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Quantitative Structure-Activity Relationships in MAO-Inhibitor~' 2-Phenylcyclopropylarnines: Insights into the Topography of MAO-A and MAO-B

  • Kang, Gun-Il;Hong, Suk-Kil
    • Archives of Pharmacal Research
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    • v.13 no.1
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    • pp.82-96
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    • 1990
  • Ten (E)-and (Z)-isomers of 2-phenylcyclopropylamine (PCA), 1-Me PCA, 2-Me-PCA, N-Me-PCA, and N, N-diMe PCA and fifteen o-. m-, p- isomers of (E) PCA with substituents of Me, Cl, F, OMe, OH were synthesized in this laboratory and tested for the inhibition of rat brain mitochondrial MAO-A and MAO-B. The effects of substituents, their positions, and stereochemistry on the inhibition were assessed for the compounds with substituents at cyclopropyl and amino groups and QSAR analyses were performed using the potency data of ring-substituted compounds. The best correlated QSAR equations are as follows : pI$_{50}$ = 0.804 $\pi^2$-0.834 Blo-1.069 Blm + 0.334 Lp-1.709 HDp +7.897 (r = 0.945, s =0.211, F = 16.691, p = 0.000) for the inhibition of MAO-A;PI$_{50}$= 1.815$\pi$-0.825 $\pi^2$-1.203R + 0.900 Es$^2$ + 0.869 Es$^3$ + 0.796 Es$^4$-0.992 HDp + 0.562 HAo + 3.893 (r = 0.982, s =0.178, F = 23.351, p = 0.000) for the inhibition of MAO-B. Based on the potency difference between stereoisomers of cyclopropylamine-modified compounds and an QSAR cavity near para position, two hydrophobic carities interacting with Me group, a hydrophobic site near para position, and an amino group binding site and that in addition to the same two hydrophotic cavities, hydrophotic area, steric boundaries, hydrogen-acceptor site, and amino group binding site, another steric boundary near para position and a hydrogen donating site near ortho position constitute active sites of MAO-B.

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Effects of Thermal Effluents from Wolseong Nuclear Power Plant on Macroalgal Composition and Community Structure (월성원자력발전소 온배수가 해조류 종조성 및 군집구조에 미치는 영향)

  • Choi, Han-Gil
    • ALGAE
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    • v.23 no.2
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    • pp.151-162
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    • 2008
  • Marine algal flora and community structure were seasonally examined at three sites in the vicinity of the Wolseong nuclear power plant in Korea from February to November 2006. A total of 126 seaweeds including 25 green, 31 brown, 70 red algae, and 1 marine plant were identified. The greatest number of species occurred at Jeonchonri (101 species) followed by intake (88 species) and discharge (29 species) during the study period. Of 126 seaweeds, 76 annuals and 13 warm tolerance species were recorded. Dominant species based on important value (IV > 10) were Ulva pertusa and Enteromorpha linza at intake, U. pertusa and Padina arborescens at discharge, and Sargassum horneri and Corallina pilulifera at Jeonchonri shore. Annual average biomass exhibited a wide range of variations, from 40.67g m-2 in dry weight at discharge to 133.69g m-2 at Jeonchonri. Among six functional groups, dominant group was coarsely-branched form at intake and Jeonchonri, but it was different at discharge site as filamentous form. Seaweed community structures of discharge site were distinguishable in decreasing species richness, biomass, species diversity index (H’), richness index (R), and evenness index (J’). Also, the ratios of green algae, warm tolerance species, annual algae, filamentous form and dominance index (DI) remarkably increased. Such phenomenons of discharge site are usually found under environmentally stressful conditions such as high disturbance. Thus, I can conclude that the heated effluents of nuclear power plant act as environmental stress influencing seaweed community structures and it can be detected with various community indices.

Sources and Distributions of Organic Wastewater Compounds on the Mokpo Coast of Korea

  • Choi, Min-Kyu;Choi, Hee-Gu;Moon, Hyo-Bang;Yu, Jun;Kang, Sung-Kyung;Choi, Su-Kyung
    • Fisheries and Aquatic Sciences
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    • v.10 no.4
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    • pp.205-214
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    • 2007
  • Surface water and sediment samples collected from the Mokpo coast of Korea were analyzed for molecular markers of organic municipal wastewaters, i.e., 11 fecal sterols including coprostanol (Cop) and nonylphenolic compounds (NPs), to characterize the main routes of these wastewaters to the coast and to assess contamination levels. Concentrations of Cop ranged from 94 to 7,568 ng/L in surface water and from 43 to 38,108 ng/g dry weight in sediments. Concentrations of NPs [nonylphenol (NP) and nonylphenol mono- and di-ethoxylates ($NP_{1-2}EOs$)] ranged from 123 to 4,729 ng/L in surface water and from 4 to 2,119 ng/ng dry weight in sediments. The levels of these compounds were much higher at stations near the rivers that pass through the urban center of Mokpo and the outfall of the wastewater treatment plant (WWTP). The spatial distribution of Cop levels was statistically similar to that of NPs (r=0.809 and 0.982 in surface water and sediments, respectively), indicating that these compounds may have similar discharge points, transport, mixing, and deposition in the study area. These results suggest that considerable amounts of organic wastewater compounds are discharged through rivers and WWTP effluent to the Mokpo coast.

Detection and Characterization of PCR-SSCP Markers of the Bovine Lactoferrin Gene for Clinical Mastitis

  • Zhou, Lei;Yang, Yuan-Yuan;Li, Zhong-Hao;Kong, Li-Juan;Xing, Guan-Dong;Di, He-Shuang;Wang, Gen-Lin
    • Asian-Australasian Journal of Animal Sciences
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    • v.19 no.10
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    • pp.1399-1403
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    • 2006
  • A total of 80 cows, including 40 top mastitis resistant and 40 top mastitis susceptible animals as Group I and Group II, were selected from a population of 520 cows based on clinical mastitis occurrence. PCR-SSCP analysis on four fragments within the 5'region and two fragments of Exons 4,15 of bovine lactoferrin (bLF) revealed that four fragments-P1,P4,E4,E15-had polymorphisms which totally included six base mutations, and only two of them had significant differences in allele frequencies between resistant and susceptible groups, P1 (53.7% vs. 70.0%, p<0.05) and P4 (55.0% vs. 68.8%, p<0.05). Further study on these two promising markers combined with the milk performance traits of cows demonstrated that their selection would result in higher fat percentage (p<0.05), lower Somatic Cell Score (SCS) (p<0.05) and Clinical Mastitis Residuals (CMR) (p<0.01) indicating higher mastitis resistance and lower milk yield (p<0.05). The putative transcription factor binding sites in the 5'region were also studied by using MatInspector 7.2.2 software, and two signal pathways regulating the expression of bLF including the NF-${\kappa}B$ pathway and nuclear hormone receptor pathway were predicted.

Fruit Wall Anatomy of Ocotea (Lauraceae)

  • Heo, Kweon
    • Korean Journal of Plant Resources
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    • v.9 no.3
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    • pp.298-304
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    • 1996
  • The fruit wall anatomy of Ocotea was investigated on the basis of 14 species within the genus to contribute to a better understanding of specific relationships and homogeneity of genus. The species have a similar mature fruit wall structure, but diUerences among the species are found with respect to whether or not sdc.nchyma cells are present in the mesocarp. if present, whether or not they are present in particular positions and forms. Comparisons with species studied suggested that at least a few groups of species can be distinguished in Ocotea. They arc divided into five groups on the basis of anatomical structures. i.e., group 1) O. atrriensis, O. cujumari, O. helicterifolia, O. rubra and O. schomburgkiana; group 2) O. aeiphylla, O. javitensis, and O. sp. [Werff et ai. 12676]; group 3) O. tonduzii: group 4) O. foetens, O. quixos, and O. veraguensis; and group 5) O. floribunda and O. nitida. These various variations in Ocntea were also discussed to invite its respective systematic revisions. By the comparisons with species, on the other hand, it suggested that the specialized species are evolved from non-specialized species.

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Effects of Jowiseungcheung-tang Extract on the Lipid Metabolism, Anti-oxidation and Inflammatory Reflex High Fat Diet Obese Rats (조위승청탕(調胃升淸湯) 추출액이 비만유도 쥐의 지질대사, 항산화계 및 염증반응계에 미치는 영향)

  • Oh, Sung-Won;Kim, Byoung-Woo
    • The Journal of Internal Korean Medicine
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    • v.34 no.1
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    • pp.1-13
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    • 2013
  • Objectives : The purpose of this study was to investigate the effects of Jowiseungcheung-tang (JWSCT) extract on the lipid metabolism, anti-oxidation and inflammatory reflex. Methods : Male Sprague-Dawley rats were fed a high fat diet for 8 weeks and were randomly divided into 4 groups (10 mice in each group): control group, 100 mg/kg JWSCT group, 200 mg/kg JWSCT group, 300 mg/kg JWSCT group. The control group was administered 100 mg/kg of water, but the other three groups were administered 100, 200, 300 mg/kg JWSCT extract for 4 weeks. After 4 weeks, we measured lipid level, thiobarbituric acid reactive substance (TBARS), glutathione peroxidase (GSH-Px), superoxide dismutase (SOD), catalase (CAT), aspartate aminotransferase (AST), alanine aminotransferase (ALT) and cytokines in plasma and liver. The gene expression level and the ratio of apo-B and apo-E were then investigated by way of reverse transcription -polymerase chain reaction (RT-PCR). Results : In the JWSCT group, compared with the control, free fatty acid, triglyceride, total cholesterol, LDL-cholesterol, TBARS, IL-$1{\beta}$, IL-6 and TNF-${\alpha}$ decreased significantly in plasma and liver. However HDL-cholesterol, IL-10, GSH-Px, SOD and CAT increased. In the JWSCT group, compared with the control, the gene expression level and the ratio of apo-A and apo-E decreased significantly in the RT-PCR analysis. Conclusions : The extract of JWSCT has anti-obesity, anti-inflammatory and anti-oxidant effects.

Nω-Nitro-L-Arginine Methylester Ameliorates Myocardial Toxicity Induced by Doxorubicin

  • Mansour, Mahmoud Ahmed;El-Din, Ayman Gamal;Nagi, Mahmoud N.;Al-Shabanah, Othman A.;Al-Bekairi, Abdullah M.
    • BMB Reports
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    • v.36 no.6
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    • pp.593-596
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    • 2003
  • The effects of $N{\omega}$-nitro-L-arginine methylester (L-NAME) and L-arginine on cardiotoxicity that is induced by doxorubicin (Dox) were investigated. A single dose of Dox 15 mg/kg i.p. induced cardiotoxicity, manifested biochemically by a significant elevation of serum creatine phosphokinase (CPK) activity [EC 2.7.3.2]. Moreover, cardiotoxicity was further confirmed by a significant increase in lipid peroxides, measured as malon-di-aldehyde (MDA) in cardiac tissue homogenates. The administration of L-NAME 4 mg/kg/d p.o. in drinking water 5 days before and 3 days after the Dox injection significantly ameliorated the cardiotoxic effects of Dox, judged by the improvement in both serum CPK activity and lipid peroxides in the cardiac tissue homogenates. On the other hand, the administration of L-arginine 70 mg/kg/d p.o. did not protect the cardiac tissues against the toxicity that was induced by the Dox treatment. The findings of this study suggest that L-NAME can attenuate the cardiac dysfunction that is produced by the Dox treatment via the mechanism(s), which may involve the inhibition of the nitric oxide (NO) formation. L-NAME may, therefore, be a beneficial remedy for cardiotoxicity that is induced by Dox and can then be used to improve the therapeutic index of Dox.

Effect of Dietary Energy and Protein Contents on Buffalo Milk Yield and Quality during Advanced Lactation Period

  • Bovera, F.;Calabro, S.;Cutrignelli, M.I.;Di Lella, T.
    • Asian-Australasian Journal of Animal Sciences
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    • v.15 no.5
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    • pp.675-681
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    • 2002
  • Among Italian buffalo farmers, it is widely held that administering diets with high energy and protein concentrations is an effective way to increase milk production. In order to assess the validity of this opinion, we verified milk yield and physico-chemical characteristics from buffaloes that, from the $5^{th}$ month of lactation, were fed two total mixed rations (TMRs) which, given the same intake, should have led to satisfaction of protein requirements though with a slight energy deficit (diet A) or excessive amounts of energy and protein (diet B). Estimate of the energy and protein value of the diets and that of the corresponding requirements was carried out both by using two software programs derived from the Cornell Net Carbohydrate and Protein System (1992), and with the method set up by INRA researchers (1988). The results obtained show that the two diets administered did not result in significant changes to the quantity of milk produced. However, with Diet B the protein concentration in the milk was significantly (p<0.01) higher, although this was partly offset by the higher concentration (p<0.05) of non-protein nitrogen (NNP). The Group B buffaloes also showed significantly higher blood urea levels (p<0.01), with concentrations exceeding those considered physiological for lactating buffaloes. Finally, while administering Diet A the Body Condition Score (BCS) was close to 6.5 (Wagner et al., 1988), whereas in buffaloes which used Diet B it sometimes increased by over 0.5 points. As regards which of the two methods compared is more suitable for expressing dietary energy and protein value and corresponding requirements, we feel that due to the high variability in the Italian Mediterranean buffalo's milk production aptitude, it would be premature to express a judgement on methods which rest on a common scientific base and do not differ substantially.

Carrier Transport of Quantum Dot LED with Low-Work Function PEIE Polymer

  • Lee, Kyu Seung;Son, Dong Ick;Son, Suyeon;Shin, Dong Heon;Bae, Sukang;Choi, Won Kook
    • Proceedings of the Korean Vacuum Society Conference
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    • 2014.02a
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    • pp.432.2-432.2
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    • 2014
  • Recently, colloidal core/shell type quantum dots lighting-emitting diodes (QDLEDs) have been extensively studied and developed for the future of optoelectronic applications. In the work, we fabricate an inverted CdSe/ZnS quantum dot (QD) based light-emitting diodes (QDLED)[1]. In order to reduce work function of indium tin oxide (ITO) electrode for inverted structure, a very thin (<10 nm) polyethylenimine ethoxylated (PEIE) is used as surface modifier[2] instead of conventional metal oxide electron injection layer. The PEIE layer substantially reduces the work function of ITO electrodes which is estimated to be 3.08 eV by ultraviolet photoemission spectroscopy (UPS). From transmission electron microscopy (TEM) study, CdSe/ZnS QDs are uniformly distributed and formed by a monolayer on PEIE layer. In this inverted QD LED, two kinds of hybrid organic materials, [poly (9,9-di-n-octyl-fluorene-alt-benzothiadiazolo)(F8BT) + poly(N,N'-bis (4-butylphenyl)-N,N'-bis(phenyl)benzidine (poly-TPD)] and [4,4'-N,N'-dicarbazole-biphenyl (CBP) + poly-TPD], were adopted as hole transport layer having high highest occupied molecular orbital (HOMO) level for improving hole transport ability. At a low-operating voltage of 8 V, the device emits orange and red spectral radiation with high brightness up to 2450 and 1420 cd/m2, and luminance efficacy of 1.4 cd/A and 0.89 cd/A, respectively, at 7 V applied bias. Also, the carrier transport mechanisms for the QD LEDs are described by using several models to fit the experimental I-V data.

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Biochemical Reactions on a Microfluidic Chip Based on a Precise Fluidic Handling Method at the Nanoliter Scale

  • Lee, Chang-Soo;Lee, Sang-Ho;Kim, Yun-Gon;Choi, Chang-Hyoung;Kim, Yong-Kweon;Kim, Byung-Gee
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.11 no.2
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    • pp.146-153
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    • 2006
  • A passive microfluidic delivery system using hydrophobic valving and pneumatic control was devised for microfluidic handling on a chip. The microfluidic metering, cutting, transport, and merging of two liquids on the chip were correctly performed. The error range of the accuracy of microfluid metering was below 4% on a 20 nL scale, which showed that microfluid was easily manipulated with the desired volume on a chip. For a study of the feasibility of biochemical reactions on the chip, a single enzymatic reaction, such as ${\beta}-galactosidase$ reaction, was performed. The detection limit of the substrate, i.e. fluorescein $di-{\beta}-galactopyranoside$ (FDG) of the ${\beta}-galactosidase$ (6.7 fM), was about 76 pM. Additionally, multiple biochemical reactions such as in vitro protein synthesis of enhanced green fluorescence protein (EGFP) were successfully demonstrated at the nanoliter scale, which suggests that our microfluidic chip can be applied not only to miniaturization of various biochemical reactions, but also to development of the microfluidic biochemical reaction system requiring a precise nano-scale control.