catenin/TCF signaling. Conclusions: In this study, we established a transiently transfected cell line as a screening system and found that various medicinal herb extracts had inhibitory effects on ${\beta}$signaling.

Characteristics of Organic Carbon and Apparent Oxygen Utilization in the NE Pacific KODOS Area (북동태평양 KODOS 해역의 유기탄소 및 겉보기산소량 특성)

  • Son, Ju-Won;Son, Seung-Kyu;Kim, Kyeong-Hong;Kim, Ki-Hyune;Park, Yong-Chul;Kim, Dong-Hwa;Kim, Tae-Ha
    • Ocean and Polar Research
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    • v.27 no.1
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    • pp.1-13
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    • 2005
  • The samples for organic carbon analysis were collected between $5^{\circ}\;and\;17^{\circ}N$ along $131.5^{\circ}W$ in the northeast Pacific KODOS (Korea Deep Ocean Study) area. The mean concentration of total organic carbon (TOC) in the surface mixed layer $({\sim}50 m)$ was $100.13{\pm}2.05{\mu}M-C$, while the mean concentration of TOC in the lower 500m of the water column was $50.19{\pm}4.23{\mu}M-C$. A strong linear regression between TOC and temperature $(r^2=0.70)$ showed that TOC distribution was controlled by physical process. Results from the linear regression between chlorophyll-a and TOC, and between chlorophyll-a and particulate organic carbon (POC), decreasing of dissolved organic carbon (DOC) in the surface layer caused by non-biological photo-oxidation process. Below the surface layer, biological production and consumption occurred. DOC accumulation dominated in the depth range of $30{\sim}50m$ and DOC consumption occurred in the depth range of $50{\sim}200m$. TOC was inversely correlated with apparent oxygen utilization (AOU) and TOC/AOU molar ratios ranged from -0.077 to -0.21. These ratios indicated that TOC oxidation was responsible fur $10.9{\sim}30.1%$ (mean 20.2%) of oxygen consumption in the NE Pacific KODOS area. In the euphotic zone, distributions of dissolved and particulate organic matter were controlled by photo-chemical, chemical, biological and physical processes.

Theoretical Characterization of Binding Mode of Organosilicon Inhibitor with p38: Docking, MD Simulation and MM/GBSA Free Energy Approach

  • Gadhe, Changdev G.;Balupuri, Anand;Kothandan, Gugan;Cho, Seung Joo
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2494-2504
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    • 2014
  • P38 mitogen activated protein (MAP) kinase is an important anti-inflammatory drug target, which can be activated by responding to various stimuli such as stress and immune response. Based on the conformation of the conserved DFG loop (in or out), binding inhibitors are termed as type-I and II. Type-I inhibitors are ATP competitive, whereas type-II inhibitors bind in DFG-out conformation of allosteric pocket. It remains unclear that how these allosteric inhibitors stabilize the DFG-out conformation and interact. Organosilicon compounds provide unusual opportunity to enhance potency and diversity of drug molecules due to their low toxicity. However, very few examples have been reported to utilize this property. In this regard, we performed docking of an inhibitor (BIRB) and its silicon analog (Si-BIRB) in an allosteric binding pocket of p38. Further, molecular dynamics (MD) simulations were performed to study the dynamic behavior of the simulated complexes. The difference in the biological activity and mechanism of action of the simulated inhibitors could be explained based on the molecular mechanics/generalized Born surface area (MM/GBSA) binding free energy per residue decomposition. MM/GBSA showed that biological activities were related with calculated binding free energy of inhibitors. Analyses of the per-residue decomposed energy indicated that van der Waals and non-polar interactions were predominant in the ligand-protein interactions. Further, crucial residues identified for hydrogen bond, salt bridge and hydrophobic interactions were Tyr35, Lys53, Glu71, Leu74, Leu75, Ile84, Met109, Leu167, Asp168 and Phe169. Our results indicate that stronger hydrophobic interaction of Si-BIRB with the binding site residues could be responsible for its greater binding affinity compared with BIRB.

A Study on the Degradation of PAH in Organic and Aqueous Phases by Ozone (다환방향족탄화수소에 대한 오존처리의 방법에 관한 연구)

  • Choi, Young Ik;Son, Hee-Jong;Jung, Chul-Woo
    • Journal of Korean Society on Water Environment
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    • v.22 no.6
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    • pp.1123-1129
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    • 2006
  • Pyrene of natural and anthropogenic sources is one of the toxic, mutagenic polycyclic aromatic hydrocarbons (PAHs) listed as priority pollutants. The objectives of this research are to break down pyrene by using ozonation, identify the intermediates and byproducts of pyrene, and test the biodegradability of intermediates and byproducts of pyrene in the aqueous phase. Since pyrene is non-polar, hexane was chosen as a solvent to effectively dissolve pyrene. Pyrene solutions were treated with ozone, as it has high oxidation capacity and electrophilic characteristic. After different ozonation pretreatment times (2, 3, and 10 minutes), intermediates of pyrene in the form of yellowish solid were collected from the hexane solution using a centrifuge. They were identified by gas chromatography/mass spectrometer (GC/MS). $BOD_5$, COD, and E-coli toxicity tests have been performed to assess the ozonation products.

Effect of Boron Content and Temperature on Interactions and Electron Transport in BGaN Bulk Ternary Nitride Semiconductors

  • Bouchefra, Yasmina;Sari, Nasr-Eddine Chabane
    • Transactions on Electrical and Electronic Materials
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    • v.18 no.1
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    • pp.7-12
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    • 2017
  • This work takes place in the context of the development of a transport phenomena simulation based on group III nitrides. Gallium and boron nitrides (GaN and BN) are both materials with interesting physical properties; they have a direct band gap and are relatively large compared to other semiconductors. The main objective of this paper is to study the effect of boron content on the electron transport of the ternary compound $B_xGa_{(1-x)}N$ and the effect of the temperature of this alloy at x=50% boron percentage, specifically the piezoelectric, acoustic, and polar optical scatterings as a function of the energy, and the electron energy and drift velocity versus the applied electric field for different boron compositions ($B_xGa_{(1-x)}N$), at various temperatures for $B_{0.5}Ga_{0.5}N$. Monte carlo simulation, was employed and the three valleys of the conduction band (${\Gamma}$, L, X) were considered to be non-parabolic. We focus on the interactions that do not significantly affect the behavior of the electron. Nevertheless, they are introduced to obtain a quantitative description of the electronic dynamics. We find that the form of the velocity-field characteristic changes substantially when the temperature is increased, and a remarkable effect is observed from the boron content in $B_xGa_{(1-x)}N$ alloy and the applied field on the dynamics of holders within the lattice as a result of interaction mechanisms.

Long-Term Treatment Response to Lithium and Valproate in Patients with Bipolar 1 Disorder Treated More Than 2 Years : A Retrospective Study (1형 양극성 장애 환자에서 리튬과 발프로산의 장기간 치료 효과에 대한 후향적 평가 : 2년 이상 치료받은 환자의 효과 비교)

  • Ahn, Sung Woo;Yang, So-Yung;Choi, Yujin;Hong, Kyung Sue
    • Korean Journal of Biological Psychiatry
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    • v.23 no.4
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    • pp.185-192
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    • 2016
  • Objectives Treatment response of bipolar disorders (BDs) to long-term mood stabilizers maintenance has not been well explored because of complicated clinical and treatment courses. This study aims at investigating long-term clinical response of BDs to lithium and/or valproate in a naturalistic setting of a tertiary-care university-affiliated hospital. Methods Subjects were 65 patients with bipolar I (BD-I) disorders who had been treated with lithium and/or valproate for more than two years at single bipolar disorder clinic. Long-term response to the best treatment based on treatment algorithms and the current clinical standard of care was retrospectively evaluated using the Alda Scale and the Clinical Global Impression Scale for use in bi-polar illness (CGI-BP). Patients were classified into full responder and partial/non responder groups based on the total score of the Alda Scale with the cut-off score generated from the frequentist mixture analysis of the authors' previous study. Results The mean duration of treatment with the index medication was 69.2 months. Baseline demographic and clinical characteristics were not different among three mood stabilizer groups (valproate, lithium, and combination groups). Twenty-one subjects were classified into full responder group (32.3%). Treatment response assessed by the Alda Scale and CGI-BP scores was not different between lithium and valproate groups. The Alda Scale scores were well correlated with the CGI-BP scores (p < 0.05). Conclusions One third of the patients showed a full response to the long-term lithium and/or valproate treatment in BD-I. The degree of response was similar between lithium and valproate groups.

Comparison of Lipid Classes and Fatty Acid Compositions among Eight Species of Wild and Cultured Seawater Fishes

  • Moon Soo-Kyung;Choi Byeong-Dae;Jeong Bo-Young
    • Fisheries and Aquatic Sciences
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    • v.3 no.2
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    • pp.118-125
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    • 2000
  • Lipid classes and fatty acid compositions of eight species of wild and cultured seawater fish in Korea were investigated. Total lipid (TL) contents of wild and cultured fish were $2.64\pm1.88\%$ and $5.42\pm1.76\%$, respectively, except for rockfish and striped beakperch. Non-polar lipids (NL) in all fish samples comprised approximately $84\%$ of the TL content. The proportion equation of NL content to TL content was y=0.9296x-0.4468 $(R^2=0.98l2, p<0.001)$. The most abundant NL class was triglyceride. The prominent fatty acids in all fish samples were 16: 0, 18: 1(n-9), 22 : 6(n-3) (docosahexaenoic acid, DHA), 16: 1(n-7), 20 : 5 (n-3) (eicosapentaenoic acid, EPA), 18 : 0 and 18 : 1(n-7). The polyunsaturated fatty acid (PUFA) group was the richest among the total fatty acids (TFA). DHA and EPA were comprised of approximately $85\%$ of n-3 PUFA. There was a positive correlation between TFA content and n-3 PUFA content; y=0.292x-0.0055 $(R^2=0.9349, p<0.001)$. The n-3 PUFA content of the cultured fish was approximately twice as much as that of the wild fish. Therefore, cultured fish were proven to provide better sources of n-3 PUFA if compared to wild fish.

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Distribution Patterns of Sandy Bottom Macrobenthic Community on the Hupo Coastal Area, in the East Sea of Korea (동해 후포주변 사질조하대에 서식하는 대형저서동물군집의 분포특성)

  • Paik, Sang-Gyu;Kang, Rae-Seon;Jeon, Jae-Ok;Lee, Jae-Hac;Yun, Sung-Gyu
    • Ocean and Polar Research
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    • v.29 no.2
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    • pp.123-134
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    • 2007
  • Distribution patterns of sandy bottom macrobenthic communities were studied around the Hupo coastal area. The seasonal surveys were conducted at 15 chosen sites within a depth range of 10 to 50 m along 10 km of the coastline using a Smith-McIntyre grab $(0.05\;m^2)$ in 2005. Overall depth distribution following the direction of the offshore become deeper parallel to the coastline. A total of 319 macrobenthic species were sampled with a mean density of $1,972\;ind./m^2$, and mean biomass was 82.5 wet-weight $g/m^2$. The major individual-dominant species were three polychaetes Spiophanes bombyx ($436\;ind./m^2$), Scoletoma longifolia ($250\;ind./m^2$) and Magelona japonica ($170\;ind./m^2$), and bivalve Adontorhina subquadrata ($73\;ind./m^2$). Cluster analysis and non-metric multidimensional scaling (nMDS) analysis based on Bray-Curtis similarity identified 2 major station groups which corresponded to macrobenthic faunal assemblages and their characteristic species. In addition, environmental conditions were significantly different between station groups. Group I contained mostly 20 and 50 m deep sites and was associated with sandy mud. Group I was characterized by high abundance of S. bombyx, S. longifolia, A. subquadrata. It was divided into two sub-groups (I-I and I-II) in relation to depth. Sub-group I-I was associated with deeper sites than sub-group I-II. Group II included mostly inshore area shallower than 15 m and was associated with coarse and medium sand. Group II was characterized by Lumbrinerides hayashii and Urothoe grimaldii japonica.

Seasonal Variation of Mesozooplankton Communities in the Semi-enclosed Muan Bay, Korea (반 폐쇄된 무안만 중형동물플랑크톤 군집의 계절 변동)

  • Moon, Seong-Yong;Seo, Min-Ho;Shin, Yong-Sik;Soh, Ho-Young
    • Ocean and Polar Research
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    • v.34 no.1
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    • pp.1-18
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    • 2012
  • We investigated seasonal changes in the mesozooplankton community structure in November 2006 and February, May, and August 2007 at 12 stations in the semi-enclosed Muan Bay, Korea. Forty taxa were sampled, with an average abundance ranging from 1,459 to 20,078 indiv. $m^{-3}$; the highest abundance was detected in August 2007, and the lowest in February 2007. Acartia omorii, A. hudsonica, A. ohtsukai, Bestiolina coreana, Calanopia sp., Paracalanus parvus s. l., Cirripedia larvae, Decapoda larvae, and Gastropoda larvae were the most abundant taxa detected. The species diversity of the mesozooplankton was high around the inner regions in August 2007 but it was relatively low in November 2006. Non-metric multidimensional scaling (nMDS) revealed significant differences in the structure of mesozooplankton community among the seasons. Canonical correspondence analysis (CCA), performed to examine the relationships among dominant taxa, stations, and environmental variables, showed that most species of copepods were positively correlated with temperature, salinity, chlorophyll a, and COD concentration. Our results suggested that the mesozooplankton community structure observed in this study might be affected partly by the seasonal changes in environmental variables, such as the status of the sluice gates (i.e., open or closed) and the in situ production of resting eggs by major copepods.

Applicability of Fluorescein Diacetate (FDA) and Calcein-AM to Determine the Viability of Marine Plankton (FDA와 Calcein-AM 방법을 이용한 해양플랑크톤 생사판별기법)

  • Baek, Seung-Ho;Shin, Kyoung-Soon
    • Ocean and Polar Research
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    • v.31 no.4
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    • pp.349-357
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    • 2009
  • Ballast water is widely recognized as a serious environmental problem due to the risk of introducing non-indigenous aquatic species. In this study we aimed to investigate measures which can minimize the transfer of aquatic organisms from ballast water. Securing more reliable technologies to determine the viability of aquatic organisms is an important initiative in ballast water management systems. To evaluate the viability of marine phytoplankton, we designed the staining methods of fluorescein diacetate (FDA) and Calcein-AM assay on each target species belonging to different groups, such as bacillariphyceae, dinophyceae, raphidophyceae, chrysophyceae, haptophyceae and chlorophyceae. The FDA method, which is based on measurements of cell esterase activity using a fluorimetric stain, was the best dye for determining live cells of almost all phytoplankton species, except several diatoms tested in this study. On the other hand, although fluorescence of Calcein-AM was very clear for a comparatively longer time, green fluorescence per cell volume was lacking in most of the tested species. According to the Flow CAM method, which is a continuous imaging technique designed to characterize particles, green fluorescence values of stained cells by FDA were significantly higher than those of Calcein-AM treatments and control, implying that the Flow CAM using FDA assay could be adapted as an important tool for distinguishing living cells from dead cells. Our results suggest that the FDA and Calcein-AM methods can be adapted for use on phytoplankton, though species-specific characters are greatly different from one organism to another.