• Title/Summary/Keyword: Protection IC

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Inhibition of Human Leukocyte Cathepsin G by NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) (NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)에 의한 사람 중성구 Cathepsin G의 활성도 억제)

  • Bae, Sung-Jun;Ghim, Sa-Youl;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.26 no.1
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    • pp.51-54
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    • 1990
  • Human leukocyte cathepsin-Gs are active participant in the active phase of inflammations like rheumatoid arthritis, emphysema and glomerular injury. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for treatment of these inflammatory diseases. Mechanism of action of NSAIDs for treatment of inflammatory diseases, especially like rheumatoid arthritis, are known as the inhibitors of prostaglandin synthesis. Inhibitions of the activities of human leukocyte cathepsin-Gs by non-steroidal anti-inflammatory drugs, however, were not same as the known pharmacological effects (inhibition of cyclooxygenase) of these drugs. Among them, especially, sulindac, salicylate, phenylbutazone, oxyphenbutazone, and salicyluric acid inhibited human leukocyte cathepsin-Gs effectively. $IC_{50}s$ of each drug were 4.3mM, 14.3mM, 6.5mM, 11mM and 15mM respectively. The drugs which have same chemical structure and same degree of inhibition effect on cyclooxygenase showed different degree or no effect on inhibition of cathepsin G. These inhibition effect might be, beside of inhibition of cyclooxygenase in the prostaglandin synthesis pathway, another benefitial antiinflammatory effect of NSAIDs by direct protection against tissue destruction in inflammatory diseases.

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BMS-191095, a Cardioselective Mitochondrial $K_{ATP}$ Opener, Inhibits Human Platelet Aggregation by Opening Mitochondrial $K_{ATP}$ Channels

  • Cho Mi-Ra;Park Jung-Wook;Jung In-Sang;Yi Kyu-Yang;Yoo Sung-Eun;Chung Hun-Jong;Yun Yeo-Pyo;Kwon Suk-Hyung;Shin Hwa-Sup
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.61-67
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    • 2005
  • We evaluated the antiplatelet effects of two classes of ATP-sensitive potassium channel openers $(K_{ATP}\;openers)$ on washed human platelets, and the study's emphasis was on the role of mitochondrial $K_{ATP}$ in platelet aggregation. Collagen-induced platelet aggregation was inhibited in a dose dependent manner by lemakalim and SKP-450, which are potent cardio-nonselective $K_{ATP}$ openers, and also by cardioselective BMS-180448 and BMS-191095 $(IC_{50}\;:\;1,130,\;>\;1,500,\;305.3\;and\;63.9\;{\mu}M,\;respectively)$, but a significantly greater potency was noted for the cardioselective $K_{ATP}$ openers. The latter two $K_{ATP}$ openers also inhibited platelet aggregation induced by thrombin, another important blood-borne platelet activator, with similar rank order of potency $(IC_{50}\;:\;498.0\;and\;104.8{\mu}M\; for\;BMS-180448\;and\;BMS-191095,\;respectively)$. The inhibitory effects of BMS-191095 on collagen-induced platelet aggregation were significantly blocked by a 30-min pretreatment of platelets with glyburide $(1{\mu}M)$ or sodium 5-hydroxyde­canoate$(5-HD,\;100{\mu}M)$, a nonselective and selective mitochondrial $K_{ATP}$ antagonist, respectively, at similar magnitudes; this indicates the role of mitochondrial $K_{ATP}$ in the antiplatelet activity of BMS-191095. However, glyburide and 5-HD had no effect when they were added to the platelet cuvette immediately prior to the addition of BMS-191095. These findings indicate that cardioselective mitochondrial $K_{ATP}$ openers like BMS-191095 are able to exert cardioprotective effects in cardiac ischemia/reperfusion injury via dual mechanisms directed at the inhibition of platelet aggregation and the protection of cardiomyocytes, and both these mechanisms are mediated by mitochondrial$K_{ATP}$.

Quality Characteristics and Antioxidant Activities of Noodles Added with Rehmanniae Radix Preparata Powder (숙지황 분말을 첨가한 국수의 품질 특성 및 항산화성)

  • Min, A Young;Son, Ah Young;Kim, Hyun Jeong;Shin, Suk Kyung;Kim, Mee Ree
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.3
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    • pp.386-392
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    • 2015
  • The purpose of this study was to evaluate the quality characteristics and antioxidant activities of noodles added with Rehmanniae Radix Preparata powder (RP). Wheat flour noodles were prepared with four levels of RP (0, 2.5, 5, and 7.5%). Moisture absorption of RP added noodles was somewhat greater than that of control. The turbidity of RP noodles decreased according to addition of RP. Hunter L (lightness) and b (yellowness) values of RP added noodles decreased according to addition of RP amount. Textural properties (measured by a texture analyzer), hardness, and springiness of RP noodles up to 5% were not significantly different from those of control. Antioxidant activity of RP added noodles increased according to addition of RP: $IC_{50}$ values of DPPH radical scavenging activity for raw noodles was 3.77 mg/g, whereas values of raw noodles with RP 2.5 and 7.5% were 3.69 mg/g and 2.47 mg/g, respectively. Polyphenol content increased according to addition of RP. Amylogram showed that RP addition increased initial gelatinization temperature, decreased breakdown, and reduced setback and consistency, which indicates protection against retrogradation. The sensory preference test revealed that cooked noodles with added 2.5% RP showed the highest scores for color, odor, taste, and overall preference. It is suggested that RP up to 2.5% could be substituted for wheat flour to improve noodle quality.

An On-chip ESD Protection Method for Preventing Current Crowding on a Guard-ring Structure (가드링 구조에서 전류 과밀 현상 억제를 위한 온-칩 정전기 보호 방법)

  • Song, Jong-Kyu;Jang, Chang-Soo;Jung, Won-Young;Song, In-Chae;Wee, Jae-Kyung
    • Journal of the Institute of Electronics Engineers of Korea SD
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    • v.46 no.12
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    • pp.105-112
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    • 2009
  • In this paper, we investigated abnormal ESD failure on guard-rings in the smart power IC fabricated with $0.35{\mu}m$ Bipolar-CMOS-DMOS (BCD) technology. Initially, ESD failure occurred below 200 V in the Machine Model (MM) test due to current crowding in the parasitic diode associated with the guard-rings which are generally adopted to prevent latch-up in high voltage devices. Optical Beam Induced Resistance Charge (OBIRCH) and Scanning Electronic Microscope (SEM) were used to find the failure spot and 3-D TCAD was used to verify cause of failure. According to the simulation results, excessive current flows at the comer of the guard-ring isolated by Local Oxidation of Silicon (LOCOS) in the ESD event. Eventually, the ESD failure occurs at that comer of the guard-ring. The modified comer design of the guard-ring is proposed to resolve such ESD failure. The test chips designed by the proposed modification passed MM test over 200 V. Analyzing the test chips statistically, ESD immunity was increased over 20 % in MM mode test. In order to avoid such ESD failure, the automatic method to check the weak point in the guard-ring is also proposed by modifying the Design Rule Check (DRC) used in BCD technology. This DRC was used to check other similar products and 24 errors were found. After correcting the errors, the measured ESD level fulfilled the general industry specification such as HBM 2000 V and MM 200V.

Anti-thrombic Properties of the Oriental Herbal Medicine, Daejowhan

  • Chang Gyu-Tae;Kim Jang-Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.5
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    • pp.1391-1398
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    • 2005
  • The anti-thrombic properties of the oriental herbal medicine Daejowhan(DJW, 大造丸) which consists of 11 kinds of herbs (indicated as ratio) of Rehmanniae Radix 24%, Hominis Placenta 5%, Testudinis Carapax 9%, Eucommiae Cortex 9%, Asparagi Radix 9%, Phellodendri Cortex 9%, Achyranthis Radix 7%, Liriopis Tuber 7%, Angelicae Sinensis Radix 7%, Ginseng Radix 5% and Schizandrae Fructus 3% were investigated. The water extracts from DJW inhibited Platelet-activating factor(PAF) induced platelet aggregation. DJW was extracted with methanol and further fractionated by ethylacetate. A 70% methanol extract showed a strong inhibition against PAF-induced aggregation in vitro and in vivo assays. The ethylacetate soluble fraction was shown to have inhibitory effect on PAF-induced platelet aggregation in vitro assay. The ethylacetate soluble fraction specially protected against the lethality of PAF, while verapamil did not afford any protection. These results indicate that the water extracts and alcoholic-fractions inhibit the action of PAF in vivo by an antagonistic effect on PAF, so that it may be useful in treating disorders caused by PAF, such as acute allergy, inflammation, asthma, gastrointestinal ulceration, toxic shock and so forth. DJW was investigated regarding its assumed anti-thrombic action on human platelets which was deduced from its ability to suppress Arachidonic acid(AA)-induced aggregation, exocytosis of ATP, and inhibition of Cyclooxygenase(COX) and Thromboxane synthase(TXS) activity. The latter two effects were estimated from the generation of Prostaglandin $E_2(PGE_2)$ and Thromboxane $A_2(TXA_2)$ respectively. Exogenously applied AA ($100{\mu}mol/{\ell}$) provoked a $89\%$ aggregation of platelets, the release of 14 pmol ATP, and the formation of either 225 pg $TXA_2$ or 45 pg $PGE_2$, each parameter being related to 106 platelets. An application of DJW 5 min before AA dose-dependently diminished aggregation, ATP-release and the synthesis of $TXA_2$ and $PGE_2$ with $IC_{50}$ values of 74, 108, 65, $72{\mu}g/m{\ell}$, respectively. The similarity of the $IC_{50}$ values suggest an inhibition of COX by DJW as primary target, thus suppressing the generation of $TXA_2$ which induces aggregation of platelets and exocytosis of ATP by its binding on $TXA_2$-receptors.

Automatic On-Chip Glitch-Free Backup Clock Changing Method for MCU Clock Failure Protection in Unsafe I/O Pin Noisy Environment (안전하지 않은 I/O핀 노이즈 환경에서 MCU 클럭 보호를 위한 자동 온칩 글리치 프리 백업 클럭 변환 기법)

  • An, Joonghyun;Youn, Jiae;Cho, Jeonghun;Park, Daejin
    • Journal of the Institute of Electronics and Information Engineers
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    • v.52 no.12
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    • pp.99-108
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    • 2015
  • The embedded microcontroller which is operated by the logic gates synchronized on the clock pulse, is gradually used as main controller of mission-critical systems. Severe electrical situations such as high voltage/frequency surge may cause malfunctioning of the clock source. The tolerant system operation is required against the various external electric noise and means the robust design technique is becoming more important issue in system clock failure problems. In this paper, we propose on-chip backup clock change architecture for the automatic clock failure detection. For the this, we adopt the edge detector, noise canceller logic and glitch-free clock changer circuit. The implemented edge detector unit detects the abnormal low-frequency of the clock source and the delay chain circuit of the clock pulse by the noise canceller can cancel out the glitch clock. The externally invalid clock source by detecting the emergency status will be switched to back-up clock source by glitch-free clock changer circuit. The proposed circuits are evaluated by Verilog simulation and the fabricated IC is validated by using test equipment electrical field radiation noise

Differentially Expressed Genes by Methylmercury in Neuroblastoma cell line using suppression subtractive hybridization (SSH) and cDNA Microarray

  • Kim, Youn-Jung;Chang, Suk-Tai;Yun, Hye-Jung;Ryu, Jae-Chun
    • Proceedings of the Korea Society of Environmental Toocicology Conference
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    • 2003.05a
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    • pp.187-187
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    • 2003
  • Methylmercury (MeHg), one of the heavy metal compounds, can cause severe damage to the central nervous system in humans. Many reports have shown that MeHg is poisonous to human body through contaminated foods and has released into the environment. Despite many studies on the pathogenesis of MeHg-induced central neuropathy, no useful mechanism of toxicity has been established so far. In this study, two methods, cDNA Microarray and SSH, were performed to assess the expression profile against MeHg and to identify differentially expressed genes by MeHg in neuroblastoma cell line. TwinChip Human-8K (Digital Genomics) was used with total RNA from SH-SY5Y (human neuroblastoma cell line) treated with solvent (DMSO) and 6.25 uM (IC50) MeHg. And we performed forward and reverse SSH method on mRNA derived from SH-SY5Y treated with DMSO and MeHg (6.25 uM). Differentially expressed cDNA clones were sequenced and were screened by dot blot and ribonuclease protection assay to confirm that individual clones indeed represent differentially expressed genes. These sequences were identified by BLAST homology search to known genes or expressed sequence tags (ESTs). Analysis of these sequences may provide an insight into the biological effects of MeHg in the pathogenesis of neurodegenerative disease and a possibility to develop more efficient and exact monitoring system of heavy metals as environmental pollutants.

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Fractionation and Characterization of Fractions with High Antioxidative Activity from the Gelatin Hydrolysates of Korean Rockfish Sebastes schlegelii Skin

  • Kim, Hyung-Jun;Park, Kwon-Hyun;Shin, Jun-Ho;Lee, Ji-Sun;Heu, Min-Soo;Lee, Dong-Ho;Kim, Jin-Soo
    • Fisheries and Aquatic Sciences
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    • v.14 no.3
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    • pp.168-173
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    • 2011
  • The purpose of this study was to obtain a fraction with high antioxidative activity from second rockfish gelatin hydrolysates (SRSGHs), which were hydrolyzed with Alcalase and Flavourzyme through ultrafiltration membranes with serial digestions for 1 and 2 h, respectively, and to investigate the feasibility of this fraction as a potential functional food ingredient. Among various fractions that were ultrafiltered from the SRSGH with four types of membrane (1, 5, 10, and 30 kDa), the SRSGH-III fraction, which permeated the 10 kDa membrane but not the 5 kDa membrane, showed the highest antioxidant activity (protection factor=5.13) and angiotensin-I-converting enzyme-inhibiting activity ($IC_{50}$=0.82 mg/mL). These results suggest that the SRSGH-III fraction from the SRSGH can be used as a functional food ingredient. However, further studies examining its antioxidant activity in vivo as well as the different antioxidant mechanisms are needed.

Identification of Soluble Epoxide Hydrolase Inhibitors from the Seeds of Passiflora edulis Cultivated in Vietnam

  • Cuong, To Dao;Anh, Hoang Thi Ngoc;Huong, Tran Thu;Khanh, Pham Ngoc;Ha, Vu Thi;Hung, Tran Manh;Kim, Young Ho;Cuong, Nguyen Manh
    • Natural Product Sciences
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    • v.25 no.4
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    • pp.348-353
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    • 2019
  • Soluble epoxide hydrolases (sEH) are enzymes present in all living organisms, metabolize epoxy fatty acids to 1,2-diols. sEH in the metabolism of polyunsaturated fatty acids plays a key role in inflammation. In addition, the endogenous lipid mediators in cardiovascular disease are also broken down to diols by the action of sEH that enhanced cardiovascular protection. In this study, sEH inhibitory guided fractionation led to the isolation of five phenolic compounds trans-resveratrol (1), trans-piceatannol (2), sulfuretin (3), (+)-balanophonin (4), and cassigarol E (5) from the ethanol extract of the seeds of Passiflora edulis Sims cultivated in Vietnam. The chemical structures of isolated compounds were determined by the interpretation of NMR spectral data, mass spectra, and comparison with data from the literature. The soluble epoxide hydrolase (sEH) inhibitory activity of isolated compounds was evaluated. Among them, trans-piceatannol (2) showed the most potent inhibitory activity on sEH with an IC50 value of 3.4 μM. This study marks the first time that sulfuretin (3) was isolated from Passiflora edulis as well as (+)-balanophonin (4), and cassigarol E (5) were isolated from Passiflora genus.

Detection of Misfire in Car Engines using Walsh Discrete Fourier Transform (WDFT를 이용한 자동차 엔진의 실화검출)

  • 김종부;이태표;오정수;임국현
    • Journal of the Korean Institute of Telematics and Electronics T
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    • v.35T no.1
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    • pp.67-74
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    • 1998
  • The primary cause of air pollution by vehicles is imperfect combustion of fuel. One of the most usual causes of this imperfect combustion is the misfire in IC engins. The U.S. EPA(Environment Protection Agency) and the CARB(California air Resources Board) have imposed regulations for the detection of misfiring in automotive engines. The OBD-II regulations require that misfire should be monitored by the engine diagnostic system, and that the goal of OBD-II is to alert the driver to the presence of a malfunction of the emission control system. Several solutions to the misfire detection problem have been proposed for the detection of misfires. However, the performance of these methods in the presence of misfire is not altogether clear. This paper presents a precise method and system for internal combustion engine misfire. Present invention based upon measurements of engine roughness as derived from crankshaft angular velocity measurements with special signal processing method. Crankshaft angular velocity signals are processed by WDPT, so that the more reliable misfire detection than the time domain analysis. Experimental work confirms that it is possible to apply the WDFT for the detection of misfires in no-load idle and road testing.

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