• 제목/요약/키워드: half-dose

검색결과 536건 처리시간 0.023초

Inhibitory Effects of Ginsenoside Metabolites, Compound K and Protopanaxatriol, on $GABA_C$ Receptor-Mediated Ion Currents

  • Lee, Byung-Hwan;Hwang, Sung-Hee;Choi, Sun-Hye;Kim, Hyeon-Joong;Lee, Joon-Hee;Lee, Sang-Mok;Ahn, Yun Gyong;Nah, Seung-Yeol
    • The Korean Journal of Physiology and Pharmacology
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    • 제17권2호
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    • pp.127-132
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    • 2013
  • Ginsenosides, one of the active ingredients of Panax ginseng, show various pharmacological and physiological effects, and they are converted into compound K (CK) or protopanaxatriol (M4) by intestinal microorganisms. CK is a metabolite derived from protopanaxadiol (PD) ginsenosides, whereas M4 is a metabolite derived from protopanaxatriol (PT) ginsenosides. The ${\gamma}$-aminobutyric acid $receptor_C$ ($GABA_C$) is primarily expressed in retinal bipolar cells and several regions of the brain. However, little is known of the effects of ginsenoside metabolites on $GABA_C$ receptor channel activity. In the present study, we examined the effects of CK and M4 on the activity of human recombinant $GABA_C$ receptor (${\rho}$ 1) channels expressed in Xenopus oocytes by using a 2-electrode voltage clamp technique. In oocytes expressing $GABA_C$ receptor cRNA, we found that CK or M4 alone had no effect in oocytes. However, co-application of either CK or M4 with GABA inhibited the GABA-induced inward peak current ($I_{GABA}$). Interestingly, pre-application of M4 inhibited $I_{GABA}$ more potently than CK in a dose- dependent and reversible manner. The half-inhibitory concentration ($IC_{50}$) values of CK and M4 were $52.1{\pm}2.3$ and $45.7{\pm}3.9{\mu}M$, respectively. Inhibition of $I_{GABA}$ by CK and M4 was voltage-independent and non-competitive. This study implies that ginsenoside metabolites may regulate $GABA_C$ receptor channel activity in the brain, including in the eyes.

얼갈이배추의 재배기간 중 Chlorothalonil, Indoxacarb, Lufenuron, Metalaxyl 및 Methomyl의 잔류량 변화 (Residual Pattern of Chlorothalonil, Indoxacarb, Lufenuron, Metalaxyl and Methomyl during the Cultivation Periods in Chinese Cabbage)

  • 고광용;김성헌;장영희;이규승
    • 농약과학회지
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    • 제12권1호
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    • pp.34-42
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    • 2008
  • 국립농산물 품질관리원 출하 전 농산물 검사시 얼갈이배추에서 검출빈도가 높은 chlorothalonil, indoxacarb, lufenuron, metalaxyl 및 methomyl 등 농약 5종에 대하여 수확 10일전에 대상약제를 살포하고 생산기간중의 경시적인 잔류량 변화를 조사하고 이를 토대로 반감기를 산출하였다. 얼갈이배추의 생산기간동안 표준량 살포 처리구에서 chlorothalonil의 잔류량은 55.58 mg/kg(0 day)에서 20.08 mg/kg(10 day)로 감소하고, 반감기는 7.45일 이었으며, indoxacarb는 7.85 mg/kg(0 day)에서 1.46 mg/kg(10 day)로 감소하고 반감기는 4.2일 이었으며, lufenuron는 1.57 mg/kg(0 day)에서 0.49 mg/kg(10 day)로 감소하고 반감기는 5.85일 이었으며, metalaxyl은 8.12 mg/kg(0 y)에서 0.10 mg/kg(10 day)로 감소하고 반감기는 1.75일 이었고 methomyl은 11.51 mg/kg(0 day)에서 0.80 mg/kg(10 day)로 감소하고 반감기는 2.42일 이었다. 또한 배량 처리구에서의 반감기는 chlorothalonil 9.05일, indoxacarb 7.09일, lufenuron 8.82일, metalaxyl 3.32일, methomyl 2.72일 이었다.

구리가 Ferroportin-1 유전자 발현 조절에 미치는 영향 (Effect of Copper on the Regulation of Ferroportin-1 Gene Expression)

  • 박보연;정자용
    • Journal of Nutrition and Health
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    • 제42권5호
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    • pp.434-441
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    • 2009
  • 본 연구는 J774 대식세포에서 FPN 유전자 발현 조절에 구리가 미치는 영향을 알아보기 위하여 수행되었으며 그 결과는 다음과 같다. J774 대식 세포에 구리를 처리하였을 때, iron exporter FPN의 mRNA 수준이 농도 의존적으로 증가하는 것으로 나타났다. 반면, iron importer DMT1의 mRNA 수준은 구리 처리에 의해 영향을 받지 않았다. Actinomycin D를 이용하여 mRNA 합성을 억제한 상태에서 FPN mRNA 분해 정도를 시간별로 추적한 결과, acitnomycin D 처리 후 9시간 경과시 FPN mRNA 수준이 처음 수준의 약 60% 정도로 감소하였다. 배양액에 구리를 첨가한 경우에도 FPN mRNA의 분해 정도는 아무것도 처리하지 않은 대조군과 유의적인 차이가 없었으며, 이로 볼 때 구리는 FPN mRNA의 안정성에 영향을 미치지 않는 것으로 생각된다. 한편, reporter assay 실험 결과 구리의 첨가는 FPN 프로모터 활성을 유의적으로 증가시키는 것으로 나타나, 구리가 FPN mRNA의 전사 과정을 직접적으로 촉진함을 알 수 있었다. 또한, FPN 5'-UTR에 위치하는 IRE (iron response element)의 존재 여부는 구리에 의한 FPN 전사 개시 활성에 영향을 주지 않는 것으로 나타났으며, 이로 볼 때 구리는 철분과는 독립적인 작용 기작에 의해 FPN 유전자 발현을 조절하는 것으로 사료된다. 이상의 결과를 종합해 볼 때, 구리는 대식 세포에서 전사개시 과정을 활성화함으로써 농도 의존적으로 FPN 유전자 발현을 촉진하는 것으로 생각되며, 이는 구리가 철분의 대사에 미치는 새로운 작용 기작을 제시한다. 앞으로, 구리와 철 분의 상호 작용이 FPN의 철분 및 다른 무기질 이온의 세포내 외 수송 (transport)에 어떤 영향을 미치는지에 대한 기능적 연구가 계속적으로 이루어져야 할 것으로 사료된다.

Super-resolution Convolutional Neural Network를 이용한 전산화단층상의 화질 평가 (Image Quality Evaluation in Computed Tomography Using Super-resolution Convolutional Neural Network)

  • 남기복;조정효;이승완;김번영;임도빈;이다혜
    • 한국방사선학회논문지
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    • 제14권3호
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    • pp.211-220
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    • 2020
  • 고화질의 전산화단층촬영상을 통해 정확한 병변 검출과 진단을 할 수 있다. 이와 같은 장점 때문에 전산화단층촬영 시 방사선량을 줄이면서 영상 화질을 개선하기 위해 많은 연구가 수행되었다. 최근 전산화단층촬영상 화질을 향상시키기 위한 딥러닝 기반 기술이 개발되었고, 기존의 기술에 비해 우수한 성능을 보이고 있다. 본 연구에서는 전산화단층촬영상의 공간분해능을 향상시키기 위해 초고해상도 합성곱 신경망 모델을 사용하였으며, 초고해상도 합성곱 신경망 모델의 성능을 결정하는 초 매개 변수 변화에 따른 영상 화질을 평가하여 초고해상도 합성곱 신경망 모델에 대한 초 매개 변수의 효과를 검증하였다. Profile, 구조적 유사성 지수, 최대신호 대 잡음비 및 반치폭을 측정하여 초 매개 변수 변화에 따른 초고해상도 합성곱 신경망 모델의 성능을 평가하였다. 연구결과, 초고해상도 합성곱 신경망 모델의 성능은 epoch와 training set이 증가함에 따라 향상되었으며, 전산화단층촬영상 화질을 향상시키기 위해 learning rate 최적화가 필요하다는 사실을 확인하였다. 따라서 최적의 초 매개 변수와 함께 구현된 초고해상도 합성곱 신경망 모델은 전산화단층촬영상의 품질을 향상시킬 수 있다.

8-Fluorociprofloxacin과 Ciprofloxacin의 시험관내 및 생체내 항균효과와 약물동태의 비교 (In vitro and in vivo Antibacterial Activities and Pharmacokinetics of 8-Fluorociprofloxacin and Ciprofloxacin)

  • 최경업;정용환;김제학
    • 약학회지
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    • 제37권3호
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    • pp.235-242
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    • 1993
  • 8-Fluorociprofloxacin(8-FCP) is an investigational quinolone derivative that is substituted with fluorine at the C-8 position of ciprofloxacin(CP). It was found that the in vitro activity of 8-FCP against Gram(+) bacteria was more potent that of CP, but the opposite against Gram(-) bacteria was true. However, 8-FCP showed better in vivo efficacy than CP against representative Gram(-) organisms, E. coli and K pneumoniae. In an attempt to seek for factors causing this discrepancy in the antibacterial activities, a comparative pharmacokinetic study of 8-FCP and CP was conducted in mice and rats treated either intravenously or orally at a single dose of 30 mg/kg. The pharmacokinetic parameters in mice were as follows; the mean peak serum concentrations(C$_{max}$) following i.v. and oral doses were 12.4 and 5.3 $\mu\textrm{g}$/ml for 8-FCP, and 9.5 and 2.5 $\mu\textrm{g}$/ml for CP, respectively. The terminal half-life(t$_{1/2\beta}$) was 72.9 min for 8-FCP, and 98.2 min for CP, and the oral bioavailability(F) was 89.9% for 8-FCP, and 50.5% for CP. In rats, the mean ($\pm$SD) $C_{max}$ after i.v. administration were 11.6$\pm$1.6 $\mu\textrm{g}$/ml for 8-FCP, and 10.2$\pm$1.3 $\mu\textrm{g}$/ml for CP, whereas oral administration produced $C_{max}$ of 5.9$\pm$1.8 $\mu\textrm{g}$/ml for 8-FCP and 1.1$\pm$0.9 $\mu\textrm{g}$/ml for CP, respectively. The t$_{1/2\beta}$ was 67.9$\pm$8.4 min for 8-FCP, and 76.4$\pm$7.2 min for CP. The F was 88.6$\pm$6.3% for 8-FCP, and 40.7$\pm$6.5% for CP. Marked differences were observed between the two quinolones in the $C_{max}$ and the area under the concentration-time curve obtained after oral administration in mice and rats. The extent of 8-FCP absorption in both mice and rats was approximately 2-fold higher than that of CP, suggesting that the fluorine atom attached to C-8 plays an important role in facilitating oral absorption from the gastrointestinal tract.

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Assessment of Radionuclide Deposition on Korean Urban Residential Area

  • Lee, Joeun;Han, Moon Hee;Kim, Eun Han;Lee, Cheol Woo;Jeong, Hae Sun
    • Journal of Radiation Protection and Research
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    • 제45권3호
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    • pp.101-107
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    • 2020
  • Background: An important lesson learned from the Fukushima accident is that the transition to the mid- and long-term phases from the emergency-response phase requires less than a year, which is not very long. It is necessary to know how much radioactive material has been deposited in an urban area to establish mid- and long-term countermeasures after a radioactive accident. Therefore, an urban deposition model that can indicate the site-specific characteristics must be developed. Materials and Methods: In this study, the generalized urban deposition velocity and the subsequent variation in radionuclide contamination were estimated based on the characteristics of the Korean urban environment. Furthermore, the application of the obtained generalized deposition velocity in a hypothetical scenario was investigated. Results and Discussion: The generalized deposition velocities of 137Cs, 106Ru, and 131I for each residence type were obtained using three-dimensional (3D) modeling. For all residence types, the deposition velocities of 131I are greater than those of 106Ru and 137Cs. In addition, we calculated the generalized deposition velocities for each residential types. Iodine was the most deposited nuclide during initial deposition. However, the concentration of iodine in urban environment drastically decreases owing to its relatively shorter half-life than 106Ru and 137Cs. Furthermore, the amount of radioactive material deposited in nonresidential areas, especially in parks and schools, is more than that deposited in residential areas. Conclusion: In this study, the generalized urban deposition velocities and the subsequent deposition changes were estimated for the Korean urban environment. The 3D modeling was performed for each type of urban residential area, and the average deposition velocity was obtained and applied to a hypothetical accident. Based on the estimated deposition velocities, the decision-making systems can be improved for responding to radioactive contamination in urban areas. Furthermore, this study can be useful to predict the radiological dose in case of large-scale urban contamination and can support decision-making for long-term measurement after nuclear accident.

쥐를 이용한 새로운 가돌리늄 조영제 Gd-DTPA-bis(amide)(L3)의 약동학 및 생체내 분포 특성에 대한 연구 (Pharmacokinetics and Bio-distribution of New Gd-complexes of DTPA-bis (amide) (L3) in a Rat Model)

  • ;;장용민;강덕식
    • Investigative Magnetic Resonance Imaging
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    • 제17권4호
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    • pp.259-266
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    • 2013
  • 목적: DTPA-bis-amide (L3) Gd(III) 복합체의 약동학 및 생체내 분포특성을 조사하고자 하였다. 대상과 방법: Sprague-Dawley 쥐의 꼬리정맥을 통하여 0.1 mmol Gd/kg의 DTPA-bis-amide (L3) Gd(III) 복합체를 주사한 후 약동학 및 생체내 분포 특성을 조사하였다. 조직 및 장기 그리고 혈중 Gd 농도를 ICP-AES를 사용하여 정량 측정하였으며 혈중 약동학적 파라미터는 two-compartment 모델을 사용하여 계산하였다. 결과: DTPA-bis-amide (L3) Gd(III) 복합체의 혈중 반감기는 ${\alpha}$-phase의 경우 $2.286{\pm}0.11$ min 그리고 ${\beta}$-phase의 경우 $146.1{\pm}7.5$ min 이었다. 생체내 분포특성은 주요 배설 경로는 신장을 통한 배설이 주요 경로였으며 일부 담도계를 통한 배설이 확인되었다. 또한 Gd(III)의 농도비는 다른 장기에 비해 간과 비장에서 매우 높은 농도를 보였으며 일부 Gd(III)이 정맥주사 후 7일후에 혈액 및 일부 장기에서 매우 소량 검출되었다. 결론: 새로운 조영제인 DTPA-bis-amide (L3) Gd(III) 복합체는 혈중 잔류시간이 상대적으로 길면서도 체내 축적없이 체외로 배출되는 특성을 나타내었다. 따라서 친지질성과 친수성의 균형이 잘 이루어진 가돌리늄 조영제의 합성은 향후 blood pool MRI 조영제로써의 가능성이 매우 높은 것으로 판단된다.

Usefulness of serum cystatin C to determine the dose of vancomycin in neonate

  • Shin, Jeong Eun;Lee, Soon Min;Eun, Ho Seon;Park, Min Soo;Park, Kook In;Namgung, Ran
    • Clinical and Experimental Pediatrics
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    • 제58권11호
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    • pp.421-426
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    • 2015
  • Purpose: The vancomycin dosage regimen is regularly modified according to the patient's glomerular filtration rate (GFR). In the present study, we aimed to assess the usefulness of serum cystatin C (Cys-C) concentration, compared with serum creatinine (SCr) concentration, for predicting vancomycin clearance (CLvcm) in neonates. Methods: We retrospectively analyzed the laboratory data of 50 term neonates who were admitted to the neonatal intensive care unit and received intravenous vancomycin, and assessed the pharmacokinetic profiles. Creatinine clearance (CLcr) and GFR based on Cys-C (GFRcys-c) were estimated using the Schwartz and Larsson formulas, respectively. Results: The mean CLvcm (${\pm}$standard deviation) was $74.52{\pm}31.17L/hr$, the volume of distribution of vancomycin was $0.67{\pm}0.14L$, and vancomycin half-life was $9.16{\pm}17.42hours$. The SCr was $0.46{\pm}0.25mg/dL$ and serum Cys-C was $1.43{\pm}0.34mg/L$. The peak and trough concentrations of vancomycin were $24.65{\pm}14.84$ and $8.10{\pm}5.35mcg/mL$, respectively. The calculated GFR based on serum creatinine concentration (GFR-Cr) and GFRcys-c were $70.2{\pm}9.45$ and $63.6{\pm}30.18mL/min$, respectively. The correlation constant for CLvcm and the reciprocal of Cys-C (0.479, P=0.001) was significantly higher than that for CLvcm and the reciprocal of SCr (0.286, P=0.044). GFRcys-c was strongly correlated with CLvcm (P=0.001), and the correlation constant was significantly higher than that for CLvcm and CLcr (0.496, P=0.001). Linear regression analysis showed that only GFRcys-c was independently and positively correlated with CLvcm (F=41.9, P<0.001). Conclusion: The use of serum Cys-C as a marker of CLvcm could be beneficial for more reliable predictions of serum vancomycin concentrations, particularly in neonates.

방사선촬영 보조기구를 이용한 어린이 흉부 엑스선 검사에 관한 연구 (A Study on Chest X-ray Using Ancillary Device for Child Radiography)

  • 이도병;이소미;최현우;김종기;이종민
    • 대한의용생체공학회:의공학회지
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    • 제39권1호
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    • pp.48-54
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    • 2018
  • In this study, We developed a Ancillary device for child radiography for X-ray of children under 5 years old and verified its effectiveness. Chest X-rays of children younger than 5 years of age were performed by Supine method at the position of Table detector, Short - Source to Image Receptor Distance(SID). Existing Supine and Short -SID imaging methods cause many problems, such as errors in image reading and excessive radiation exposure dose to patients, but the use of an Ancillary device for child radiography(ADCR) solves these problems. A total of 160 children were divided into the Upright group using ADCR and Supine group without ADCR. The chest X-ray image was visually evaluated by two radiologists with reference to the European Commission's List of Quality Criteria for Diagnostic Radiographic Images in Pediatrics. The total score of the qualitative evaluation was 5.15% higher in the chest upright method using ADCR than in the chest supine method without ADCR, and the chest upright method score was higher than that of the chest supine method in items 1 to 7. whether infants have deep inspiration or not, 4.87% higher for item 1, whether infants rotate or not and the degree of tilting, 0% higher for the item 2, the reproduction of image from just above apices of lungs to T12/L1, 0% for the item 3, reproduction of the vascular pattern in central 2/3 of the lungs, 6.92% higher for the item 4, reproduction of the trachea and the proximal bronchi, 12.9% higher for the item 5, visually sharp reproduction of the diaphragm and costo-phrenic angles, 10% higher for the item 6, reproduction of the spine and paraspinal structures and visualisation of the retrocardiac lung and the mediastinum, and 3.65% higher for the item 7. Items 2 and 3 showed no statistically significant differences(P > 0.05), and items 1, 4, 5, 6, and 7 showed statistically significant differences(P < 0.05). In conclusion, Upright method using ADCR in pediatric chest X-ray is considered as a good alternative to existing Supine method.

Management of Enteral Nutrition in the Pediatric Intensive Care Unit: Prokinetic Effects of Amoxicillin/Clavulanate in Real Life Conditions

  • Chiusolo, Fabrizio;Capriati, Teresa;Erba, Ilaria;Bianchi, Roberto;Atti, Marta Luisa Ciofi degli;Picardo, Sergio;Diamanti, Antonella
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • 제23권6호
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    • pp.521-530
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    • 2020
  • Purpose: Malnutrition is a common feature in critically ill children. Enteral nutrition (EN) is the main strategy to nutritionally support critical ill children, but its use can be hindered by the development of intolerance. The study aimed to assess the effectiveness and safety of amoxicillin/clavulanate (A/C) to treat EN intolerance. Methods: We retrospectively evaluated patients admitted to the pediatric intensive care unit from October 2018 to October 2019. We conducted a case-control study: in the first 6 months (October 2018-April 2019) we implemented the nutritional protocol of our Institution with no drug, whereas in the second half (May 2019-October 2019) we employed A/C for 1 week at a dose of 10 mg/kg twice daily. Results: Twelve cases were compared with 12 controls. At the final evaluation, enteral intake was significantly higher than that at baseline in the cases (from 2.1±3.7 to 66.1±27.4% of requirement, p=0.0001 by Wilcoxon matched-pairs signed rank test) but not in the controls (from 0.2±0.8 to 6.0±14.1% of the requirement, p=NS). Final gastric residual volume at the end of the observation was significantly lower in the cases than in the controls (p=0.0398). The drug was well tolerated as shown by the similar safety outcomes in both cases and controls. Conclusion: Malnutrition exposes critically ill children to several complications that affect the severity of disease course, length of stay, and mortality; all may be prevented by early EN. The development of intolerance to EN could be addressed with the use of A/C. Future prospective clinical trials are needed to confirm these conclusions.