• Title/Summary/Keyword: Ang II

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Anti-inflammatory Action of Phenolic Compounds from Gastrodia elata Root

  • Lee, Ji-Yun;Jang, Young-Woon;Kang, Hyo-Sook;Moon, Hee;Sim, Sang-Soo;Kim, Chang-Jong
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.849-858
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    • 2006
  • Previous screening of the pharmacological action of Gastrodia elata (GE) root (Orchidaceae) showed that methanol (MeOH) extracts have significant anti-inflammatory properties. The antiinflammatory agents of GE, however, remain unclear. In this experiment, MeOH extracts of GE were fractionated with organic solvents for the anti-inflammatory activity-guided separation of GE. Eight phenolic compounds from the ether (EtOEt) and ethyl acetate (EtOAc) fractions were isolated by column chromatography: 4-hydroxybenzaldehyde (I), 4-hydroxybenzyl alcohol (II), benzyl alcohol (III), bis-(4-hydroxyphenyl) methane (IV), 4(4'-hydroxybenzyloxy)benzyl-methylether (V), 4-hydroxy-3-methoxybenzyl alcohol (VI), 4-hydroxy-3-methoxybenzaldehyde (VII), and 4-hydroxy-3-methoxybenzoic acid (VIII). To investigate the anti-inflammatory and anti-oxidant activity of these compounds, their effects on carrageenan-induced paw edema, arachidonic acid (AA)-induced ear edema and analgesic activity in acetic acid (HAc)-induced writhing response were carried out in vivo; cyclooxygenase (COX) activity, reactive oxygen species (ROS) generation in rat basophilic leukemia (RBL 2H3) cells and 1,1-diphenyl-2-picryl-hydroazyl (DPPH) scavenging activity were determined in vitro. These phenolic compounds not only had anti-inflammatory and analgesic properties in vivo, but also inhibited COX activity and silica-induced ROS generation in a dose-dependent manner. Among these phenolic compounds, compound VII was the most potent anti-inflammatory and analgesic. Compound VII significantly inhibited silica-induced ROS generation and compound VI significantly increased DPPH radical scavenging activity. Compounds I, II and III significantly inhibited the activity of COX-I and II. These results indicate that phenolic compounds of GE are anti-inflammatory, which may be related to inhibition of COX activity and to anti-oxidant activity. Consideration of the structure-activity relationship of the phenolic derivatives from GE on the anti-inflammatory action revealed that both C-4 hydroxy and C-3 methoxy radicals of benzyl aldehyde play an important role in anti-inflammatory activities.

Variational Image Dehazing using a Fuzzy Membership Function

  • Park, Hasil;Park, Jinho;Kim, Heegwang;Paik, Joonki
    • IEIE Transactions on Smart Processing and Computing
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    • v.6 no.2
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    • pp.85-92
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    • 2017
  • This paper presents a dehazing method based on a fuzzy membership function and variational method. The proposed algorithm consists of three steps: i) estimate transmission through a pixel-based operation using a fuzzy membership function, ii) refine the transmission using an L1-norm-based regularization method, and iii) obtain the result of haze removal based on a hazy image formation model using the refined transmission. In order to prevent color distortion of the sky region seen in conventional methods, we use a trapezoid-type fuzzy membership function. The proposed method acquires high-quality images without halo artifacts and loss of color contrast.

Synthesis and $\beta$-lactamase inhibitory activity of 6-exomethylene penamsulfone derivatives-II (Synthesis of 6-exomethylene penamsulfone derivatives)

  • Park, Hee-Suk;Yoon, Sang-Bae;Chaeuk Im;Yim, Chul-Bu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.71-71
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    • 1997
  • $\beta$-lactamase를 생성하는 균들이 $\beta$-lactam계 항생제를 분해하여 불활성화 시키므로 이를 해결하기 위하여 그 효소에 대하여 억제활성을 나타내는 새로운 6-exomethylenepenamsulfone화합물들을 합성하였다. Dibromopenamsulfone과 heterocyclic ring을 함유한 thioethyl triazole-4-carboxaldehyde를 반응시키고, acetic anhydride와 Zn으로 처리하여 E-form과 Z-form의 6-exomethylene penmsulfones을 합성하였다. 이것을 AlCl$_3$로 처리하여 deprotection시킨 후, NaHCO$_3$로 처리하여 6-exomethylene penam sulfones의 Na-salt의 형태로 목적물질을 합성하였다.

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Synthesis and $\beta$-lactamase inhibitory activity of 6-exomethylene penamsulfone derivatives-III (In vitro $\beta$-lactamase inhibitory activity and comparative susceptibility test of 6-exomethylene penamsulfone derivatives)

  • Park, Hee-Suk;Yoon, Sang-Bae;Chaeuk Im;Yim, Chul-Bu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.72-72
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    • 1997
  • 합성한 5종의 6-Exomethylene penamsulfone 유도체의 Type I, Type II, Type III, TypeIV, TEM 효소에 대한 $\beta$-lactamase저해효과를 spectrophotometric assay방법으로 측정하였다. 또한 여기서 우수한 효소억제활성을 보여준 3종의 화합물을 가지고 In vitro antibacterial activity를 Agar dilution method법으로 27종의 $\beta$-lactamase생성균주에 대하여, Sulbactam, Ampicillin 및 Cefoperazone과 병용투여하여 MIC를 측정하였다.

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Flavonoids from Salix hallaisanensis Leaves (떡버들 잎의 플라보노이드)

  • Oh, Mi-Hyun;Ham, In-Hye;Chung, Sung-Hee;Whang, Wan-Kyun
    • Korean Journal of Pharmacognosy
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    • v.36 no.4 s.143
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    • pp.282-290
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    • 2005
  • The MeOH extract of the the leaves of Salix hallaisanensis (Salicaceae) was partitioned successively with $CHCl_3$, 20% MeOH, 40% MeOH and 60% MeOH solution. From the fractions obtained, 9 compounds were isolated, $diosmetin-7-O-{\beta}-d-glucoside$ (I), $diosmetin-7-O-{\beta}-D-glucosyl-(1{\rightarrow)6)-{\beta}-d-glucoside$ (II), $diosmetin-7-O-{\beta}-d-xylosyl-(1{\rightarrow}6)-{\beta}-D-glucoside$ (III), $quercetin-3-O-{\beta}-d-galactoside$ (hyperoside) (IV), $quercetin-3-O-{\alpha}-l-rhamnosyl-(1{\rightarrow}6)-{\beta}-D-glucoside(rutin)$ (V), luteolin (VI), $luteolin-7-O-{\beta}-d-glucoside$ (VII), $kaempferol-3-O-{\alpha}-l-rhamnosyl-(1{\rightarrow}6)-{\beta}-D-glucoside$ (VIII), and (+)-catechin (IX).

Pharmacological Studies on the Antihypertensive Effects of Cinnarizine Coadministered with Propranolol or Metoprolol(II) -Effects on the Isolated Smooth Muscle- (Cinnarizine을 Propranolol이나 Metoprolol과 병용할 때의 혈압(血壓) 강하(降下) 효과(效果)에 관한 약리학적(藥理學的) 연구(硏究)(II) -적출(摘出) 평활근(平滑筋)에 대한 효과-)

  • Huh, In-Hoi;Ann, Hyung-Soo
    • YAKHAK HOEJI
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    • v.28 no.5
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    • pp.257-263
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    • 1984
  • In our former report we observed that cinnarizine influenced the antihypertensive effect of propranolol beneficially, but not of metoprolol in SHR and normal cat. Cardiac contractilities and smooth muscle relaxations induced by above drugs were measured to elucidate their mechanism of action. In cinnarizine and propranolol treated group, both of negative inotropic and ${\beta}-blocking$ activity of propranolol in perfused rat hearts were increased and propranolol induced contraction in isolated arterial and trachea smooth muscle of the guinea pig was antagonized comparing to propranolol alone treated group. However, in the cinnarizine and metoprolol treated group, no significant differences in activity on the above were observed compared to metoprolol alone treated group.

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Pharmaceutical Studies on Esterification of Chloramphenicol with Antipyretics ( II ) (Chloramphenicol과 해열제(解熱劑)와의 Ester 화합물(化合物)에 관(關)한 약제학적(藥劑學的) 연구(硏究) ( II ))

  • Kim, Jung-Woo;Kim, Jong-Kap
    • Journal of Pharmaceutical Investigation
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    • v.14 no.2
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    • pp.76-85
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    • 1984
  • Antibiotic activity and antipyretic effect of three synthetic prodrugs, chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate(CAF-NAX) and chloramphenicol acetaminophen succinate (CAF-SUC-ACET), were studied in vitro and in vivo. In the experimental results, the CAF-NAX showed the moat rapid absorption and the highest blood levels, and the CAF-SUC-ACET and CAF-ASP also were more rapid absorption and higher blood levels than controls, chloramphenicol and chloramphenicol palmitate. The synthetic prodrugs also showed the antipyretic effect by modified Roszkowski method using endotoxin.

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The Study on Dissolution Rate of Polymorphs of Piperacillin Monohydrate (Piperacillin Monohydrate Polymorphs의 용출속도(溶出速度)에 관(關)한 연구(硏究))

  • Kim, Johng-Kap;Ur, Kyung-Nam
    • Journal of Pharmaceutical Investigation
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    • v.15 no.4
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    • pp.186-197
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    • 1985
  • Polymorphs of piperacillin monohydrate were prepared by various sedimentation methods from piperacillin base for the purpose of developing piperacillin preparations for oral use. Solubility and dissolution rate of each form of the polymorphs were compared with each other. It was found that Form IV showed the highest solubility and the fastest dissolution rate among four forms of polymorphs. In general, the solubility and dissolution rate of two amorphous forms, Form IV and II were higher than those of two crystal forms, Form I and III. The apparent dissolution rates in the artificial gastric juice within 60 minutes were $0.65{\times}10^{-6}mole{\cdot}min^{-1}\;cm^{-2}$ for From IV, $0.36{\times}10^{-6}mole{\cdot}min^{-1}{\cdot}cm^{-2}$ for From II, $0.30{\times}10^{-6}mole{\cdot}min^{-1}{\cdot}cm^{-2}$ for From III and $0.18{\times}10^{-6}mole{\cdot}min^{-1}{\cdot}cm^{-2}$ for From I, respectively.

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An Analysis on the Material Removal Mechanism of Chemical-Mechanical Polishing Process Part II: Dynamic Simulation (화학-기계적 연마 공정의 물질제거 메커니즘 해석 Part II: 동적 시뮬레이션)

  • Seok, Jong-Won;Oh, Seung-Hee
    • Journal of the Semiconductor & Display Technology
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    • v.6 no.3
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    • pp.1-6
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    • 2007
  • The integrated thermal-chemical-mechanical (TCM) material removal model presented in the companion paper is dynamically simulated in this work. The model is applied to a Cu CMP process for the simulation and the results of the three individual ingredients composing the model are presented separately first. These results are then incorporated to calculate the total material removal rate (MRR) of the Cu CMP. It is shown that the non-linear trend of MRR with respect to the applied mechanical power (i.e., non-Prestonian behavior), which is not well explained with the models established in principle on conventional contact mechanics, may be due to the chemical reaction(s) varying non-linearly with the temperature in the wafer.

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Simulation of optimal ion implantation for symmetric threshold voltage determination of 1 ${\mu}m$ CMOS device (1 ${\mu}m$ CMOS 소자의 대칭적인 문턱전압 결정을 위한 최적 이온주입 시뮬레이션)

  • Seo, Yong-Jin;Choi, Hyun-Sik;Lee, Cheol-In;Kim, Tae-Hyung;Kim, Chang-Il;Chang, Eui-Goo
    • Proceedings of the KIEE Conference
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    • 1991.11a
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    • pp.286-289
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    • 1991
  • We simulated ion implantation and annealing condition of 1 ${\mu}m$ CMOS device using process simulator, SUPREM-II. In this simulation, optimal condition of ion implantation for symmetric threshold voltage determination of PMOS and NMOS region, junction depth and sheet resistance of source/drain region, impurity profile of each region are investigated. Ion implantation dose for 3 ${\mu}m$ N-well junction depth and symmetric threshold voltage of $|0.6|{\pm}0.1$ V were $1.9E12Cm^{-2}$(for phosphorus), $1.7E122Cm^{-2}$(for boron) respectively. Also annealing condition for dopant activation are examined about $900^{\circ}C$, 30 minutes. After final process step, N-well junction, P+ S/D junction and N+ S/D junction depth are calculated 3.16 ${\mu}m$, 0.45 ${\mu}m$ and 0.25 ${\mu}m$ respectively.

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