• Title/Summary/Keyword: hPc2

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Synthesis and Inhibitory Activity on NF-${\kappa}B$ Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives (크로만-2-카르복실산 N-헤테로아릴아마이드 유도체 합성 및 NF-${\kappa}B$ 저해 활성)

  • Yi, Won-Hui;Kwak, Jae-Hwan;Han, Sang-Bae;Kim, Young-Soo;Jung, Jae-Kyung;Lee, Hee-Soon
    • YAKHAK HOEJI
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    • v.56 no.3
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    • pp.186-190
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    • 2012
  • Nuclear factor-${\kappa}B$ (NF-${\kappa}B$) has been considered as one of the major targets for therapeutic agents of diverse human diseases. In the previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) and chroman-2-carboxylic acid N-(4-chlorophenyl)amide were identified as good inhibitors of NF-${\kappa}B$ activation. In this continuous study, we describe the synthesis and NF-${\kappa}B$ inhibitory activities of chroman derivatives containing N-heteroaryl groups for exploration of SAR (structure-activity relationship). In addition, inhibitory effects of cell proliferation are evaluated against human cancer cell lines (NCI-H23 and PC-3).

Evaluation of Bacteriophage Supplementation on Growth Performance, Blood Characteristics, Relative Organ Weight, Breast Muscle Characteristics and Excreta Microbial Shedding in Broilers

  • Wang, J.P.;Yan, L.;Lee, J.H.;Kim, In Ho
    • Asian-Australasian Journal of Animal Sciences
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    • v.26 no.4
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    • pp.573-578
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    • 2013
  • A total of 720 1-d-old male broilers (Arbor Acres) with the initial BW = $45{\pm}2$ g were used in a 32-d experiment. Birds were randomly allotted into 1 of 4 treatments according to a completely random block design. Dietary treatments included: i) CON (basal diet), ii) ANT (CON+0.5 g antibiotics/kg feed (bacitracin methylene disalicylate)), iii) BP1 (CON+0.25 bacteriophage/kg feed), and iv) BP2 (CON+0.5 g bacteriophage/kg feed). The BWG and FI were not affected by dietary treatments throughout the whole experiment, whereas BP2 treatment reduced (p<0.05) the feed conversion ratio compared with the CON treatment during 0 to 14 d. The birds fed bacteriophages at the level of 0.25 g/kg increased (p<0.05) the relative liver weight. The inclusion of antibiotic and bacteriophage significantly reduced (p<0.05) the Escherichia coli and Salmonella concentration in the excreta compared with the NC group. Broilers fed the BP2 treatment had higher (p<0.05) lactobacillus counts compared with those fed NC and PC treatments. In conclusion, dietary supplementation of 0.5 g/kg bacteriophages increased feed efficiency and liver weight without effects on the breast muscle properties; also pathogens were inhibited by addition of bacteriophages.

A Study of Shielding Properties of X-ray and Gamma in Barium Compounds

  • Seenappa, L.;Manjunatha, H.C.;Chandrika, B.M.;Chikka, Hanumantharayappa
    • Journal of Radiation Protection and Research
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    • v.42 no.1
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    • pp.26-32
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    • 2017
  • Background: Ionizing radiation is known to be harmful to human health. The shielding of ionizing radiation depends on the attenuation which can be achieved by three main rules, i.e. time, distance and absorbing material. Materials and Methods: The mass attenuation coefficient, linear attenuation coefficient, Half Value Layer (HVL) and Tenth Value Layer (TVL) of X-rays (32 keV, 74 keV) and gamma rays (662 keV) are measured in Barium compounds. Results and Discussion: The measured values agree well with the theory. The effective atomic numbers ($Z_{eff}$) and electron density (Ne) of Barium compounds have been computed in the wide energy region 1 keV to 100 GeV using an accurate database of photon-interaction cross sections and the WinXCom program. Conclusion: The mass attenuation coefficient and linear attenuation coefficient for $BaCO_3$ is higher than the $BaCl_2$, $Ba(No_3)_2$ and BaSO4. HVL, TVL and mean free path are lower for $BaCO_3$ than the $BaCl_2$, $Ba(No_3)_2$ and $BaSO_4$. Among the studied barium compounds, $BaCO_3$ is best material for x-ray and gamma shielding.

Determination of Optimal Welding Parameter for an Automatic Welding in the Shipbuilding

  • Park, J.Y.;Hwang, S.H.
    • International Journal of Korean Welding Society
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    • v.1 no.1
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    • pp.17-22
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    • 2001
  • Because the quantitative relationships between welding parameters and welding result are not yet blown, optimal values of welding parameters for $CO_2$ robotic arc welding is a difficult task. Using the various artificial data processing methods may solve this difficulty. This research aims to develop an expert system for $CO_2$ robotic arc welding to recommend the optimal values of welding parameters. This system has three main functions. First is the recommendation of reasonable values of welding parameters. For such work, the relationships in between the welding parameters are investigated by the use of regression analysis and fuzzy system. The second is the estimation of bead shape by a neural network system. In this study the welding current voltage, speed, weaving width, and root gap are considered as the main parameters influencing a bead shape. The neural network system uses the 3-layer back-propagation model and a generalized delta rule as teaming algorithm. The last is the optimization of the parameters for the correction of undesirable weld bead. The causalities of undesirable weld bead are represented in the form of rules. The inference engine derives conclusions from these rules. The conclusions give the corrected values of the welding parameters. This expert system was developed as a PC-based system of which can be used for the automatic or semi-automatic $CO_2$ fillet welding with 1.2, 1.4, and 1.6mm diameter the solid wires or flux-cored wires.

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3D Brain-Endoscopy Using VRML and 2D CT images (VRML을 이용한 3차원 Brain-endoscopy와 2차원 단면 영상)

  • Kim, D.O.;Ahn, J.Y.;Lee, D.H.;Kim, N.K.;Kim, J.H.;Min, B.G.
    • Proceedings of the KOSOMBE Conference
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    • v.1998 no.11
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    • pp.285-286
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    • 1998
  • Virtual Brain-endoscopy is an effective method to detect lesion in brain. Brain is the most part of the human and is not easy part to operate so that reconstructing in 3D may be very helpful to doctors. In this paper, it is suggested that to increase the reliability, method of matching 3D object with the 2D CT slice. 3D Brain-endoscopy is reconstructed with 35 slices of 2D CT images. There is a plate in 3D brain-endoscopy so as to drag upward or downward to match the relevant 2D CT image. Relevant CT image guides the user to recognize the exact part he or she is investigating. VRML Script is used to make the change in images and PlaneSensor node is used to transmit the y coordinate value with the CT image. The result is test on the PC which has the following spec. 400MHz Clock-speed, 512MB ram, and FireGL 3000 3D accelerator is set up. The VRML file size is 3.83MB. There was no delay in controlling the 3D world and no collision in changing the CT images. This brain-endoscopy can be also put to practical use on medical education through internet.

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Synthesis, Radiolabeling and Gastrin Releasing Peptide Receptor Binding Affinity of a Novel Bombesin Antagonist-Based Peptide, DOTA-Ala(SO3H)-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-NH2

  • Lim, Jae Cheong;Choi, Sang Mu;Cho, Eun Ha;Kim, Jin Joo
    • Journal of Radiation Industry
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    • v.7 no.2_3
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    • pp.127-134
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    • 2013
  • Bombesin receptors are overexpressed in many kinds of human tumors. In particular, the gastrin releasing peptide receptor (GRPR) which is also called bombesin receptor subtype 2, has been identified in prostate cancer. In the present study, we developed a bombesin antagonist-based $^{177}Lu$-labeled peptide, $^{177}Lu$-DOTA-$Ala(SO_3H)$-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-$NH_2$ (DOTA-sBBNA). DOTA-sBBNA was prepared using a solid phase synthesis method. It was labeled with $^{177}Lu$ by a high radiolabeling yield (>98%), and its Log P value was -2.05. The radiolabeled peptide was highly stable in serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-Bombesin on the PC-3 human prostate carcinoma cells revealed that the $IC_{50}$ value of the peptide was 6.76 nM indicating a highly nanomolar binding affinity for GRPR. These results suggest that $^{177}Lu$-DOTA-sBBNA can be a potential candidate for targeting prostate cancer, and further studies to evaluate its biological characteristics are needed.

Novel Bombesin Analogues Conjugated with DOTA-Ala(SO3H)-4 aminobenzoic acid and DOTA-Lys(glucose)-4 aminobenzoic acid: Synthesis, Radiolabeling, and Gastrin Releasing Peptide Receptor Binding Affinity

  • Lim, Jae Cheong;Choi, Sang Mu;Cho, Eun Ha;Kim, Jin Joo
    • Journal of Radiation Industry
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    • v.7 no.2_3
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    • pp.191-200
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    • 2013
  • In this study, a novel bombesin (BBN) analogues, DOTA-Ala($SO_3H$)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-sBBN) and DOTA-Lys(glucose)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-gluBBN), were synthesized and radiolabeled, and their binding affinities were evaluated. Peptides were prepared by a solid phase synthesis method and their purities were over 98%. DOTA is the chelating agent for $^{177}Lu$-labeling, and the DOTA-conjugated peptides were radiolabeled with $^{177}Lu$ by a high radiolabeling yield (>98%). The Log P values of DOTA-sBBN and DOTA-gluBBN were -2.20 and -2.79, respectively. 50.41% of $^{177}Lu$-DOTA-sBBN and 72.97% of $^{177}Lu$-DOTA-gluBBN were left undegraded by the serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-BBN on the PC-3 human prostate carcinoma cells revealed that 50% inhibitory concentration ($IC_{50}$) were 1.46 nM of DOTA-sBBN and 4.67 nM of DOTA-gluBBN indicating a highly nanomolar binding affinity for GRPR. Therefore, it is concluded that $^{177}Lu$-DOTA-sBBN and $^{177}Lu$-DOTA-gluBBN can be potential candidates as a targeting modality for the Gastrin-releasing peptide receptor (GRPR)-over-expressing tumors, and further studies to evaluate their biological and pharmacological characteristics are needed.

Hydrophilic surface formation of polumer treated by ion assisted reaction and its applications (이온빔보조 반응법을 이용한 고분자 표면의 친수성처리와 그 응용)

  • Cho, J.;Choi, S. C.;Yun, K.H.;Koh, S. K.
    • Journal of the Korean Vacuum Society
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    • v.8 no.3B
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    • pp.262-268
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    • 1999
  • Polycarbonate (PC) and Polymethylmethacrylate (PMMA) surface was modified by ion assisted reaction (IAR) technique to obtain the hydrophilic functional groups and improve the wettability. In conditions of ion assisted reaction, ion beam energy was changed from 500 to 1500eV, and ion dose and oxygen gas blown rate were fixed $1\times10^{16}$ ions/$\textrm{cm}^2$ and 4ml/min, respectively. Wetting angle of water on PC and PMMA surface modified by $Ar^+$ ion without blowing oxygen at 4ml/mon showed $5^{\circ}$ and $10^{\circ}$. Changes of wetting angle with oxygen gas and $Ar^+$ ion irradiation were explained by considering formation of hydrophilic group due to a reaction between irradiated polymer chain by energetic ion irradiation and blown oxygen gas. X-ray photoelectron spectroscopy analysis shows that hydrophilic groups such as -C-O, -(C=O)- and -(C=O)-O- are formed on the surface of polymer by chemical interaction. The polymer surface modification using ion assisted reaction only changed the surface physical properties and sept the bulk properties. In comparison with other modification methods, the surface modification by IAR treatment was chemically stable and enhanced the adhesion between metal and polymer surface. The applications of various kinds of polymer surface modification methods, metal and polymer surface. The applications of various kinds of polymer surface modification could be appled to the new materials about hydrophilic surface properties by IAR treatment. The adhesion between metal film and polymer measured by Scotch tape test whether the hydrophilic surfaces could improve the adhesion strength or not.

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Isolation of Anthraquinone Derivatives from the Root of Rumex japonicus H. (참소리쟁이 뿌리에서 안트라퀴논계 화합물의 분리 및 생리활성)

  • Hwang, Seon-Woo;Ha, Tae-Joung;Lee, Jong-Rok;Lee, Jun;Nam, Sang-Hae;Park, Ki-Hun;Yang, Min-Suk
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.274-278
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    • 2004
  • Four anthraquinone derivatives were isolated from the root of Rumex japonicus Houtt. These compounds were identified as physcion, emodin, chrysophanol-10,10'-bianthrone and $physcion-10,10'-bianthrone^(a)$, respectively. The last compound (a), especially, showed strong activity against A549, PC-3, UO-31 and HCT-15 human cancer cell lines with $IC_{50}$ values, ranging from 0.45 to $1.33\;{\mu}g/ml^{-1})$.

Effects of Seomaeyakssuk (Artemisia argyi H.) Vinegar on Lipid Metabolism in Rats Fed a High-Fat and High-Cholesterol Diet (섬애약쑥 식초가 고지방-고콜레스테롤 급이 흰쥐의 체내 지질대사에 미치는 영향)

  • Shin, Jeong Yeon;Kang, Jae Ran;Shin, Jung Hye;Seo, Weon Taek;Byun, Hee Uk;Choi, Jin Sang;Kang, Min Jung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.46 no.7
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    • pp.779-789
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    • 2017
  • The effects of orally administered Seomaeyakssuk (Artemisia argyi H.) vinegar on lipid metabolism in Sprague-Dawley rats fed a high-fat and high-cholesterol (HFC) diet were analyzed. The experimental animals were divided into five groups: a normal diet group (normal, N), HFC diet group (control, C), HFC diet with lovastatin at 20 mg/kg body weight (B.W.) group (positive control, PC), HFC diet with malt vinegar group (TM), and HFC diet with Seomaeyaksuk vinegar group (TS) (2 mL/kg B.W.). After 4 weeks of feeding rats the experimental diet, contents of serum total lipids and total cholesterol levels of TM and TS groups were significantly lower than those of the PC group. Triglyceride contents of the TM and TS groups were not significantly different from those of the PC group but significantly lower than those of the C group. Content of serum high density lipoprotein-cholesterol was significantly lower than that of the N group but higher than that of the C group. Low density lipoprotein-cholesterol content of serum was 190.68 mg/dL in the TS group, which was the lowest except for the N group. Aspartate transaminase and albumin transaminase activities as a measurement of liver damage index were not significantly different between the TM, TS, and C groups. Serum thiobarbituric acid reactive substance content of the TS group was reduced to a similar level as the N group but was lower than that of the C group in the liver and significantly higher than that of the N group. Antioxidant activity of the TS group was 55.69% in serum, which was a similar to that of the N group, and was 52.39% in the liver, which was not significantly different than that of the C group. From these results, we conclude that Seomaeyakssuk vinegar improves serum lipid content as a result of the complex action of vinegar, an active ingredient of Seomaeyakssuk and a product of the fermentation process.