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Pharmacokinetics of KR-30075, A Potent Phosphodiesterase III Inhibitor in Rats (포스포디에스테라제 III의 저해물인 KR-30075의 흰쥐에서의 약물속도론)

  • Lee, Kwang-Pyo;Kim, Hyo-Jin;Kwon, Kwang-Il;Cho, Song-Ja
    • YAKHAK HOEJI
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    • v.36 no.3
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    • pp.259-268
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    • 1992
  • A procedure for the determination of KR-30075 and its metabolites in plasma and urine by high performance liquid chromatography is described. For the study of pharmacokinetic properties of KR-30075, a new PDE III inhibitor, the plasma concentration and urinary excretion after an oral administration of KR-30075 (4 mg/kg) in the male rat (Sprague Dawley) were determined by high performance liquid chromatography. The best extraction efficiency of KR-30075 and KR-30072 is obtained with ethyl ether adjusted to pH 4.0. Retention times of both KR-30072 and KR-30075 were within 5 min and resolution was complete at the flow rate of 1.0 ml/min. The sensitivity and specificity of this HPLC assay appears to be satisfactory for the pharmacokinetic study of KR-30075 and its metabolites. One-compartment open model with first-order absorption was applied to evaluate the pharmacokinetic parameters of KR-30075 according to Minimum AIC Estimation. $T_{max}$ was 1 hr, $C_{max}$ was $0.789{\pm}0.31\;{\mu}g/ml$ and elimination half $T_{1/2}$ was 6.31 min after oral administration of 4 mg/kg KR-30075 to male rats.

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The Analysis of Electron Transport Coefficients in Kr and Xe Atom Gas (Kr과 Xe 원자기체의 전자수송계수의 해석)

  • Jeon, Byung-Hoon
    • Journal of the Korean Institute of Illuminating and Electrical Installation Engineers
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    • v.22 no.8
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    • pp.104-108
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    • 2008
  • Accurate sets of electron collision cross sections and the electron transport coefficients for atoms and molecules are necessary for quantitative understanding of plasma phenomena Kr and Xe atom are used in many industrial applications, such as in PDP and fluorescent induction lamps(FILs). Therefore, we analysed and calculated the electron transport coefficients, the electron drift velocity W, the longitudinal and transverse diffusion coefficient $ND_L$ and $ND_T$, and the ionization coefficient $\alpha$/N in pure Kr and Xe gases over the wide E/N range from 0.001 to 500[Td] at 1[Torr] by two-tenn approximation of the Boltzmann equation.

Regional Variability of Manganese Nodule Facies in the KR1 Area in KODOS Area, Northeastern Equatorial Pacific (북동태평양 한국 KODOS 연구지역 중 KR1 지역 망간단괴의 지역적인 특성 변화)

  • Lee, Hyun-Bok;Kim, Wonnyon;Ko, Young-Tak;Kim, Jonguk;Chi, Sang-Bum;Park, Cheong-Kee
    • Economic and Environmental Geology
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    • v.45 no.5
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    • pp.477-486
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    • 2012
  • High-resolution bathymetry and physico-chemical properties of manganese nodules were explored to identify the relationship between morphological features and nodule occurrences in the KR1, one of the Korean contract nodule fields located in the NE Pacific. The high-resolution seabed mapping showed that the southwestern sector of the KR1 (KR1-1) was relatively deeper than the northeastern sector (KR1-2) which is occupied by small-scale seamounts. In terms of nodule occurrence, manganese nodules in the KR1-1 were comparatively larger (2-4 cm) with rough surface (t-type) and discoidal shapes (D-type), while those in the KR1-2 were generally small (<2 cm) with smooth surface (s-type) and irregular shapes (I-type). In addition, the nodules in the KR1-1 had higher contents of Cu, Mn and Ni. Such connections of water depths to nodule appearances and metal contents are commonly observed in the Pacific nodule fields. On the other hand, the nodules in the KR1-2 tend to be controled by morphological features. The seamounts in the KR1-2 might continuously provide rock fragments as new nuclei of manganese nodules. As a result, the nodules could not grow over than 2 cm and showed the shapes of a newbie (i.e., smooth surface and irregular shapes). As a result, our observations indicate that occurrence features of manganese nodules could be subjected to water depths and seabed morphology simultaneously.

Biological Properties of Vero Cell-Adapted Newcastle Disease Virus (Vero 세포적응 뉴캣슬병 바이러스의 생물학적 특성)

  • Choi, Kang-Seuk;Park, Mi-Ja;Kye, Soo-Jeong;Kim, Ji-Ye;Kwon, Jun-Hun
    • Korean Journal of Poultry Science
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    • v.39 no.2
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    • pp.113-120
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    • 2012
  • Newcastle disease virus (NDV) Kr005/V strain was generated through 55 serial passages of NDV Kr005 strain in Vero cells. The Kr005/V virus yielded high infective titers of $10^{7.8}$ $TCID_{50}/mL$ in Vero cells and the infected cells showed cytopathic effects such as marked cell rounding, though less frequent syncytia. The Kr005/V virus was heat-stable and classified into the lentogenic type with a Mean Death Time (MDT) of 120h or greater while the Kr005 strain was heat-labile and velogenic (MDT of 49.6 h). Only the single amino acid substitution (T to S) was observed at position 433 of the HN protein of the Kr005/V strain, whereas no amino acid change was found in the F protein. The Kr005/V input virus correlated well (correlation coefficient $r^2$=0.97) with the Kr005 virus when ten field sera were tested by virus neutralization test. The biological properties and usefulness of Vero cell-adapted Kr005/V virus were discussed.

Pharmacokinetic analysis for the development of new potent anti-HIV-1 agents, the KR-V series (새로운 항HIV-1제, KR-V series의 개발을 위한 약물동태연구)

  • Lee, Young-mi;Kim, Jin-suk;Han, Sang-seop;Shin, Ho-chul
    • Korean Journal of Veterinary Research
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    • v.40 no.3
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    • pp.471-478
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    • 2000
  • The pharmacokinetic properties of KR-V compounds, recently developed as new anti-HIV agents, were studied after i.v. and p.o. administration in rats. The concentrations of the KR-V series were determined in rat plasma using an high-performance liquid chromatography (HPLC)-UV detection system. Of the 19 KR-V compounds investigated in the present study, only KR-V 3, 10, 14, 16 and 18-1 showed oral bioavailability. The plasma concentration-time data could be adequately described by an one-compartment open model. In the i.v. kinetic study (10mg/kg), the CLt of KR-V 3, 10, 14 and 16 (>4L/hr/kg) were significantly higher than that of KR-V 18-1 (1.1 L/hr/kg). The AUC of KR-V 18-1 was greater ($8.97{\mu}g{\cdot}hr/ml$) than that of the other compounds, but the Vd (0.58 L/kg) was lower. In the p.o. kinetic study (50mg/kg), although the t-1/2 of KR-V 18-1 was shorter than that of the other compounds, the AUC ($3.659{\mu}g{\cdot}hr/ml)$ and $C_{max}(1.891{\mu}g/ml$) were markedly higher. In a seperated in vitro experiment, only KR-V 18-1, of the 5 compounds with bioavailibility, exhibits potent activity against HIV-1 mutant strains. Therefore, KR-V 18-1 is expected to become a new potent anti-AIDS drug candidate/lead compound.

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Characterization of the Physicochemical Properties of KR-31378

  • Sohn, Young-Taek;Park, Bo-Ye
    • Archives of Pharmacal Research
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    • v.26 no.7
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    • pp.526-531
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    • 2003
  • KR-31378 is a new drug candidate intended for the use in the prevention of ischemia-reperfusion damage. The objective of this preformulation study was to determine the physicochemical properties of KR-31378. The n-octanol to water partition coefficients of KR-31378 were 0.0504 at pH 3 and 0.8874 at pH 10. Accelerated stability of KR-31378 in solution and solid state was studied at 5, 40, $60^{\circ}C$. The stability testing indicated that the t90 for the drug in solid was estimated to be 2 years and 128.6 days at $25^{\circ}C$, while the that in aquesou solution was 68.6 days at $25^{\circ}C$. The KR-31378 was also found to be unstable under the relative humidity of 76%, probably because of the hygroscopic nature of the drug. In order to study compatibility of KR-31378 with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1:1 binary mixtures of KR-31378 and Aerosil, Avicel, Eudragit, lactose, PEG, talc, CMC, PVP, starch. As a result, CMC, PVP, and starch were found to be incompatible with KR-31378, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of KR-31378 powder was in the size range of 9-93 $\mu$ m with the mean particle size of 37.9 $\mu$ m. The flowability of KR-31378 was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Crystallization of the drug with a number of organic solvents did not lead a crystalline polymorphism. In addition, dissolution of the drug from the powder was adequately rapid at $37^{\circ}C$ in water.

Physicochemical Properties of Starches from Flavored Glutinous Rice Varieties (향미찹쌀전분의 이화학적 특성비교)

  • 최영희;김광호;강미영
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.30 no.5
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    • pp.765-769
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    • 2001
  • Starches of flavored glutinous rice were analyzed by using scanning electron microscope (SEM) and differential scanning calorimetry (DSC) and tested on the starch granule susceptibility to 15% H$_2$SO$_4$, glucoamylase and $\alpha$-amylase. The shape of starch granules form flavored glutinous rice varieties was polygonal and the size was 4~6 $\mu$m in diameter. According to DSC, glutinous rice starch showed onset temperature (T$_{o}$) range 59.8~62.5$^{\circ}C$ and KR92021-B-B-42-3-B and KR92021-B-B-165-1-B showed higher enthalpy ($\Delta$H) on gelatinization than others. The starches from KR92021-B-B-5-2-B and KR92021-B-B-42-3-B showed lower hydrolysis rate using 15% H$_2$SO$_4$ than KR92021-B-B-165-1-B. KR92021-B-B-5-2-B showed higher degree of hydrolysis of glucoamylase and $\alpha$-amylase than the others.

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Synovial Cell Migration is Associated with B Cell Activating Factor Expression Increased by TNFα or Decreased by KR33426

  • Lee, Jiyoung;Yoon, Sung Sik;Thuy, Pham Xuan;Moon, Eun-Yi
    • Biomolecules & Therapeutics
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    • v.28 no.5
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    • pp.405-413
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    • 2020
  • Fibroblast-like synoviocytes (FLS) play a crucial role in initiating rheumatoid arthritis. B-cell activating factor (BAFF) plays a role in FLS survival as well as in B cell maturation and maintenance. Here, we investigated whether tumor necrosis factor (TNF)-α-induced BAFF expression controls FLS migration and whether BAFF expression in FLS could be regulated by KR33426 which is the inhibitor of BAFF binding to BAFF receptors (BAFF-R) by using MH7A synovial cells transfected with the SV40 T antigen. More TNF-α-treated cells migrated compared to the control. TNF-α increased BAFF expression in FLS, significantly. FLS migration was inhibited by the transfection with BAFF-siRNA. KR33426 also inhibited BAFF expression increased by TNF-α treatment in FLS as judged by western blotting, PCR, and transcriptional activity assay. Kinases including JNK, p38 and Erk were activated by TNF-α treatment. While JNK and p38 were inhibited by KR33426 treatment, no changes in Erk were observed. Transcription factors including p65, c-Fos, CREB and SP1 were enhanced by TNF-α treatment. Among them, c-Fos was inhibited by KR33426 treatment. Small interference(si)-RNA of c-fos decreased BAFF transcriptional activity. FLS migration induced by TNF-α was inhibited by the transfection with BAFF-siRNA. KR33426 increased Twist, Snail, Cadherin-11 and N-Cadherin. In contrast, KR33426 decreased E-cadherin and TNF-α-enhanced CCL2. Taken together, our results demonstrate that synovial cell migration via CCL2 expression could be regulated by BAFF expression which is decreased by KR33426 and c-Fos-siRNA. It suggests for the first time that the role of BAFF-siRNA on FLS migration might be matched in the effect of KR33426 on BAFF expression.

Conversion of Ginsenoside Rb1 and Taxonomical Characterization of Stenotrophomonas sp. 4KR4 from Ginseng Rhizosphere Soil (인삼 근권 토양에서 분리한 Stenotrophomonas sp. 4KR4의 Ginsenoside Rb1 전환능 및 분류학적 특성)

  • Jeon, In-Hwa;Cho, Geon-Yeong;Han, Song-Ih;Yoo, Sun Kyun;Whang, Kyung-Sook
    • Korean Journal of Microbiology
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    • v.49 no.4
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    • pp.369-376
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    • 2013
  • We isolated the ${\beta}$-glucosidase producing bacteria (BGB) in ginseng root system (rhizosphere soil, rhizoplane, inside of root). Phylogenetic analysis of the 28 BGB based on the 16S rRNA gene sequences, BGB from rhizosphere soil belong to genus Stenotrophomonas (3 strains), Bacillus (1 strain), and Pseudoxanthomonas (1 strain). BGB isolates from rhizoplane were Stenotrophomonas (16 strains), Streptomyces (1 strain) and Microbacterium (1 strain). BGB from inside of root were categorized into Stenotrophomonas (3 strains) and Lysobacter (2 strains). Especially, Stenotrophomonas comprised the largest portion (approximately 90%) of total isolates and Stenotrophomonas was a dominant group of the ${\beta}$-glucosidase producing bacteria. We selected strain 4KR4, which had high ${\beta}$-glucosidase activity (108.17 unit), could transform ginsenoside Rb1 into Rd, Rg3, and Rh2 ginsenosides. In determining its relationship on the basis of 16S rRNA sequence, 4KR4 strain was most closely related to Stenotrophomonas rhizophila e-$p10^T$ (AJ293463) (99.62%). Therefore, on the basis of these polyphasic taxonomic evidence, the ginsenoside Rb1 converting bacteria 4KR4 was identified as Stenotrophomonas sp. 4KR4 (=KACC 17635).

Kriging Regressive Deep Belief WSN-Assisted IoT for Stable Routing and Energy Conserved Data Transmission

  • Muthulakshmi, L.;Banumathi, A.
    • International Journal of Computer Science & Network Security
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    • v.22 no.7
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    • pp.91-102
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    • 2022
  • With the evolution of wireless sensor network (WSN) technology, the routing policy has foremost importance in the Internet of Things (IoT). A systematic routing policy is one of the primary mechanics to make certain the precise and robust transmission of wireless sensor networks in an energy-efficient manner. In an IoT environment, WSN is utilized for controlling services concerning data like, data gathering, sensing and transmission. With the advantages of IoT potentialities, the traditional routing in a WSN are augmented with decision-making in an energy efficient manner to concur finer optimization. In this paper, we study how to combine IoT-based deep learning classifier with routing called, Kriging Regressive Deep Belief Neural Learning (KR-DBNL) to propose an efficient data packet routing to cope with scalability issues and therefore ensure robust data packet transmission. The KR-DBNL method includes four layers, namely input layer, two hidden layers and one output layer for performing data transmission between source and destination sensor node. Initially, the KR-DBNL method acquires the patient data from different location. Followed by which, the input layer transmits sensor nodes to first hidden layer where analysis of energy consumption, bandwidth consumption and light intensity are made using kriging regression function to perform classification. According to classified results, sensor nodes are classified into higher performance and lower performance sensor nodes. The higher performance sensor nodes are then transmitted to second hidden layer. Here high performance sensor nodes neighbouring sensor with higher signal strength and frequency are selected and sent to the output layer where the actual data packet transmission is performed. Experimental evaluation is carried out on factors such as energy consumption, packet delivery ratio, packet loss rate and end-to-end delay with respect to number of patient data packets and sensor nodes.