• Title/Summary/Keyword: Binding Ability

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Korean Red Ginseng attenuates ethanol-induced steatosis and oxidative stress via AMPK/Sirt1 activation

  • Han, Jae Yun;Lee, Sangkyu;Yang, Ji Hye;Kim, Sunju;Sim, Juhee;Kim, Mi Gwang;Jeong, Tae Cheon;Ku, Sae Kwang;Cho, Il Je;Ki, Sung Hwan
    • Journal of Ginseng Research
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    • v.39 no.2
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    • pp.105-115
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    • 2015
  • Background: Alcoholic steatosis is the earliest and most common liver disease, and may precede the onset of more severe forms of liver injury. Methods: The effect of Korean Red Ginseng extract (RGE) was tested in two murine models of ethanol (EtOH)-feeding and EtOH-treated hepatocytes. Results: Blood biochemistry analysis demonstrated that RGE treatment improved liver function. Histopathology and measurement of hepatic triglyceride content verified the ability of RGE to inhibit fat accumulation. Consistent with this, RGE administration downregulated hepatic lipogenic gene induction and restored hepatic lipolytic gene repression by EtOH. The role of oxidative stress in the pathogenesis of alcoholic liver diseases is well established. Treatment with RGE attenuated EtOH-induced cytochrome P450 2E1, 4-hydroxynonenal, and nitrotyrosine levels. Alcohol consumption also decreased phosphorylation of adenosine monophosphate-activated protein kinase, which was restored by RGE. Moreover, RGE markedly inhibited fat accumulation in EtOH-treated hepatocytes, which correlated with a decrease in sterol regulatory element-binding protein-1 and a commensurate increase in sirtuin 1 and peroxisome proliferator-activated receptor-a expression. Interestingly, the ginsenosides Rb2 and Rd, but not Rb1, significantly inhibited fat accumulation in hepatocytes. Conclusion: These results demonstrate that RGE and its ginsenoside components inhibit alcoholic steatosis and liver injury by adenosine monophosphate-activated protein kinase/sirtuin 1 activation both in vivo and in vitro, suggesting that RGE may have a potential to treat alcoholic liver disease.

Anticarcinogenic Activity of a Novel Anthraquinone Derivative DHAQ-97: Induction of Apoptosis in Human Breast Cancer Cell Line MCF-7 (새로운 Anthraquinone 유도체, DHAQ-97의 항암작용: 아폽토시스에 의한 인체 유방암세포 사멸 유도)

  • 허연진;김정환;장정희;안병준;서영준
    • Environmental Mutagens and Carcinogens
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    • v.20 no.1
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    • pp.14-20
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    • 2000
  • DHAQ-97, (2-(3-[p-bis(2-chloroethyl)aminophenyl]-2 formylaminopropanoyloxy) methy1-1,4-dihy-droxy-9,10-anthraquinone), is a novel anthraquinone derivative synthesized for use as an anti-neoplastic agent. In the present study, we have evaluated the selective cytotoxicity of DHAQ-97 by comparing its effects on viability and proliferation of human breast cancer cell line (NCF-7) versus normal immortalized breast epithelial cell line (MCF-10A). Thus, DHAQ-97 reduced both viability and proliferation of MCF-7 cells to a much greater extent than did for MCF-10A cells. The growth inhibitory and anti-proliferative properties of DHAQ-97 appear to be attributable to its ability to induce apoptosis as revealed by positive staining after in 냐셔 nick-end labeling (TUNEL), cleavage of poly(ADP-ribose)polymerase, release of mitochondrial cytochrome c into cytoplasm, and increased expression of pro-apoptotic Bax protein. Recent studies have indicated possible involvement of the ubiquitous eukaryotic transcription factor, NF-kappa B (NF-kB) in the regulation of apoptotic cell death. In line induced cytotoxicity in cultured MCF-7 cells. Furthermore, mild activation of NF-kB, as determined by its increased DNA binding capability, was observed 30 min after treatment with 10$\mu\textrm{m}$ DHAQ-97. Taken together, the above findings suggest that DHAQ-97 exerts selective cytotoxicity towards cancer cells through induction of apoptosis, which appears to be regulated by NF-kB.

A novel pattern recognition protein of the Chinese oak silkmoth, Antheraea pernyi, is involved in the pro-PO activating system

  • Wang, Xialu;Zhang, Jinghai;Chen, Ying;Ma, Youlei;Zou, Wenjun;Ding, Guoyuan;Li, Wei;Zhao, Mingyi;Wu, Chunfu;Zhang, Rong
    • BMB Reports
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    • v.46 no.7
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    • pp.358-363
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    • 2013
  • In this paper, we firstly reported a C-type lectin cDNA clone of 1029 bps from the larvae of A. Pernyi (Ap-CTL) using PCR and RACE techniques. The full-length cDNA contains an open reading frame encoding 308 amino acid residues which has two different carbohydrate-recognition domains (CRDs) arranged in tandem. To investigate the biological activities in the innate immunity, recombinant Ap-CTL was expressed in E. coli with a 6-histidine at the amino-terminus (Ap-rCTL). Besides acted as a broad-spectrum recognition protein binding to a wide range of PAMPs and microorganisms, Ap-rCTL also had the ability to recognize and trigger the agglutination of bacteria and fungi. In the proPO activation assay, Ap-rCTL specifically restored the PO activity of hemolymph blocked by anti-Ap-rCTL antibody in the presence of different PAMPs or microorganisms. In summary, Ap-rCTL plays an important role in insect innate immunity as an pattern recognition protein.

3D-QSAR and Molecular Docking Studies on Benzotriazoles as Antiproliferative Agents and Histone Deacetylase Inhibitors

  • Li, Xiaolin;Fu, Jie;Shi, Wei;Luo, Yin;Zhang, Xiaowei;Zhu, Hailiang;Yu, Hongxia
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2387-2393
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    • 2013
  • Benzotriazole is an important synthetic auxiliary for potential clinical applications. A series of benzotriazoles as potential antiproliferative agents by inhibiting histone deacetylase (HDAC) were recently reported. Three-dimensional quantitative structure-activity relationship (3D-QSAR), including comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA), were performed to elucidate the 3D structural features required for the antiproliferative activity. The results of both ligand-based CoMFA model ($q^2=0.647$, $r^2=0.968$, ${r^2}_{pred}=0.687$) and CoMSIA model ($q^2=0.685$, $r^2=0.928$, ${r^2}_{pred}=0.555$) demonstrated the highly statistical significance and good predictive ability. The results generated from CoMFA and CoMSIA provided important information about the structural characteristics influence inhibitory potency. In addition, docking analysis was applied to clarify the binding modes between the ligands and the receptor HDAC. The information obtained from this study could provide some instructions for the further development of potent antiproliferative agents and HDAC inhibitors.

Differential Coupling of G$\alpha$q Family of G-protein to Muscarinic $M_1$ Receptor and Neurokinin-2-Receptor

  • Lee, Chang-Ho;Shin, In-Chul;Kang, Ju-Seop;Koh, Hyun-Chul;Ha, Ji-Hee;Min, Chul-Ki
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.423-428
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    • 1998
  • The ligand binding signals to a wide variety of seven transmembrane cell surface receptors are transduced into intracellular signals through heterotrimeric G-proteins. Recently, there have been reports which show diverse coupling patterns of ligand-activated receptors to the members of Gq family $\alpha$ subunits. In order to shed some light on these complex signal processing networks, interactions between G$\alpha$q family of G protein and neurokinin-2 receptor as well as muscarinic M$_{1}$ receptor, which are considered to be new thearpeutic targets in asthma, were studied. Using washed membranes from Cos-7 cells co-transfected with different G.alpha.q and receptor cDNAs, the receptors were stimulated with various concentrations of carbachol and neurokinin A and the agonist-dependent release of [$^3H$]inositol phosphates through phospholipase C beta-1 activation was measured. Differential coupling of Gaq family of G-protein to muscarinic M$_{1}$ receptor and neurokinin-2 receptor was observed. The neurokinin-2 receptor shows a ligand-mediated response in membranes co-transfected with G$\alpha$q, G$\alpha$11 and G$\alpha$14 but not G$\alpha$16 and the ability of the muscarinic $M_1$ receptor to activate phospholipase C through G$\alpha$/11 but not G$\alpha$14 and G$\alpha$16 was demonstrated. Clearly G$\alpha$/11 can couple $\M_1$ and neurokinin-2 receptor to activate phospholipase C. But, there are differences in the relative coupling of the G$\alpha$14 and G$\alpha$16 subunits to these receptors.

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Helicobacter pylori Infection is a Risk Factor for Iron-Deficiency Anemia in Korean High School Girls

  • Hong, Soon-Myung;Hwang, Hye-Jin;Park, Sang-Kyu
    • Preventive Nutrition and Food Science
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    • v.8 no.1
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    • pp.70-74
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    • 2003
  • This study investigated the relationship of Helicobacter pylori (H. pylori) infection to iron-deficiency anemia in high school girls. Four hundred and fourty-five subjects resided in Ulsan City in Korea were evaluated by questionnaire or blood analysis for serum indicators of iron status, daily nutrient intakes, symptoms of anemia, and H. pylori IgG antibody status. In H. pylori infected subjects, total energy intake of was 1534.14±350.81 kcal (73.0% of the Korean RDA), the iron intake of subjects was 11.38±3.90 mg (71.1% of Korean RDA) and calcium intake was 467.63±175.96 mg (58.3% of the Korean RDA). Carbohydrate (p < 0.05), vitamin A (p < 0.05), vitamin C (p < 0.01) intakes were significantly lower in infected subjects than in non-infected subjects. The prevalence of anemia (hemoglobin (Hb) < 12 g/dL.) in H. pylori infected subjects was 22.7% as compared to 14.7% in non-infected subjects. The mean serum ferritin of infected subjects (21.71±21.50 ng/mL) was significantly lower than in non-infected subjects (p < 0.05) (as was the mean Hb concentration (12.54±1.51 g/dL) and hematocrit (37.99±3.64%)). Total iron binding capacity (TIBC) of H. pylori infected subjects (449.09±78.23 ㎍/dL) was significantly higher than that of non-infected subjects (432.99+76.15 ㎍/dL) (P < 0.05). The levels of iron, red blood cell (RBC) and transferrin saturation were similar in infected and non-infected subjects. Two symptoms of anemia, 'pale face (p < 0.01)' and 'decreased ability to concentrate (p < 0.005)', were significantly higher in H. pylori infected subjects than in non-infected subjects. High school girls are known to be more vulnerable to iron deficiency than other age groups, and this research demonstrates that infection with H. pylori increases their risk of iron-deficiency anemia.

Absorption analysis of streptavidin-biotin complexes using AFM (AFM을 이용한 스트렙타비딘-바이오틴 단백질 복합체의 흡착 분석)

  • Park, Jee-Eun;Kim, Dong-Sun;Choi, Ho-Jin;Shin, Jang-Kyoo;Kim, Pan-Kyeom;Lim, Geun-Bae
    • Journal of Sensor Science and Technology
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    • v.15 no.4
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    • pp.237-244
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    • 2006
  • Atomic force microscope (AFM) has become a common tool for the structural and physical studies of biological macromolecules, mainly because it provides the ability to perform experiments with samples in a buffer solution. In this study, structure of proteins and nucleic acids has been studied in their physiological environment that allows native intermolecular complexes to be formed. Cr and Au were deposited on p-Si (100) substrate by thermal evaporation method in sequence with the thickness of $200{\AA}$ and $500{\AA}$, respectively, since Au is adequate for immobilizing biomolecules by forming a self-assembled monolayer (SAM) with semiconductor-based biosensors. The SAM, streptavidin and biotin interacted each other with their specific binding energy and their adsorption was analyzed using the Bio-AFM both in a solution and under air environment. A silicon nitride tip was used as a contact tip of Bio-AFM measurement in a solution and an antimony doped silicon tip as a tapping tip under air environment. Actual morphology could also be obtained by 3-dimensional AFM images. The length and agglomerate size of biomolecules was measured in stages. Furthermore, $R_{a}$ (average of surface roughness) and $R_{ms}$ (mean square of surface roughness) and surface density for the adsorbed surface were also calculated from the AFM image.

Heavy Metal Accumulation in Cell of Heavy Metal-Tolerant Bacteria by Some Physical and Chemical Treatments (물리화학적 전처리에 의한 중금속 내성세균의 균체내 중금속 축적 변화)

  • Cho, Ju-Sik;Lee, Hong-Jae;Heo, Jong-Soo
    • Korean Journal of Environmental Agriculture
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    • v.16 no.4
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    • pp.311-319
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    • 1997
  • Heavy metal-tolerant microorganisms, such as Pseudomonas putida, P. aeruginosa, P. chlororaphis and P. stutzeri which possessed the ability to accumulate cadmium, lead, zinc and copper, respectively, were isolated from industrial wastewaters and mine wasewaters polluted with various heavy metals. Metal binding sites in the cells were investigated by extracting the components of the cells through pretreatments with hot water, acid, alkli, chloroform-methanol or chloroform-methanol/concentrated alkali. The heavy metal accumulation was drastically decreased by pretreatment with alkali or chloroform-methanol/concentrated alkali, but the heavy metal accumulation was not changed by pretreatment with chloroform-methanol. The amount of heavy metal accumulation was remarkably decreased by decreasing crude protein remaining in the cell. These results suggested that proteins of cell components played an important role on the heavy metal accumulation.

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Heparin Attenuates the Expression of TNF $\alpha$-induced Cerebral Endothelial Cell Adhesion Molecule

  • Lee, Jeong-Ho;Kim, Chul-Hoon;Seo, Gi-Ho;Lee, Jin-U;Kim, Joo-Hee;Kim, Dong-Goo;Ahn, Young-Soo
    • The Korean Journal of Physiology and Pharmacology
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    • v.12 no.5
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    • pp.231-236
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    • 2008
  • Heparin is a well-known anticoagulant widely used in various clinical settings. Interestingly, recent studies have indicated that heparin also has anti-inflammatory effects on neuroinflammation-related diseases, such as Alzheimer's disease and meningitis. However, the underlying mechanism of its actions remains unclear. In the present study, we examined the anti-inflammatory mechanism of heparin in cultured cerebral endothelial cells (CECs), and found that heparin inhibited the tumor necrosis factor $\alpha$ ($TNF{\alpha}$)-induced and nuclear factor kappa B (NF-${\kappa}B$)-dependent expression of adhesion molecules, such as intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1), which are crucial for inflammatory responses. Heparin selectively interfered with NF-${\kappa}B$ DNA-binding activity in the nucleus, which is stimulated by $TNF{\alpha}$. In addition, non-anticoagulant 2,3-O desulfated heparin (ODS) prevented NF-${\kappa}B$ activation by $TNF{\alpha}$, suggesting that the anti-inflammatory mechanism of heparin action in CECs lies in heparin's ability to inhibit the expression of cell adhesion molecules, as opposed to its anticoagulant actions.

Mobile Router Decision Using Multi-layered Perceptron in Nested Mobile Networks (중첩 이동 네트워크에서 Multi-layered Perceptron을 이용한 최적의 이동 라우터 지정 방안)

  • Song, Jiyoung
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.17 no.12
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    • pp.2843-2852
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    • 2013
  • In the nested mobile network environment, the mobile node selects one of multiple mobile routers. The MR(Mobile Router) by existing top-down or bottom-up methods may not be the optimal MR if the numbers of mobile nodes and routers are substantially increased, and the scale of the network is increased drastically. Since an inappropriate MR decision causes handover or binding renewal to mobile nodes, determining of the optimal MR is important for efficiency. In this paper, we propose an algorithm that decides on the optimal MR using MR QoS(Quality of Service) information, and we describe how to understand the various structured MLP(Multi-Layered Perceptron) based on the algorithm. In conclusion, we prove the ability of the suggested neural network for a nesting mobile network through the performance analysis of each learned MLP.