• Title/Summary/Keyword: Pre-AMP

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Pharmacokinetic and Pharmacodynamic Interaction between Metformin and (-)-Epigallocatechin-3-gallate

  • Ko, Jeong-Hyeon;Jang, Eun-Hee;Park, Chang-Shin;Kim, Hyoung-Kwang;Cho, Soon-Gu;Shin, Dong-Wun;Yi, Hyeon-Gyu;Kang, Ju-Hee
    • Molecular & Cellular Toxicology
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    • v.5 no.4
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    • pp.298-303
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    • 2009
  • (-)-Epigallocatechin-3-gallate (EGCG), a major flavonoid in green tea has multiple health benefits including chemoprevention, anti-inflammatory, anti-diabetic, and anti-obesity effects. In connection with these effects, EGCG can be a candidate to help the treatment of metabolic diseases. Metformin is a widely used anti-diabetic drug regulating cellular energy homeostasis via AMP-activated protein kinase (AMPK) activation. Therefore, the combination of metformin with EGCG may have additive or synergistic effects on treatment of type 2 diabetes. Nevertheless, there is no report for the pharmacokinetic and/or pharmacodynamic interaction of EGCG with metformin. Here, we evaluated the pharmacokinetic and pharmacodynamic interaction between metformin and EGCG in rats. Pharmacokinetics parameters of metformin were measured after oral administration of metformin in rats pre-treated with EGCG (10 mg/kg) or saline for 7 days. The results showed that there is no significant difference in pharmacokinetic parameters between saline control and EGCG-treated group. In addition, the hepatic AMPK activation by metformin in EGCG-treated rats was also similar to the control. The lack of additive effects of EGCG on AMPK activation or intracellular uptake of metformin was also evaluated in cells in the presence or absence of EGCG. Treatment of HepG2 cells with EGCG inhibited the metformin-induced AMPK activation. Combined results suggested that EGCG has no effect on the pharmacokinetics of metformin but may contribute to metformin action.

Georadar System Using Network-Analyzer (네트웍 분석기를 이용한 레이다탐사 시스템의 구현)

  • Cho Seong-Jun;Kim Jung-Ho;Lee Seoung Kon;Son Jeong-Sul;Chung Seung-Hwan
    • Geophysics and Geophysical Exploration
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    • v.5 no.4
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    • pp.272-279
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    • 2002
  • During field survey of ground penetrating radar or borehole radar, we often encounter some problems which could be solved easily by modifying structure of the system such as antenna length, shape or array. In addition, it is necessary that the user could easily modify configuration of the radar system na test various array of antennas in order to verify and confirm numerical modeling results concerning radar antennas. We have developed network-analyzer-based, stepped-frequency georadar system. This system had been comprised with coaxial cable to confirm possibility of the system, then we have upgraded the system to use optical cable that is composed of optical/electric transducers, electric/optical transducers, amp, pre-amp and antennas. The software for the aquisition of data has been developed to control the system automatically using PC with GPIB communication and to display the obtained data graphically. We have tested the system in field survey na the results have been compared with those of RAMAC/GPR system.

Metabolomic analysis of healthy human urine following administration of glimepiride using a liquid chromatography-tandem mass spectrometry

  • Do, Eun Young;Gwon, Mi-Ri;Kim, Bo Kyung;Ohk, Boram;Lee, Hae Won;Kang, Woo Youl;Seong, Sook Jin;Kim, Hyun-Ju;Yoon, Young-Ran
    • Translational and Clinical Pharmacology
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    • v.25 no.2
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    • pp.67-73
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    • 2017
  • Glimepiride, a third generation sulfonylurea, is an antihyperglycemic agent widely used to treat type 2 diabetes mellitus. In this study, an untargeted urinary metabolomic analysis was performed to identify endogenous metabolites affected by glimepiride administration. Urine samples of twelve healthy male volunteers were collected before and after administration of 2 mg glimepiride. These samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS), and then subjected to multivariate data analysis including principal component analysis and orthogonal partial least squares discriminant analysis. Through this metabolomic profiling, we identified several endogenous metabolites such as adenosine 3', 5'-cyclic monophosphate (cAMP), quercetin, tyramine, and urocanic acid, which exhibit significant metabolomic changes between pre- and posturine samples. Among these, cAMP, which is known to be related to insulin secretion, was the most significantly altered metabolite following glimepiride administration. In addition, the pathway analysis showed that purine, tyrosine, and histidine metabolism was affected by pharmacological responses to glimepiride. Together, the results suggest that the pharmacometabolomic approach, based on LC-MS/MS, is useful in understanding the alterations in biochemical pathways associated with glimepiride action.

Inhibitory Effect of the Ethanol Extract of Rudbeckia laciniata var. hortensis Bailey on Adipocyte Differentiation in 3T3-L1 Cells (겹삼잎국화 에탄올 추출물의 지방세포 분화 억제 효과)

  • Nam, Gun He;Wee, Ji-Hyang;Kim, Sang Yung;Baek, Ji-Young;Kim, Young Min
    • Journal of Life Science
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    • v.29 no.10
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    • pp.1152-1158
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    • 2019
  • Rudbeckia laciniata var. hortensis Bailey is used in home remedy for colic and gastritis in South Korea. Although Rudbeckia laciniata var. hortensis Bailey is used extensively for home remedies, no single study on its efficacy exists. In this study, we investigated the anti-obesity effects of Rudbeckia laciniata var. hortensis Bailey. The anti-obesity effect of a 70% ethanol extract from Rudbeckia laciniata var. hortensis Bailey on the differentiation of 3T3-L1 pre-adipocytes to adipocytes was investigated with an Oil Red O assay, western blot analysis, and mRNA analysis. Compared to the control (only treated with DM), the 70% ethanol extract of Rudbeckia laciniata var. hortensis Bailey significantly inhibited adipocyte differentiation and intracellular triglyceride (TG) levels at a concentration of $100{\mu}g/ml$. To determine how the TG content was reduced, we measured the level of protein and mRNA expression of obesityrelated agents, such as peroxisome proliferators-activated receptor ${\gamma}$ ($PPAR{\gamma}$), CCAAT/enhancer- binding protein ${\alpha}$ ($C/EBP{\alpha}$), AMP-activated protein kinase (AMPK) phosphorylation, LPL, and FAS. As a result, the 70% ethanol extract of Rudbeckia laciniata var. hortensis Bailey significantly increased the expression of AMPK and decreased the expression of genes related to adipogenesis and fat storage, such as $PPAR{\gamma}$, $C/EBP{\alpha}$, LPL, and FAS.

Extract of Ranunculus sceleratus Reduced Adipogenesis by Inhibiting AMPK Pathway in 3T3-L1 Preadipocytes (3T3-L1 전구지방세포에서 개구리자리(Ranunculus sceleratus) 추출물의 AMPK 신호전달을 통한 지방생성 억제 효과)

  • Kim, Yae-Ji;Cho, Sung-Pil;Lee, Hui-Ju;Hong, Geum-Lan;Kim, Kyung-Hyun;Ryu, Si-Yun;Jung, Ju-Young
    • Journal of Korean Medicine for Obesity Research
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    • v.22 no.1
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    • pp.30-37
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    • 2022
  • Objectives: Adipogenesis is the process by which pre-adipocytes are differentiated into adipocytes. It also plays an important role in adipocyte formation and lipid accumulation. Ranunculus sceleratus (R. sceleratus) extracts are used for the treatment of various diseases such as hepatitis, jaundice, and tuberous lymphadenitis in oriental medicine. However, its effect on adipogenesis has not yet been studied. In this study, we investigated the effects of R. sceleratus on adipogenesis in 3T3-L1 cells. Methods: Cells were treated with 50, 100, and 200 ㎍/ml of R. sceleratus and cell viability was evaluated. To differentiate the 3T3-L1 preadipocytes, a 3-isobutyl-1-methylxanthine, dexamethasone, and insulin (MDI) solution were used. The accumulation of lipid droplets was determined by Oil Red O staining. The expression levels of adipogenesis-related proteins were also determined. Results: MDI solution differentiated the preadipocytes into adipocytes and accumulation of lipids was observed in the differentiated 3T3-L1 cells. Interestingly, the amount of lipid droplets was reduced after R. sceleratus treatment. In addition, the expression levels of key adipogenic transcription factors, such as CCAAT/enhancer-binding proteins-𝛼 (C/EBP-𝛼) and peroxisome proliferator-activated receptors-𝛾 (PPAR-𝛾) were also reduced after R. sceleratus treatment. Furthermore, R. sceleratus increased AMP-activated kinase (AMPK) phosphorylation and decreased sterol regulatory element-binding protein-1 expression. Conclusions: Our results showed that R. sceleratus reduced preadipocyte differentiation by inhibiting C/EBP-𝛼 and PPAR-𝛾 levels via the AMPK pathway. Therefore, we suggest that R. sceleratus may be potentially used as an anti-adipogenic agent.

Comparison of Inflammatory Response and Myocardial injury Between Normoxic and Hyperoxic Condition during Cardiopulmonary Bypass (체외순환 시 정상 산소분압과 고 산소분압의 염증반응 및 심근손상에 관한 비교연구)

  • 김기봉;최석철;최국렬;정석목;최강주;김양원;김병훈;이양행;조광현
    • Journal of Chest Surgery
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    • v.34 no.7
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    • pp.524-533
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    • 2001
  • Background: Hyperoxemic cardiopulmonary bypass (CPB) has been recognized as a safe technique and is widely used in cardiac surgery. However, hyperoxemic CPB may produce higher toxic oxygen species and cause more severe oxidative stress and ischemia/reperfusion injury than normoxemic CPB. This study was undertaken to compare inflammatory responses and myocardial injury between normoxemic and hyperoxemic CPB and to examine the beneficial effect of normoxemic CPB. Material and method: Thirty adult patients scheduled for elective cardiac surgery were randomly divided into normoxic group (n=15), who received normoxemic CPB (about Pa $O_{2}$ 120 mmHg), and hyperoxic group (n=15), who received hyperoxemic CPB (about Pa $O_{2}$ 400 mmHg). Myeloperoxidase (MPO), malondialdehyde (MDA), adenosine monophosphate (AMP), and troponin-T (TnT) concentrations in coronary sinus blood were determined at pre- and post-CPB. Total leukocyte and neutrophil counts in arterial blood were measured at the before, during, and after CPB. Lactate concentration in mixed venous blood was analyzed during CPB, and cardiac index (Cl) and pulmonary vascular

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Implementation of a High Speed Comparator for High Speed Automatic Test Equipment (고속 자동 테스트 장비용 비교기 구현)

  • Cho, In-Su;Lim, Shin-Il
    • Journal of Korea Society of Industrial Information Systems
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    • v.19 no.3
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    • pp.1-7
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    • 2014
  • This paper describes the implementation of high speed comparator for the ATE (automatic test equipment) system. The comparator block is composed of continuous comparator, differential difference amplifier(DDA) and output stage. For the wide input dynamic range of 0V to 5V, and for the high speed operation (1~800MHz), high speed rail-to-rail amplifier is used in the first stage. And hysteresis circuits, pre-amp and latch are followed for high speed operation. To measure the difference of output signals between the two devices under test (DUTs), a DDA is applied because it can detect the differences of both common signals and differential signals. This comparator chip was implemented with $0.18{\mu}m$ BCDMOS process and can compare the signal difference of 5mV up to the frequency range of 800 MHz. The chip area of the comparator is $620{\mu}m{\times}830{\mu}m$.

Miniature PZT actuated microdrive for chronic neural recording in small animals (신경신호 기록을 위한 PZT기반 마이크로 드라이브)

  • Park, Sang-Kyu;Park, Hyun-Jun;Park, Suk-Ho;Kim, Byung-Kyu;Shin, Hee-Sub;Lee, Suk-Chan;Kim, Hui-Su;Kim, Eun-Tai
    • Proceedings of the KIEE Conference
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    • 2005.10b
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    • pp.38-40
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    • 2005
  • Microdrive with high precision and light mass enough to install on mouse head was fabricated for recording the reliable signal of neuron cell to understand the brain study. The proposed microdrive has three H-form PZT actuators and its guide structure. The microdrive operation principle is based on the well known inchworm principle. The synchronization of three PZT actuators is able to produce the linear motion along the guide structure. Our proposed microdrive has a precise accuracy of about 100nm and a long stroke of about 5mm. The electrode which is used for the recording of the action potential of the neuron cell was fixed at one of PZT actuators. The proposed microdrive was suited to acquisition of signals from in vivo extra-cellular single-unit recoding. On the condition of the anesthetized mouse, the single-unit signals could be recorded by using the proposed microdrive. In addition, applying the PZT microdrive to an alert mouse, we try to implant it on a mouse brain skull to explore single neuron firing.

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Novel GPR43 Agonists Exert an Anti-Inflammatory Effect in a Colitis Model

  • Park, Bi-Oh;Kang, Jong Soon;Paudel, Suresh;Park, Sung Goo;Park, Byoung Chul;Han, Sang-Bae;Kwak, Young-Shin;Kim, Jeong-Hoon;Kim, Sunhong
    • Biomolecules & Therapeutics
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    • v.30 no.1
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    • pp.48-54
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    • 2022
  • GPR43 (also known as FFAR2), a metabolite-sensing G-protein-coupled receptor stimulated by short-chain fatty acid (SCFA) ligands is involved in innate immunity and metabolism. GPR43 couples with Gαi/o and Gαq/11 heterotrimeric proteins and is capable of decreasing cyclic AMP and inducing Ca2+ flux. The GPR43 receptor has additionally been shown to bind β-arrestin 2 and inhibit inflammatory pathways, such as NF-κB. However, GPR43 shares the same ligands as GPR41, including acetate, propionate, and butyrate, and determination of its precise functions in association with endogenous ligands, such as SCFAs alone, therefore remains a considerable challenge. In this study, we generated novel synthetic agonists that display allosteric modulatory effects on GPR43 and downregulate NF-κB activity. In particular, the potency of compound 187 was significantly superior to that of pre-existing compounds in vitro. However, in the colitis model in vivo, compound 110 induced more potent attenuation of inflammation. These novel allosteric agonists of GPR43 clearly display anti-inflammatory potential, supporting their clinical utility as therapeutic drugs.

The CsSTE50 Adaptor Protein in Mitogen-Activated Protein Kinase Cascades Is Essential for Pepper Anthracnose Disease of Colletotrichum scovillei

  • Jong-Hwan, Shin;Byung-Seong, Park;Kyoung Su, Kim
    • The Plant Pathology Journal
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    • v.38 no.6
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    • pp.593-602
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    • 2022
  • Anthracnose, caused by the ascomycete fungus Colletotrichum scovillei, is a destructive disease in pepper. The fungus germinates and develops an infection structure called an appressorium on the plant surface. Several signaling cascades, including cAMP-mediated signaling and mitogen-activated protein kinase (MAPK) cascades, are involved in fungal development and pathogenicity in plant pathogenic fungi, but this has not been well studied in the fruit-infecting fungus C. scovillei. Ste50 is an adaptor protein interacting with multiple upstream components to activate the MAPK cascades. Here, we characterized the CsSTE50 gene of C. scovillei, a homolog of Magnaporthe oryzae MST50 that functions in MAPK cascades, by gene knockout. The knockout mutant ΔCsste50 had pleiotropic phenotypes in development and pathogenicity. Compared with the wild-type, the mutants grew faster and produced more conidia on regular agar but were more sensitive to osmotic stress. On artificial and plant surfaces, the conidia of the mutant showed significantly reduced germination and failed to form appressoria. The mutant was completely non-pathogenic on pepper fruits with or without wounds, indicating that pre-penetration and invasive growth were both defective in the mutant. Our results show that the adaptor protein CsSTE50 plays a role in vegetative growth, conidiation, germination, appressorium formation, and pathogenicity in C. scovillei.