• Title/Summary/Keyword: H17/28

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Pharmacokinetics of thalidomide in dogs: can feeding affect it? A preliminary study

  • Pierini, Alessio;Sartini, Irene;Giorgi, Mario;Lebkowska-Wieruszewska, Beata;Lisowski, Andrzej;Poapolathep, Amnart;Marchetti, Veronica
    • Journal of Veterinary Science
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    • v.21 no.5
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    • pp.60.1-60.11
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    • 2020
  • Background: Tumor-associated neoangiogenesis is a crucial target for antitumor therapies. Thalidomide (TAL) is a promising anti-neoangiogenetic drug that has recently been used in the treatment of several malignancies in dogs. Objectives: The aim of the study was to assess the pharmacokinetics of TAL after single oral administration in dogs. Additionally, the influence of feeding on the pharmacokinetic profile of TAL in dogs has been preliminarily investigated. Methods: Six healthy adult female Labradors were enrolled according to a randomized single-dose, 2-treatment, 2-phase, paired 2 × 2 cross-over study design. The dogs were administered a single 400 mg capsule of TAL in fasted and fed conditions. Blood was collected from 15 min to 48 h after dosing, and TAL quantified in plasma by a validated high-performance liquid chromatography method. The pharmacokinetics of TAL were analyzed using a non-compartmental approach. Results: TAL concentration was quantifiable up to 10 h and 24 h after fasted and fed conditions, respectively. Cmax (fasted, 1.34 ± 0.12 ㎍/mL; fed, 2.47 ± 0.19 ㎍/mL) and Tmax (fasted, 3 h; fed, 10 h) differed substantially between the 2 groups. AUC and t1/2λz were significantly higher in fed (42.46 ± 6.64 mg × h/L; 17.14 ± 4.68 h) compared to fasted (12.38 ± 1.13 mg × h/L; 6.55 ± 1.25 h) dogs. The relative oral bioavailability of TAL for the fasted group was low (36.92% ± 3.28%). Conclusions: Feeding affects the pharmacokinetics of oral TAL in dogs, showing a delayed, but higher absorption with different rate of elimination. These findings are of importance in clinical veterinary settings, and represent a starting point for further related studies.

Vinegar Produced from Chrysanthemum zawadskii and Pearl Shell (구절초진주식초)

  • Ann, Yong-Geun;Oh, Moon-Hun;Lee, Byung-Yup
    • The Korean Journal of Food And Nutrition
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    • v.25 no.1
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    • pp.90-98
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    • 2012
  • With the addition of ethanol to wax gourd extract and by acetic fermentation, 5.0% acidity vinegar was produced. After putting 10% extract(10% concentration) of Chrysanthemum zawadskii in this, and by dissolving shell, Chrysanthemum zawadskii-pearl vinegar was produced. When a 1% of ark shell, oyster shell, or ear shell was added to wax gourd vinegar, 95.6~98.4% of the shell dissolved, and when a 2% content of shell was added, 97.2~98.4% was dissolved. The acidity of vinegar which dissolved 1% shell was pH 3.0~3.17, and the acidity of vinegar which dissolved 2% shell was pH 1.11~ 1.20. The pH values of vinegar which dissolved 1%, and 2% shell contents were 4.54~4.55, and 4.86~4.95, respectively. When 1% shell was dissolved, the acidity was higher than that of commercial vinegar, with a high pH value and low level of free acid. This shows that when Chrysanthemum zawadskii 1% is added during acetic acid fermentation, the inhibition was 44.4%, and 22.2% respectively. In this regard, Chrysanthemum zawadskii should be added after the fermentation of acetic acid. The calcium content of 1% shell vinegar is 0.4%, and that of 2% vinegar is 0.78%. Non-heated native wax gourd shows an angiotensin converting enzyme inhibition rate of 21.7%, an antioxidant activity of 5.23%, and a tyrosinase inhibition rate of 5.5%. In the case of heated-extracted wax gourd, the angiotensin converting enzyme inhibition rate was 16.1%, superoxide dismutase activity was 20.5%, antioxidant activity was 23.2%, and the tyrosinase inhibition rate was 7.1%. Also, in the case of Chrysanthemum zawadskii, the angiotensin converting enzyme inhibition rate was 28.8%, the xanthine oxidase inhibition rate was 28.2%, the superoxide dismutase activity was 14.5%, the antioxidant activity was 3.2%, and the tyrosinase inhibition rate was 9.2% Data also revealed that when a 10% sample of the heated-wax gourd extract was added to A549 human lung cancer epithelial cells of, the number of cancer cells declined by 80% in 72 hours, When a 10% native extract was added, the number of cells declined by, 74% in 48 hours, and when a heated-extract of Chrysanthemum zawadskii was added, 100% of the cells died after 72 hours.

Effects of Thermal Wastewater Effluent and Hydrogen Ion Potential (pH) on Water Quality and Periphyton Biomass in a Small Stream (Buso) of Pocheon Area, Korea (포천지역 계류 (부소천)의 수질과 부착조류 생물량에 온배수와 수소이온농도 (pH) 영향)

  • Jeon, Gyeonghye;Eum, Hyun Soo;Jung, Jinho;Hwang, Soon-Jin;Shin, Jae-Ki
    • Korean Journal of Ecology and Environment
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    • v.50 no.1
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    • pp.96-115
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    • 2017
  • Understanding effects of thermal pollution and acidification has long been a concern of aquatic ecologists, but it remains largely unknown in Korea. This study was performed to elucidate the effects of thermal wastewater effluent (TWE) and acid rain on water quality and attached algae in a small mountain stream, the Buso Stream, a tributary located in the Hantan River basin. A total of five study sites were selected in the upstream area including the inflowing point of hot-spring wastewater (HSW), one upstream site (BSU), and three sites below thermal effluent merged into the stream (1 m, 10 m and 300 m for BSD1, BSD2, and BSD3, respectively). Field surveys and laboratory analyses were carried out every month from December 2015 to September 2016. Water temperature ranged $1.7{\sim}28.8^{\circ}C$ with a mean of $15.0^{\circ}C$ among all sites. Due to the effect of thermal effluent, water temperature at HSW site was sustained at high level during the study period from $17.5^{\circ}C$ (January) to $28.8^{\circ}C$ (September) with a mean of $24.2{\pm}3.7^{\circ}C$, which was significantly higher than other sites. Thermal wastewater effluent also brought in high concentration of nutrients(N, P). The effect of TWE was particularly apparent during dry season and low temperature period (December~March). Temperature effect of TWE did not last toward downstream, while nutrient effect seemed to maintain in longer distance. pH ranged 5.1~8.4 with a mean of 6.9 among all sites during the study period. The pH decrease was attributed to seasonal acid rain and snow fall, and their effects was identified by acidophilic diatoms dominated mainly by Eunotia pectinalis and Tabellaria flocculosa during March and August. These findings indicated that water quality and periphyton assemblages in the upstream region of Buso Stream were affected by thermal pollution, eutrophication, and acidification, and their confounding effects were seasonally variable.

A Study on the Greenhouse Heating Performance of Heat Pump System (온실난방을 위한 히트펌프의 성능에 관한 연구)

  • 윤용철;서원명;이석건
    • Magazine of the Korean Society of Agricultural Engineers
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    • v.40 no.3
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    • pp.94-102
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    • 1998
  • This experiment was carried out to study on the effect of greenhouse heating by water-to-water heat pump system employing heating water tank(ground water) as the heat source. Followings are the results obtained from this study ; 1. The heat amount absorbed from evaporator and the heat amount rejected from condenser were approximately 9, 000~ 12, 000kcal/h and 13, 000~ 17, OOOkcal/h, respectively. 2. The heat efficiencies of evaporator and condenser used in this experiment were approximately 79% and 83%, respectively. 3. The maximum heating load estimated for the experimental greenhouse was about 18, 000 ~ 25, OOOkcal/h, which was found to be about 28 ~ 32% higher than the heating capacity of the heat pump system adopted for this experiment. 4. The coefficients of performance(COP) for the heat pump and the total heat pump system were approximately 2.9~3.5 and 1.5~2.4, respectively. 5. The coefficient of performance(COP) calculated from the Mollier Diagram was about 3.2 ~ 3.4, which was reasonably close to the COP estimated on the basis of measured values. 6. The temperature of experimental greenhouse heated by the heat pump system could be maintained about 12~15 。C higher than that of a control greenhouse.

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Growth Environment and Vegetation Structure of Natural Habitat of Polygonatum stenophyllum Maxim (멸종위기식물 층층둥굴레의 자생지 생육환경 및 식생구조)

  • Song, Jae-Mo;Lee, Gi-Yeoung;Yi, Jae-Seon
    • Journal of Forest and Environmental Science
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    • v.25 no.3
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    • pp.187-194
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    • 2009
  • This study was carried out to investigate vegetation structure and soil property of natural habitat of Polygonatum stenophyllum to provide basic information for propagation, conservation and restoration. Habitats of Polygonatum stenophyllum were classified into Hemiptelea davidii-Robinia pseudo-acacia dominant population (Yeongwol-eup), Pinus densiflora-Hemiptelea davidii-Callicarpa japonica dominant population (Nam-myeon), and Hemiptelea davidii-Rubus crataegifolius dominant population (Gangchon-ri). The soil pH 6.49~7.28; and electron conductivity 0.10~0.19 ds/m. The average content of organic matter, total nitrogen, available $P_2O_5$, $Ca^{2+}$, $Mg^{2+}$, $K^+$, and $Na^+$ were 8.24~16.45 g/kg, 0.02~0.13%, 45.67~123.67 mg/kg, 4.61~6.71 cmol(+)/kg, 0.17~0.63 cmol(+)/kg, 0.06~0.27 cmol(+)/kg and 0.03~0.30 cmol(+)/kg, respectively. Species diversity index (H'), maximum species diversity index (H' max), evenness (J') and dominance (1-J') of investigated sites ranged 1.0323 (Nam-myeon)~1.1134 (Yeongwol -eup), 1.4914 (Gangchon-ri)~1.6128 (Nam-myeon), 0.6401 (Nam-myeon)~0.7270 (Yeongwol-eup) and 0.2730 (Yeongwol-eup)~0.3599 (Nam-myeon) respectively.

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Blood Analysis for Indirect Doping Control of Erythropoietin in Sports (운동선수들의 혈액분석을 통한 Etrythropoietin 간접도핑검사)

  • 이정란;김소영;홍지연;김명수;최명자
    • YAKHAK HOEJI
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    • v.47 no.6
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    • pp.422-431
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    • 2003
  • The use of recombinant human erythropoietin (rhEPO), a stimulator of erythropoiesis, banned in sports because of the medical risk associated with thrombosis. Due to analytical difficulties to differentiate between natural human EPO (hEPO) and rhEPO, blood parameters of erythropoiesis such as contents of hemoglobin (cut-off value <17.5 g/d l for man, and < 16.0 g/dl for women), hematocrit and reticulocytes (cut-off value <2.0%) were measured to focus the misuse of rhEPO. We conducted anti-doping test for 122 blood samples of the World Cup athletes. The mean values of key parameters are as follows; 14.5$\pm$1.0 g/dl for hemoglobin, 41.7$\pm$2.8% for hematocrit, and 1.3$\pm$0.4% for reticulocyte. Blood sample was found to be stable up to 8 hours for the reticulocyte measurement. In addition, the soluble transferrin receptor and ferritin levels were measured by immunoassay methods using plasma samples (n=28) in which the mean value was 0.8$\pm$0.5 $\mu\textrm{g}$/$m\ell$ and 54.6$\pm$33.7 ng/$m\ell$, respectively. The results indicate that all samples tested were negative for the blood parameters of indirect anti-doping test for hEPO misuse. The statistical evaluation suggest that several other parameters such as red blood cell, mean corpuscular hemoglobin concentration, mean corpuscular volume, mean corpuscular hemoglobin and white blood cell could be considered as factors influencing hEPO function in addition to five parameters mentioned.

Isolation and Characterization of Antitumor Agents from Dictamnus albus

  • Kim, Se-Won;Yeo, Woon-Hyung;Ko, Young-Su;Kim, Si-Kwan
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.209-214
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    • 1997
  • This study was carried out to find new antitumor agents from plant resource. Three cytotoxic agents were isolated from the root of Dictamnus albus by hexane extraction, silica gel column chromatography and HPLC. They were identified to be dictamnine $(C_{12}H_9NO_2)$, preskimmianine $(C_{17}H_{21}NO_4)$ and fraxinellone $(C_{14}H_{16}O_3)$ on the basis of spectroscopic evidences. In this study, it was newly found that these compounds possess a cytotoxic activity against lung lymphoma L1210 cell line. Among them. Preskimmianine was the most potent against the lymphoma L1210 with a $IC_{50}$ of $3.125\;{\mu}g/ml\;(10.3\;{\mu}M)$. Toxicity of preskimmianine against normal Iymphocyte was observed at the concentration of $50\;{\mu}g/ml\;(165\;{mu}M)$. These results support the pharmacological role of D. albus, a herb known as Paeksun in Korea and used as an anticancer agent in folk medicine.

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Biochemical Characterization of Alkaliphilic Cyclodextran Glucanotransferase from an Alkaliphilic Bacterium, Paenibacillus daejeonensis

  • Yang, So-Jin;Ko, Jin-A;Kim, Hae-Soo;Jo, Min-Ho;Lee, Ha-Nul;Park, Bo-Ram;Kim, Young-Min
    • Journal of Microbiology and Biotechnology
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    • v.28 no.12
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    • pp.2029-2035
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    • 2018
  • Cycloisomaltooligosaccharide glucanotransferase (CITase) was isolated from alkaliphilic Paenibacillus daejeonensis via an amino acid homology search for the reported CITase. The recombinant alkaliphilic CITase (PDCITase) from P. daejeonensis was expressed in an Escherichia coli expression system and purified as a single protein band of 111 kDa. PDCITase showed optimum activity at pH 8.0 and retained 100% of activity within a broad pH range (7.0-11.5) after 18 h, indicating alkaliphilic or alkalistable CITase properties. In addition, PDCITase produced CI-7 to CI-17, CI-18, and CI-19, which are relatively large cycloisomaltooligosaccharides yet to be reported. Therefore, these large cycloisomaltooligosaccharides can be applied to the improvement of water solubility of pharmaceutical biomaterials.

Equilibrium Binding of Wild-type and Mutant Drosophila Heat Shock Factor DNA Binding Domain with HSE DNA Studied by Analytical Ultracentrifugation

  • Park, Jin-Ku;Kim, Soon-Jong
    • Bulletin of the Korean Chemical Society
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    • v.33 no.6
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    • pp.1839-1844
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    • 2012
  • We have investigated binding between wild-type and mutant Heat Shock Factor (HSF) DNA binding domains (DBDs) with 17-bp HSE containing a central 5'-NGAAN-3' element by equilibrium analytical ultracentrifugation using multi-wavelength technique. Our results indicate that R102 plays critical role in HSE recognition and the interactions are characterized by substantial negative changes of enthalpy (${\Delta}H^0_{\theta}=-9.90{\pm}1.13kcal\;mol^{-1}$) and entropy (${\Delta}S^0_{\theta}=-12.46{\pm}3.77cal\;mol^{-1}K^{-1}$) with free energy change, ${\Delta}G^0_{\theta}$ of $-6.15{\pm}0.03kcal\;mol^{-1}$. N105 plays minor role in the HSE interactions with ${\Delta}H^0_{\theta}$ of $-2.54{\pm}1.65kcal\;mol^{-1}$, ${\Delta}S^0_{\theta}$ of $19.28{\pm}5.50cal\;mol^{-1}K^{-1}$ and ${\Delta}G^0_{\theta}$ of $-8.35{\pm}0.05kcal\;mol^{-1}$, which are similar to those observed for wild-type DBD:HSE interactions (${\Delta}H^0_{\theta}=-3.31{\pm}1.86kcal\;mol^{-1}$, ${\Delta}S^0_{\theta}=17.38{\pm}6.20cal\;mol^{-1}K^{-1}$ and ${\Delta}G^0_{\theta}=-8.55{\pm}0.06kcal\;mol^{-1}$) indicating higher entropy contribution for both wild-type and N105A DBD bindings to the HSE.

Treatment of Malodorous Waste Air Containing Ammonia Using Biofilter System (바이오필터시스템을 이용한 암모니아 함유 악취폐가스 처리)

  • Lee, Eun Ju;Park, Sang Won;Nam, Dao Vinh;Chung, Chan Hong;Lim, Kwang-Hee
    • Korean Chemical Engineering Research
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    • v.48 no.3
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    • pp.391-396
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    • 2010
  • In this research the characteristics of ammonia removal from malodorous waste-air were investigated under various operating condition of biofiilter packed with equal volume of rubber media and compost for the efficient removal of ammonia, representative source of malodor frequently generated at compost manufacturing factory and publicly owned facilities. Then the optimum conditions were constructed to treat waste-air containing ammonia with biofilter. Biofilter was run for 30 days(experimental frequency of 2 times/day makes 60 experimental times.) with the ammonia loading from $2.18g-N/m^3/h$ to $70g-N/m^3/h$ at $30^{\circ}C$. The ammonia removal efficiency reached almost 100% for I through IV stage of run to degrade up to the ammonia loading of $17g-N/m^3/h$. However the removal efficiency dropped to 80% when ammonia loading increased to $35g-N/m^3/h$, which makes the elimination capacity of ammonia $28g-N/m^3/h$ for V stage of run. However, the removal efficiency remained 80% and the maximum elimination capacity reached $55g-N/m^3/h$ when ammonia loading was doubled $70g-N/m^3/h$ for VI stage of run. Thus the maximum elimination capacity exceeded $1,200g-N/m^3/day$(i.e., $50g-N/m^3/h$) of the experiment of biofilter packed with rock wool inoculated with night soil sludge by Kim et al.. However, the critical loading did not exceed $810g-N/m^3/day$ (i.e., $33.75g-N/m^3/h$) of the biofilter experiment by Kim et al.. The reason to exceed the maximum elimination capacity of Kim et al. may be attributed to that the rubber media used as biofilter packing material provide the better environment for the fixation of nitrifying and denitrification bacteria to its surface coated with coconut based-activated carbon powder and well-developed inner-pores, respectively.