• Title, Summary, Keyword: AP matrix

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Formulation Design of Sustained-Release Matrix Tablets Containing 4-Aminopyridine (유드라짓과 알긴산 나트륨 매트릭스를 이용한 4-Aminopyridine의 서방성 제제설계)

  • Kim, Jeong-Soo;Kim, Dong-Woo;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.6
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    • pp.453-460
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    • 2005
  • 4-Aminopyridine (AP) is a potassium channel blocker used in the treatment of neurological disorders such as multiple sclerosis and Alzheimer disease. AP‘s window of therapeutic effect appears to correlate with its plasma halflife (3.5 hours). It demonstrates pH-dependent solubility because of a weakly basic drug. In addition, the resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study is to design sustained release matrix tablet containing AP, overcoming this problem. $Eudragit^{\circledR}$ L 100 (EuL) and sodium alginate were used in an effort to achieve pH independent drug release. The effect of sodium alginate and EuL on drug release from matrix tablet was investigated. The drug release behavior from the different tablets was analyzed by $t_{20%},\;t_{40%},\;t_{60%}$, The exponential diffusion coefficient n, kinetic constant K were calculated according to the Korsmeyer-Peppas equation. The drug release from matrix tablets prepared with sodium alginate was decreased with increasing the content of sodium alginate in pH 7.4 while there is no significant difference in pH 1.2. The exponent n values were determined to be approximately 0.5 and 0.8 respectively, in both pH 1.2 and 7.4. These values indicate diffusion-based anomalous mechanism and erosion-based anomalous mechanism, respectively. The drug release from sodium alginate matrix tablets prepared with solid dispersion of EuL containing drug showed a slow drug release in an acidic medium and a more fast drug release in phosphate medium, compared with sodium alginate matrix tablets prepared with physical mixture. These results may be attributed to the gel forming ability of sodium alginate and pH dependent solubility of EuL. Therefore, sustained-release AP matrix tablets using sodium alginate and EuL were successfully prepared.

Baicalein Attenuates Oxidative Stress-Induced Expression of Matrix Metalloproteinase-1 by Regulating the ERK/JNK/AP-1 Pathway in Human Keratinocytes

  • Kim, Ki-Cheon;Kang, Sam-Sik;Lee, Jong-Sung;Park, Deok-Hoon;Hyun, Jin-Won
    • Biomolecules & Therapeutics
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    • v.20 no.1
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    • pp.57-61
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    • 2012
  • The matrix metalloproteinase (MMP) family is involved in the breakdown of the extracellular matrix during normal physiological processes such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes such as pathological aging, arthritis, and metastasis. Oxidative conditions generate reactive oxygen species (ROS) (e.g., hydrogen peroxide [$H_2O_2$]) in cells, which subsequently induce the synthesis of matrix metalloproteinase-1 (MMP-1). MMP-1, an interstitial collagenase, in turn stimulates an aging phenomenon. In this study, baicalein (5,6,7-trihydroxyfl avone) was investigated for its in vitro activity against $H_2O_2$-induced damage using a human skin keratinocyte model. Baicalein pretreatment signifi cantly inhibited $H_2O_2$-induced up-regulation of MMP-1 mRNA, MMP-1 protein expression and MMP-1 activity in cultured HaCaT keratinocytes. In addition, baicalein decreased the transcriptional activity of activator protein-1 (AP-1) and the expression of c-Fos and c-Jun, both components of the heterodimeric AP-1 transcription factor. Furthermore, baicalein reduced phosphorylation of extracellular signal-regulated kinase (ERK) and c-Jun-N-terminal kinase (JNK), which are upstream of the AP-1 transcription factor. The results of this study suggest that baicalein is involved in the inhibition of oxidative stress-induced expression of MMP-1 via inactivation of the ERK/JNK/AP-1 signaling pathway.

Pyrite Content using Quantitative X-Ray Diffraction Analysis and Its Application to Prediction of Acid Rock Drainage (정량 X-선회절분석을 이용한 황철석 함량 결정과 산성 암반 배수 발생 평가에의 응용)

  • Chon, Chul-Min;Kim, Jae-Gon;Lee, Gyoo-Ho
    • Journal of the Mineralogical Society of Korea
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    • v.19 no.2
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    • pp.71-80
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    • 2006
  • We examined the mineralogical composition of pyrite-bearing rocks by quantitative powder X-ray diffraction analysis using the matrix-flushing method and ROCKJOCK (a full pattern fitting computer program). The neutralization potential (NP) and acid generating potential (AP) were calculated on the basis of mineralogical compositions. The mineralogical AP was compared with the conventional AP calculated from bulk sulfur concentration to assess the applicability to the prediction of acid rock drainage(ARD). The pyrite content calculated by matrix-flushing method showed a high positive correlation($r^2$=0.95) with those by ROCKJOCK. The pyrite contents by matrix-flushing method was 1.45 times larger than those by ROCKJOCK. The pyrite content and mineralogical AP obtained by the matrix-flushing method had a better correlation($r^2$=0.98) with those by the total sulfur concentrations in the all samples except KB sample. The mineralogical NPs of YJ sample were 23.0 and 34.0(kg $CaCO_3$ equivalent per tonne) by matrix-flushing method and ROCKJOCK, respectively. The AP calculated by matrix-flushing method and ROCKJOCK program were 47% and 72% of those by the conventional ABA test. We hereby suggested that the quantitative analysis using XRD data can be applied to prediction of ARD. For more reliable calculation of the mineralogical NP and AP, other sulfide and carbonate minerals such as pyrrhotite, dolomite, ankerite, siderite, rhodochrosite which can affact the mineralogical NP and AP should be considered.

Performance Improvement of the Smart Antenna Placed in Wi-Fi Access Point (와이파이AP 용 FFT 전단 스마트안테나의 성능 개선)

  • Hong, Young-Jin
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.14 no.5
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    • pp.2437-2442
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    • 2013
  • OFDM Wi-Fi AP is susceptible to the co-channel interference. As a countermeasure, the insertion of a smart has been addressed. Despite of the guaranteed efficiency, the complexity of the post-FFT algorithm often keeps itself from being selected as the countermeasure. Instead, simply constructed pre-FFT smart antenna of which the algorithm is based on the received signal covariance matrix is commonly used and the mathematical modeling of it has been deployed. Computer simulations evaluating the improved BER characteristics of the proposed pre-FFT using the covariance matrix of channel estimator output have been carried out. It has been demonstrated that channel matrix output based smart antenna is superior to that using received signal covariance matrix.

Convergence Analysis of Noise Robust Modified AP(affine projection) Algorithm

  • Kim, Hyun-Tae;Park, Jang-Sik
    • Journal of information and communication convergence engineering
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    • v.8 no.1
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    • pp.23-28
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    • 2010
  • According to increasing projection order, the AP algorithm bas noise amplification problem in large background noise. This phenomenon degrades the performances of the AP algorithm. In this paper, we analyze convergence characteristic of the AP algorithm and then suggest a noise robust modified AP algorithm for reducing this problem. The proposed algorithm normalizes the update equation to reduce noise amplification of AP algorithm, by adding the multiplication of error power and projection order to auto-covariance matrix of input signal. By computer simulation, we show the improved performance than conventional AP algorithm.

Effect of Sulforaphane on LPS-Induced Matrix Metalloproteinase-9 (MMP-9) Expression (Sulfolaphane이 lipopolysaccharide (LPS)에 의해 유도된 matrix metalloproteinase-9 (MMP-9) 발현에 미치는 영향)

  • Lee, Jung-Tae;Woo, Kyung-Jin;Kwon, Taeg-Kyu
    • Journal of Life Science
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    • v.20 no.2
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    • pp.275-280
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    • 2010
  • Sulforaphane is a naturally occurring member of the iosothiocyanate family, which reveals chemopreventive capacities including anti-cancer, anti-inflammation and inhibition of MMP-9 activities. In this study, we investigated the effect of sulforaphane on the expression of matrix metalloproteinase-9 (MMP-9) in lipopolysaccharide (LPS)-induced Raw 264.7 cells. Sulforaphane strikingly suppressed the LPS-induced MMP-9 activity and mRNA expression in a dose-dependent manner. In addition, sulforaphane inhibited not only the LPS-induced MMP-9 promoter activity but also LPS-mediated activator protein-1 (AP-1) and nuclear factor-kB (NF-${\kappa}B$) promoter activity. Transient transfection by MMP-9 constructs, in which specific transcriptional factors were mutagenized, indicated that the effects of LPS and sulforaphane were mediated via AP-1 and NF-${\kappa}B$ response elements. We found that sulforaphane had the ability to suppress LPS-induced invasion in vitro. Taken together, these results demonstrated that sulforaphane effectively suppressed LPS-induced MMP-9 expression via modulation of promoter elements (AP-1 and NF-${\kappa}B$) in MMP-9 transcriptional activation.

Simple and Direct Quantitative Analysis for Quinidine Drug in Fish Tissues

  • Chen, Yuan-Chin;Abdelhamid, Hani Nasser;Wu, Hui-Fen
    • Mass Spectrometry Letters
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    • v.8 no.1
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    • pp.8-13
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    • 2017
  • Analysis of quinidine for fish tissues using single drop microextraction (SDME) coupled with atmospheric pressure matrix assisted laser desorption/ionization mass spectrometry (AP-MALDI-MS) are reported. Optimization conditions; such as extraction solvent, extraction time, pH of the aqueous solution, salt additions (NaCl), stirring rate, matrix type and concentration are investigated. Linear dynamic range (${\mu}M$), limit of detection, relative recovery%, and enrichment factor are 0.08-9.2, 0.05, $94.8{\pm}3.1-98.5{\pm}3.3%$, $4.34{\pm}0.28-4.40{\pm}0.30$, respectively. SDME-AP-MALDI-MS shows good intraday and interday reproducibility.

VLSI Implementation for the MPDSAP Adaptive Filter

  • Choi, Hun;Kim, Young-Min;Ha, Hong-Gon
    • Journal of the Institute of Convergence Signal Processing
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    • v.11 no.3
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    • pp.238-243
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    • 2010
  • A new implementation method for MPDSAP(Maximally Polyphase Decomposed Subband Affine Projection) adaptive filter is proposed. The affine projection(AP) adaptive filter achieves fast convergence speed, however, its implementation is so expensive because of the matrix inversion for a weight-updating of adaptive filter. The maximally polyphase decomposed subband filtering allows the AP adaptive filter to avoid the matrix inversion, moreover, by using a pipelining technique, the simple subband structured AP is suitable for VLSI implementations concerning throughput, power dissipation and area. Computer simulations are presented to verify the performance of the proposed algorithm.

Crotonis Fructus Extract Inhibits 12-O-Tetradecanoylphorbol-13-Acetate-Induced Expression of Matrix Metalloproteinase-9 via the Activator Protein-1 Pathway in MCF-7 Cells

  • Song, Hyun-Kyung;Lee, Guem-San;Park, Sueng Hyuk;Noh, Eun-Mi;Kim, Jeong-Mi;Ryu, Do-Gon;Jung, Sung Hoo;Youn, Hyun Jo;Lee, Young-Rae;Kwon, Kang-Beom
    • Journal of Breast Cancer
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    • v.20 no.3
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    • pp.234-239
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    • 2017
  • Purpose: Metastatic cancers spread from the primary site of origin to other parts of the body. Matrix metalloproteinase-9 (MMP-9) is essential in metastatic cancers owing to its major role in cancer cell invasion. Crotonis fructus (CF), the mature fruits of Croton tiglium L., have been used for the treatment of gastrointestinal disturbance in Asia. In this study, the effect of the ethanol extract of CF (CFE) on MMP-9 activity and the invasion of 12-O-tetradecanoylphorbol-13-acetate (TPA)-treated MCF-7 cells was examined. Methods: The cell viability was evaluated using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. The expression of MMP-9 was examined by Western blotting, zymography, and real-time polymerase chain reaction. An electrophoretic mobility gel shift assay was performed to detect activator protein-1 (AP-1) DNA binding activity and cell invasiveness was measured by an in vitro Matrigel invasion assay. Results: CFE significantly suppressed MMP-9 expression and activation in a dose-dependent manner. Furthermore, CFE attenuated the TPA-induced activation of AP-1. Conclusion: The results indicated that the inhibitory effects of CFE against TPA-induced MMP-9 expression and MCF-7 cell invasion were dependent on the protein kinase C ${\delta}$/p38/c-Jun N-terminal kinase/AP-1 pathway. Therefore, CFE could restrict breast cancer invasiveness owing to its ability to inhibit MMP-9 activity.

Diphlorethohydroxycarmalol Suppresses Ultraviolet B-Induced Matrix Metalloproteinases via Inhibition of JNK and ERK Signaling in Human Keratinocytes

  • Piao, Mei Jing;Kumara, Madduma Hewage Susara Ruwan;Kim, Ki Cheon;Kang, Kyoung Ah;Kang, Hee Kyoung;Lee, Nam Ho;Hyun, Jin Won
    • Biomolecules & Therapeutics
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    • v.23 no.6
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    • pp.557-563
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    • 2015
  • Skin aging is the most readily observable process involved in human aging. Ultraviolet B (UVB) radiation causes photo-oxidation via generation of reactive oxygen species (ROS), thereby damaging the nucleus and cytoplasm of skin cells and ultimately leading to cell death. Recent studies have shown that high levels of solar UVB irradiation induce the synthesis of matrix metalloproteinases (MMPs) in skin fibroblasts, causing photo-aging and tumor progression. The MMP family is involved in the breakdown of extracellular matrix in normal physiological processes such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes such as arthritis and metastasis. We investigated the effect of diphlorethohydroxycarmalol (DPHC) against damage induced by UVB radiation in human skin keratinocytes. In UVB-irradiated cells, DPHC significantly reduced expression of MMP mRNA and protein, as well as activation of MMPs. Furthermore, DPHC reduced phosphorylation of ERK and JNK, which act upstream of c-Fos and c-Jun, respectively; consequently, DPHC inhibited the expression of c-Fos and c-Jun, which are key components of activator protein-1 (AP-1, up-regulator of MMPs). Additionally, DPHC abolished the DNA-binding activity of AP-1, and thereby prevented AP-1-mediated transcriptional activation. These data demonstrate that by inactivating ERK and JNK, DPHC inhibits induction of MMPs triggered by UVB radiation.