• Title/Summary/Keyword: Effective permeability

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Solubilization of Quercetin , and Permeability Study of Quercetin and Rutin to Rabbit Duodenal Mucosa (퀘르세틴의 가용화 , 퀘르세틴 및 루틴의 토끼 십이지장 점막 투과성)

  • Chun, In-Koo;Seo, Eun-Ha
    • YAKHAK HOEJI
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    • v.42 no.1
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    • pp.59-69
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    • 1998
  • To increase the solubility of quercetin, which is a practically insoluble flavonoid of Ginkgo biloba leaf, the effects of nonaqueous vehicles. Their cosolvents, water-sol uble polymers and modified cyclodextrins (CDs) were observed. Polyethylene glycols, diethyleneglycol monoethyl ether, and their cosolvents with water showed a good solvency toward quercetin. Also the aqueous solutions of povidone, copolyvidone and Cremophor RH 40 was effective in solubilizing quercetin. Complex formation of quercetin with ${\beta}$-cyclodextrin (${\beta}$-CD), dimethyl-${\beta}$-cyclodextiin (DMCD), 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD) and ${\beta}$-cyclodextrin sulfobutyl ether (SBCD) in water was investigated by solubility method at $37^{\circ}C$. The addition of CDs in water markedly increased the solubility of quercetin with increasing the concentration. AL type phase solubility diagrams were obtained with CDs studied. Solubilizaton efficiency by CDs was in the order of SBCD >> DMCD > HPCD > ${\beta}$-CD. The dissolution rates of quercetin from solid dispersions with copolyvidone, povidone and HPCD were much faster than those of drug alone and corresponding physical mixtures, and exceeded the equilibrium solubility (3.03${\pm}1.72{\mu}$g/ml). The permeation of quercetin through duodenal mucosa did not occur even in the presence of enhancers such as bile salts, but the permeation was observed when the mucus layer was scraped off. This was due to the fact that quercetin had a strong binding to mucin ($58.5{\mu}$g/mg mucin). However rutin was permeable to the duodenal mucosa. The addition of enhancer significantly increased the permeation of rutin in the order of sodium glycocholate.

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Transcriptome sequencing revealed the inhibitory mechanism of ketoconazole on clinical Microsporum canis

  • Wang, Mingyang;Zhao, Yan;Cao, Lingfang;Luo, Silong;Ni, Binyan;Zhang, Yi;Chen, Zeliang
    • Journal of Veterinary Science
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    • v.22 no.1
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    • pp.4.1-4.13
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    • 2021
  • Background: Microsporum canis is a zoonotic disease that can cause dermatophytosis in animals and humans. Objectives: In clinical practice, ketoconazole (KTZ) and other imidazole drugs are commonly used to treat M. canis infection, but its molecular mechanism is not completely understood. The antifungal mechanism of KTZ needs to be studied in detail. Methods: In this study, one strain of fungi was isolated from a canine suffering with clinical dermatosis and confirmed as M. canis by morphological observation and sequencing analysis. The clinically isolated M. canis was treated with KTZ and transcriptome sequencing was performed to identify differentially expressed genes in M. canis exposed to KTZ compared with those unexposed thereto. Results: At half-inhibitory concentration (½MIC), compared with the control group, 453 genes were significantly up-regulated and 326 genes were significantly down-regulated (p < 0.05). Quantitative reverse transcription polymerase chain reaction analysis verified the transcriptome results of RNA sequencing. Gene ontology enrichment analysis and Kyoto Encyclopedia of Genes and Genomes enrichment analysis revealed that the 3 pathways of RNA polymerase, steroid biosynthesis, and ribosome biogenesis in eukaryotes are closely related to the antifungal mechanism of KTZ. Conclusions: The results indicated that KTZ may change cell membrane permeability, destroy the cell wall, and inhibit mitosis and transcriptional regulation through CYP51, SQL, ERG6, ATM, ABCB1, SC, KER33, RPA1, and RNP genes in the 3 pathways. This study provides a new theoretical basis for the effective control of M. canis infection and the effect of KTZ on fungi.

Comparison of Physical Properties of Permeability Concrete Using Acrylic Polymer (아크릴 폴리머를 사용한 투수 콘크리트의 물성 비교 평가)

  • Hwang, Byoung-Il;Kim, Hyo-Jung
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.7
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    • pp.265-271
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    • 2019
  • The aim of this paper was to improve the shortcomings of Pitcher Concrete, a conventional ethylene-based polymer used in combination with the other components, and present basic data for use as improved road pavement material by applying an acrylic polymer. Existing ethylene polymer-based pitcher concrete materials were selected. Acrylic polymer was then added and the resulting mixture was evaluated. The compressive strength of the existing ethylene-based polymer pitcher concrete combination was low due to the large air gap, and a compressive strength of 24MPa was observed on the 28th day of road use, as defined by KS for an acrylic polymer-based pitcher concrete combination. Regarding the bending strength, the combined strength of the acrylic polymer-based pitcher concrete was excellent, and the factor of the pitcher was measured above the reference, 0.1(mm/s), in all variables. All parameters measured were less than 1%. The acrylic polymer mixing characteristics were able to maintain the dynamic modulus of elasticity for more than 120 cycles, but not more than 80 cycles for the other combinations. Therefore, the addition of more acrylic polymer than conventional ethylene polymer base is effective in improving the durability.

Polymer Electrolyte Membranes of Poly(Styrene-Butadiene-Styrene) Star Triblock Copolymer for Fuel Cell (연료전지용 Poly(Styrene-Butadiene-Styrene) Star Triblock Copolymer의 고분자 전해질 분리막)

  • Garcia, Edwin D.;Jung, Bumsuk
    • Membrane Journal
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    • v.29 no.5
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    • pp.252-262
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    • 2019
  • A sulfonated star branched poly(styrene-b-butadiene-b-styrene) triblock copolymer (SSBS) was synthesized with varying degrees of sulfonation. The effective sulfonation on the butadiene block was confirmed by FT-IR spectroscopy. Ion exchange capacity by titration was used to determine the degree of sulfonation. The synthesized polymer observed enhanced water uptake and proton conductivity. At room temperature, the SSBS with 25 mol% degree of sulfonation showed an outstanding proton conductivity of 0.114 S/cm, similar to that of commercial membrane, Nafion. The effect of temperature at constant relative humidity on conductivity resulted to a remarkable increase in proton conductivity. Methanol permeability studies showed a value lower than Nafion for all the sulfonated membranes. Structural nature observed using AFM showed that the membranes observed microphase separated nanostructures and the connectivity of the interionic channels.

Systemic Analysis of Antibacterial and Pharmacological Functions of Scutellariae Radix (시스템 약리학적 분석에 의한 황금의 항균효과)

  • Kim, Hyo Jin;Bak, Se Rim;Ha, Hee Jung;Kim, Youn Sook;Lee, Boo Kyun;An, Won Gun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.34 no.4
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    • pp.184-190
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    • 2020
  • This study was performed to find antibacterial substances contained in Scutellariae Radix (SR) using a systems pharmacological analysis method and to establish an effective strategy for the prevention and treatment of infectious diseases. Analysis of the main active ingredients of SR was performed using Traditional Chinese Medicine Systems Pharmacology (TCMSP) Database and Analysis Platform. 36 active compounds were screened by the parameter values of Drug-Likeness (DL), Oral Bioavailability (OB), and Caco-2 permeability (Caco-2), which were based on the drug absorption, distribution, metabolism, and excretion indicators. The UniProt database was used to obtain information on 159 genes associated with active compounds. The main active compounds with antibacterial effects were wogonin, β-sitosterol, baicalein, acacetin and oroxylin-A. Target proteins associated with the antibacterial action were chemokine ligand 2, interleukin-6, tumor necrosis factor, caspase-8,9 and mitogen-activated protein kinase 14. In the future, systems pharmacological analysis of traditional medicine will be able to make it easy to find the important mechanism of action of active substances present in natural medicines and to optimize the efficacy of medicinal effects for combinations of major ingredients to help treat certain diseases.

The Water-Soluble Chitosan Derivative, N-Methylene Phosphonic Chitosan, Is an Effective Fungicide against the Phytopathogen Fusarium eumartii

  • Mesas, Florencia Anabel;Terrile, Maria Cecilia;Silveyra, Maria Ximena;Zuniga, Adriana;Rodriguez, Maria Susana;Casalongue, Claudia Anahi;Mendieta, Julieta Renee
    • The Plant Pathology Journal
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    • v.37 no.6
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    • pp.533-542
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    • 2021
  • Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. N-Methylene phosphonic chitosan (NMPC) is a water-soluble derivative prepared by adding a phosphonic group to chitosan. This study demonstrates that NMPC has a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii) judged by the inhibition of F. eumartti mycelial growth and spore germination. NMPC affected fungal membrane permeability, reactive oxygen species production, and cell death. Also, this chitosan-derivative exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens to exert fungicide action. In addition to water solubility, the selective biological cytotoxicity of NMPC adds value in its application as an antimicrobial agent in agriculture.

Physical Properties of Liquid Ammonia Wood for Bending (휨가공을 위한 액체암모니아 처리재의 물리적 성질)

  • Kang, Ho-Yang
    • Journal of the Korean Wood Science and Technology
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    • v.31 no.1
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    • pp.52-60
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    • 2003
  • The physical properties of small hardwood and softwood specimens treated with liquid ammonia were investigated. The specimens treated for 4 or 18 hours were compared with the controls. The EMCs of the liquid ammonia treated specimens were higher than those of the controls when conditioned at the same humidities. However once oven-dried they didn't show any significant differences in EMCs. With the increase of liquid ammonia treatment time specimens shrank in radial and tangential directions, but not in longitudinal direction. As liquid ammonia treatment time increased the ultrasonic velocities of specimens decreased and their densities increased, thus their dynamic MOEs decreased. For chestnut specimens the presteamed were more plasticized than the liquid ammonia treated. Incising on the surfaces of specimens didn't improve liquid ammonia permeability in both hardwoods and softwoods. Liquid ammonia treatment was very effective for plasticizing 5 mm thick softwoods. Relative dielectric constants and thermal conductivities were measured with both liquid ammonia treated and control specimens.

Anti-rheumatoidal Arthritis Effect of Sulfuretin Isolated from Rhus veniciflua

  • Park, J.W.;B.J. Yoon;Park, J.K.;Lee, K.T.;Y.N. Han;Park, H.J.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.84-84
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    • 2001
  • The heartwood of Rhus verniciflua has been known to be effective for lingering intoxication and diabetes mellitus and rheumatoidal arthritis in traditional folk medicine in Korea. We have previously reported that antimutagenic effect of flavonoids derived from the heartwood extract of R. verniciflua, and sulfuretin was the active component. Recently, we have demonstrated that sulfuretin could be an anti-inflammatory principle of the R. verniciflua heartwood partially dependent on cyclooxigenase-inhibitory activity. The present study was undertaken to demonstrate the anti-rheumatoidal arthritis effect of the R. verniciflua heartwood extract, its EtOAc fraction and the main flavonoids, sulfuretin and fustin. All the test samples showed variably significant inhibitory effects on hind paw edema induced by Freund's complete adjuvant reagent (FCA reagent). Sulfuretin treatment with 10 mg/kg (i.p.) for seven days showed the inhibitory effect of 54.2${\pm}$3.0%, Similar trends in RA- and CRP tests, vascular permeability test and trypsin inhibitor test were also found. In addition, no dead mouse was found even when the dose was increased up to 5,000 mg/kg (i.p.). Treatment with 250-1,500 mg/kg on normal rats did not show any marked toxicological significances in the tests of body weight gain, wet weight of organs and hepatic functions. These results suggested that the heartwood of R. verniciflua could be an adequate crude drug for rheumatoidal arthritis with an active component of sulfuretin. The toxicological safety of the heartwood of R, verniciflua is contrasted to known severe allergenic action of the stem bark or its exudate.

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THE MAGNETIC PROPERTIES OF Co-Ni-Fe-N SOFT MAGNETIC THIN FILMS

  • Kim, Y. M.;Park, D.;Kim, K. H.;Kim, J.;S. H. Han;Kim, H. J.
    • Proceedings of the Korean Magnestics Society Conference
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    • 2000.09a
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    • pp.492-499
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    • 2000
  • Co-Ni-Fe-N thin films were fabricated by a N$\sub$2/ reactive rf magnetron sputtering method. The nitrogen partial pressure (P$\sub$N2/) was varied in the range of 0∼10%. As P$\sub$N2/ increases in this range, the saturation magnetization (B$\sub$s/) linearly decreases from 19.8 kG to 14 kG and the electrical resistivity ($\rho$) increased from 27 to 155 ${\mu}$$\Omega$cm. The coercivity (H$\sub$c/) exhibits the minimum value at 4% of P$\sub$N2/. The magnetic anisotropy (H$\sub$k/) are in the range of 20∼50 Oe. High frequency characteristics of (Co$\sub$22.2/Ni$\sub$27.6/Fe$\sub$50.2/)$\sub$100-x/N$\sub$x/ films are excellent in the range of 3∼5% of P$\sub$N2/. Especially the effective permeability of the film fabricated at 4% of P$\sub$N2/ is 800, which is maintained up to 600 MHz. This film also shows Bs of 17.5 kG, H$\sub$c/ of 1.4 Oe, resistivity of 98 $\Omega$cm and H$\sub$k/ of about 25 Oe. Also, the corrosion resistance of (Co$\sub$22.2/Ni$\sub$27.6/Fe$\sub$50.2/)$\sub$100-x/N$\sub$x/ were improved with the increase in N concentration.

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Numerical Analysis on Drained and Undrained Pullout Capacity in Reinforced Soil (보강토에서의 배수 및 비배수 인발력에 대한 수치해석)

  • Lee, Hong-Sung;Son, Moo-Rak
    • Journal of the Korean Geotechnical Society
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    • v.23 no.4
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    • pp.113-123
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    • 2007
  • In order to ensure the stability of reinforced structures backfilled with low permeability soil, it is very important to determine the change in undrained pullout capacity compared to drained pullout capacity prior to design. In this research, a series of numerical analyses on laboratory pullout tests have been performed on different materials (clean sand, 5, 10, and 15% silty sand), different overburden pressures (30, 100 and 200 kPa), and different drainage conditions (drained and undrained) in order to compare drained pullout capacity with undrained pullout capacity. The results of numerical analysis also have been compared with the results of the laboratory pullout tests. The analysis results show that both drained and undrained pullout capacity are influenced by silt contents and increase with increase of friction angle of the soil and overburden pressure. In undrained condition, the effective stresses acting on the reinforcement decrease as excessive pore pressures are generated, resulting in decrease in pullout capacity; 57% for 30 kPa, and 70% for 100 and 200 kPa. These results show a good agreement with the results of the laboratory pullout tests performed under the same condition.