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Effects of Baicalein on the Bioavailability of Nicardipine in Rats

  • Son, Hong-Mook;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
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    • v.40 no.5
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    • pp.291-296
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    • 2010
  • This study was to investigate the effect of baicalein, an antioxidant, on the bioavailability of nicardipine after orally or intravenously administered nicardipine in rats. Nicardipine was administered orally (12 mg/kg) or intravenously (4 mg/kg) with or without orally administered baicalein (0.4, 2 or 10 mg/kg) to rats. In the inhibitory effect of baicalein on CYP3A4 activity, baicalein inhibited CYP3A4 activity with $IC_{50}$ values of 9.2 ${\mu}M$. The cell-based P-gp activity test using rhodamine-123 also showed that baicalein (30-10 ${\mu}M$, p<0.01) significantly inhibited P-gp activity. Compared with the control group (given nicardipine alone), the area under the plasma concentration-time curve (AUC) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 25.9-60.0%, and the peak concentration ($C_{max}$) was significantly (10 mg/kg, P<0.01) increased by 40.0% in the presence of baicalein after orally administration of nicardipine. Consequently, the relative bioavailability (R.B.) of nicardipine was increased by 1.26- to 1.60-fold and the absolute bioavailability (A.B.) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 26.0-59.9%. Compared to the i.v. control, baicalein did not significantly change pharmacokinetic parameters of nicardipine in i.v. administration. Accordingly, the enhanced oral bioavailability of nicardipine might be mainly due to increased intestinal absorption caused by P-gp inhibition rather than to reduced elimination of nicardipine by baicalein. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the small intestine via the inhibition of P-gp and reduced first-pass metabolism of nicardipine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by baicalein. Based on these results, nicardipine dosage should be adjusted when given concomitantly with baicalein.

Anxiolytic effect of chronic ginseng treatment using elevated T-maze in mice

  • Mohan, M;Kasture, SB;Balaraman, R
    • Advances in Traditional Medicine
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    • v.7 no.1
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    • pp.41-45
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    • 2007
  • The roots of the plant Korean ginseng have been extensively used in the traditional Chinese herbal medicine. The effects of chronic administration of Korean ginseng extract (KGE) were investigated on two different anxiety models: the elevated T-maze (for inhibitory avoidance and escape measurements) and the open field test (OFT). Diazepam (1 mg/kg), KGE (10, 30 and 100 mg/kg) were administered orally for 15 days. On the 14th day, mice were previously exposed for 30 min to one of the open arms of the T-maze, 24 h before the test. On 15th day, mice had two exposures to the enclosed and open arm of the elevated T-maze followed by exposure to the open field apparatus. The number of line crossings in the apparatus was used to assess locomotor changes. Cumulative Concentration Response Curve of 5-HT was plotted using rat fundus which were pre-treated in a similar way. Treatment with Diazepam (1 mg/kg) and KGE (10, 30 and 100 mg/kg) significantly (P < 0.05) impaired inhibitory avoidance performance but did not impair escape latency. In OFT, diazepam facilitated locomotion as compared to vehicle and other treatment groups. KGE at any of the selected doses did not impair locomotion. Concentration response curve of 5-HT was shifted towards the right with suppression of maxima in rats treated with KGE. The results suggest that KGE exerts anxiolytic like behaviour in a specific subset of defensive behaviour, particularly those related to generalized anxiety disorder.

Anxiolytic effect of chronic ginger treatment using elevated T-maze in mice

  • Mohan M;Kasture SB;Balaraman R
    • Advances in Traditional Medicine
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    • v.6 no.3
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    • pp.179-185
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    • 2006
  • We investigated the effects of chronic administration of different extracts of ginger rhizome [pet ether extract (PE); toluene fraction (TF) of pet ether extract] on anxiety models: the elevated T-maze (ETM) (for inhibitory avoidance and escape measurements) and the open field test. Ondansetron (1 mg/kg), FE (10, 30 &100 mg/kg) and TF (10 & 30 mg/kg) were administered orally for 15 days. On the $14^{th}$ day mice were previously exposed for 30 min to one of the open arms of the T-maze, 24 h before the test. On $15^{th}$ day mice had two exposures to the enclosed and open arm of the ETM followed by exposure to the open field apparatus. The number of line crossings in the apparatus was used to assess locomotor changes. Cumulative Concentration Response Curve of 5-HT was plotted using rat fundus which were pretreated in a similar way. Treatment with Ondansetron (1 mg/kg), PE (100 mg/kg), TF (10 mg/kg) and TF (30 mg/kg) significantly (P<0.05) impaired inhibitory avoidance performance but did not impair escape latency. Concentration response curve of 5-HT was shifted towards the right with suppression of maxima in rats treated with PE and TF. The results suggest that PE and TF of Ginger rhizome exerts anxiolytic like behaviour in a specific subset of defensive behaviour, particularly those related to generalized anxiety disorder.

Fabrication of Thermoelectric Module and Analysis of its Power Generation Characteristics (열전발전소자 제작 및 발전특성 분석)

  • Choi, Taeho;Kim, Tae Young
    • Journal of Convergence for Information Technology
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    • v.11 no.2
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    • pp.90-97
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    • 2021
  • In this study, a Bi2Te3 thermoelectric generator (TEG) was fabricated to convert unused thermal energy into useful electrical energy. For the performance test, a dedicated experiment device consisting of a heating block operating with cartridge heaters and a cooling block through which a refrigerant flows was constructed. A 3×3 array of thermocouples was mounted on the heating block and the cooling block, respectively, to derive the temperature fields and heat transfer rate onto both sides of the TEG. Experiments were conducted for a total of 9 temperature differences, obtaining V-I and P-R curves. The results of 7 variables including Seebeck coefficients that have a major effect on performance were presented as a function of the temperature difference. The feasibility of the energy recovery performance of the developed TEG was verified from the maximum power output of 7.5W and conversion efficiency of 11.3%.

Characteristics of Ultra-thin Polymer Ferroelectric Films (초박막 폴리머 강유전체 박막의 특성)

  • Kim, Kwang-Ho
    • Journal of the Semiconductor & Display Technology
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    • v.19 no.4
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    • pp.84-87
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    • 2020
  • The properties of ultra-thin two-dimensional (2D) organic ferroelectric Langmuir-Blodgett (LB) films of the poly(vinylidene fluoride-trifluoroethylene) [P(VDF-TrFE)] were investigated to find possible applicability in flexible and wearable electronics applications. In the C-V characteristics of the MFM capacitor of 2-monolayer of 5 nm films, a butterfly hysteresis curve due to the ferroelectricity of P(VDF-TrFE) was confirmed. Typical residual polarization value was measured at 2μC/㎠. When the MFM capacitor with ultra-thin ferroelectric film was measured by applying a 10 Hz bipolar pulse, it was shown that 65% of the initial polarization value in 105 cycles deteriorated the polarization. The leakage current density of the 2-monolayer film was maintained at about 5 × 10-8 A/㎠ for the case at a 5MV/cm electric field. The resistivity of the 2-monolayer film in the case at an electric field at 5 MV/cm was more than 2.35 × 1013 Ω·cm.

Near-IR study of Nova V2468 Cyg

  • Raj, Ashish;Ashok, N.M.;Banerjee, D.P.K.;Kim, Sang Chul;Pak, Mina
    • The Bulletin of The Korean Astronomical Society
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    • v.39 no.2
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    • pp.76.1-76.1
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    • 2014
  • We present near-infrared spectroscopic and photometric observations of the nova V2468 Cyg taken from 2008 March 14 till 2008 November 11 following its outburst on 2008 March 7. The JHK spectra of the nova have been taken from the Mount Abu Infrared Observatory using the Near-Infrared Imager/Spectrometer. The early spectra are dominated by strong H I lines from the Brackett and Paschen series, Fe II, O I and C I lines, typical of Fe II type novae but after 46 days from outburst there is significant reduction in the strength of the C I lines and the spectra are dominated by He I lines. The FWHM of the Pa-beta and Br-gamma lines change from 2200-2300 km s-1 to 1700-1800 km s-1 after 12 days from outburst. Three additional small amplitude outbursts are seen near 110, 185 and 240 days in the V band light curve after the discovery. The upper limit for the ejecta mass for V2468 Cyg is estimated to be $5.2{\times}10-6Msun$.

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Differential Absorption Analysis of Nonmagnetic Material in the Phantom using Dual CT

  • Kim, Ki-Youl;Lee, Hae-Kag;Cho, Jae-Hwan
    • Journal of Magnetics
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    • v.21 no.2
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    • pp.286-292
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    • 2016
  • This study evaluates the change of computer tomography (CT) number in the case of the metal artifact reduction (MAR) algorithm, using the phantom. The images were obtained from dual CT using a gammex 467 tissue characterization phantom, which is similar to human tissues. The test method was performed by dividing pre and post MAR algorithm and measured CT values of nonmagnetic materials within the phantom. In addition, the changes of CT values for each material were compared and analyzed after measuring CT values up to 140 keV, using the spectral HU curve followed by CT scan. As a result, in the cases of N rod (trabecular bone) and E rod (trabecular bone), the CT numbers decreased as keV increasing but were constant above 90 keV. In the cases of I rod (dense bone) and K rod (dense bone), the CT numbers also decreased as keV increased but were uniform above 90 keV. The CT numbers from 40 keV to 140 keV were consistent in the cases of J rod (liver), D rod (liver), L rod (muscle), and F rod (muscle). For A rod (adipose), G rod (adipose), B rod (breast) and O rod (breast), the CT numbers increased as keV increased but were constant after 90 keV. The CT numbers from 40 keV to 140 keV were consistent in the cases of C rod (lung (exhale)), P rod (lung (exhale)), M rod (lung (inhale)) and H rod (lung (exhale)). Conclusively, because dual CT exhibits no changes in image quality and is able to analyze nonmagnetic materials by measuring the CT values of various materials, it will be used in the future as a useful tool for the diagnosis of lesions.

Growth and Properties of Ultra-thin SiO2 Films by Rapid Thermal Dry Oxidation Technique (급속 건식 열산화 방법에 의한 초박막 SiO2의 성장과 특성)

  • 정상현;김광호;김용성;이수홍
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.17 no.1
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    • pp.21-26
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    • 2004
  • Ultra-thin silicon dioxides were grown on p-type(100) oriented silicon employing rapid thermal dry oxidation technique at the temperature range of 850∼1050 $^{\circ}C$. The growth rate of the ultra-thin film was fitted well with tile model which was proposed recently by da Silva & Stosic. The capacitance-voltage, current-voltage, characteristics were used to study the electrical properties of these thin oxides. The minimum interface state density around the midgap of the MOS capacitor having oxide thickness of 111.6 $\AA$ derived from the C-V curve was ranged from 6 to 10${\times}$10$^{10}$ /$\textrm{cm}^2$eV.

Direct Liquid Injection Metal Organic Chemical Vapor Deposition of $HfO_2$ Thin Films Using $Hf(dimethylaminoethoxide)_4$.

  • 송문균;강상우;이시우
    • Proceedings of the Korean Society Of Semiconductor Equipment Technology
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    • 2003.12a
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    • pp.45-49
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    • 2003
  • 본 논문에서는 gate 산화막을 위한 Hf oxide 박막을 $Hf(dmae)_4$ (dmae=dimethylaminoethoxide) 전구체로 Direct Liquid Injection Metal Organic Chemical Vapor Deposition (DLI-MOCVD)방법을 이용하여 p-type Si(100) 기판 위에 증착하였다. 이 전구체를 이용하여 $150^{\circ}C$의 낮은 증착 온도에서도 낮은 carbon 농도와 roughness를 가지는 양질의 박막을 증착할 수 있었다. 증착된 박막은 비정질 구조를 나타내었지만 annealing 온도를 증가시킴에 따라서 결정성(monoclinic phase)을 나타내었다. $500{\AA}$으로 증착한 박막을 C-V 와 I-V curve를 통하여 전기적 특성을 평가하였다. 열처리 온도가 증가함에 따라 유효유전상수(k)는 증가하지만 열처리 온도가 $900^{\circ}C$ 이상이 되면 계면층의 형성에 의해 유효유전상수는 감소하게 되고 이에 따라 누설 전류도 감소하게 된다. 산소분위기 $800^{\circ}C$에서 annealing한 $HfO_2$ 박막의 유전상수는 20.1이고, 누설 전류 밀도는 SV에서 $2.2\times10^{-6}A/\textrm{cm}^2$ 로 좋은 전기적 특성을 가진다.

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Inhibition of L-type Ca2+ current by ginsenoside Rd in rat ventricular myocytes

  • Lu, Cheng;Sun, Zhijun;Wang, Line
    • Journal of Ginseng Research
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    • v.39 no.2
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    • pp.169-177
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    • 2015
  • Background: Ginsenoside Rd (GSRd), one of the most abundant ingredients of Panax ginseng, protects the heart via multiple mechanisms including the inhibition of $Ca^{2+}$ influx.We intended to explore the effects of GSRd on L-type $Ca^{2+}$ current ($I_{Ca,L}$) and define the mechanism of the suppression of $I_{Ca,L}$ by GSRd. Methods: Perforated-patch recording and whole-cell voltage clamp techniques were applied in isolated rat ventricular myocytes. Results: (1) GSRd reduced $I_{Ca,L}$ peak amplitude in a concentration-dependent manner [half-maximal inhibitory concentration $(IC_{50})=32.4{\pm}7.1{\mu}mol/L$] and up-shifted the current-voltage (I-V) curve. (2) GSRd ($30{\mu}mol/L$) significantly changed the steady-state activation curve of $I_{Ca,L}$ ($V_{0.5}:-19.12{\pm}0.68$ vs. $-6.26{\pm}0.38mV$; n = 5, p < 0.05) and slowed down the recovery of $I_{Ca,L}$ from inactivation [the time content (${\zeta}$) from 91 ms to 136 ms, n = 5, p < 0.01]. (3) A more significant inhibitive effect of GSRd ($100{\mu}mol/L$) was identified in perforated-patch recording when compared with whole-cell recording [$65.7{\pm}3.2%$ (n = 10) vs. $31.4{\pm}5.2%$ (n = 5), p < 0.01]. (4) Pertussis toxin ($G_i$ protein inhibitor) completely abolished the $I_{Ca,L}$ inhibition induced by GSRd. There was a significant difference in inhibition potency between the two cyclic adenosine monophosphate elevating agents (isoprenaline and forskolin) prestimulation [$55{\pm}7.8%$ (n = 5) vs. $17.2{\pm}3.5%$ (n = 5), p < 0.01]. (5) 1H-[1,2,4]Oxadiazolo[4,3-a]-quinoxalin-1-one (a guanylate cyclase inhibitor) and N-acetyl-$\small{L}$-cysteine (a nitric oxide scavenger) partly recovered the $I_{Ca,L}$ inhibition induced by GSRd. (6) Phorbol-12-myristate-13-acetate (a protein kinase C activator) and GF109203X (a protein kinase C inhibitor) did not contribute to the inhibition of GSRd. Conclusion: These findings suggest that GSRd could inhibit $I_{Ca,L}$ through pertussis toxin-sensitive G protein ($G_i$) and a nitric oxide-cyclic guanosine monophosphate-dependent mechanism.