• Title/Summary/Keyword: p-conjugate.

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Urokinase Conjugated with Water-Soluble Dextran

  • Kim Nam Deuk;Kim Hyun-Pyo;Byun Si Myung;Kim Sung Wan
    • Bulletin of the Korean Chemical Society
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    • v.6 no.4
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    • pp.210-214
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    • 1985
  • Urokinase, a plasminogen activator, was conjugated with dextran by the cyanogen bromide activation-coupling method. The resulting water-soluble conjugate was purified by gel permeation chromatography on Sephadex G-200. The maximal activity was obtained when the ratio of urokinase/dextran was 1/20 for the coupling. The final preparation showed 5 CTA units/mg conjugate, 300 CTA units/mg protein, 8.4 % activity retention, and 47 % protein retention. The urokinase-dextran conjugate had good thermal, pH and storage stabilities. In addition, it showed greater resistance to the inhibitory effect of human plasma than native urokinase. Also in vitro biological half-life of urokinase increased 40 times by this conjugation. In view of activity, excellent stability and increased half-life, the conjugate can be a potential fibrinolytic agent in an injectable form.

In vitro Drug Release Characteristics of Methotrexate-Human Serum Albumin and 5-Fluorouracil-Acetic Acid Human Serum Albumin Conjugates

  • Kim, Chong-Kook;Lee, Myung-Gull;Park, Man-Ki-Heejoo;Lee, Hae-Jin;Kang, Hae-Jin
    • Archives of Pharmacal Research
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    • v.12 no.3
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    • pp.186-190
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    • 1989
  • The release rates of methotrexate (MTX) from MTX-human serum albumin (HSA) conjugate, and 5-fluorouracil (5-FU) from 5-FU acetic acid (AA)-HSA conjugate were determined after incubation of the conjugates in various conditions. The concentrations of 5-FU released from the conjugate increased monoexponentially, however those of MTX increased biexponentially in all studies. It indicated that there are two distinct types of MTX-HSA linkage, weakly and tightly bound linkages. The release rates of 5-FU were lower than those of MTX in all studies indicating that the bond of 5-FU-AA-HSA conjugate is very stable, which is supported by the higher value of activation energy (39. 9 vs 10. 7 Kcal/mole) using Arrhenius equation. The release rates of MTX and 5 -FU from the conjugates increased with incubation temperatures. Proteolytic enzyme and liver homogenates accelerated significantly the release rates of MTX and 5-FU. Approximately 1.30 and 22.0% of MTX were released after 12 hours of incubation in the absence and presence of protease, respectively. The corresponding values for 5-FU were released after 12 hours of incubation with rat liver homogenates which were diluted 6 times with phosphate buffer of pH 6.0. The MTX-HSA and 5-FU-AA-HSA conjugates were very stable in rat plasma.

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An Animal Model to Evaluate the Protective Efficacy of Haemophilus influenzae Type b Conjugate Vaccines

  • Kim Hyun Sung;Yoo Tae Hyeon;Jang Yang Suk;Kim Hun;Park Jin Yong;Hur Byung Ki;Ryu Yeon Woo;Kim Jong Su
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.9 no.6
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    • pp.490-494
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    • 2004
  • An efficacy test of PRP (polyribosylribitol phosphate)-TT (Tetanus toxoid) conjugate vaccines was carried out using BALB/c mice as an animal model by inoculating Haemophilus in­fluenzae type b (Hib) with a virulence enhancement factor (VEF). Three administrations of the conjugate vaccines at 2-week intervals elicited a significantly high level of PRP antibodies (P>0.0001). The protective activity of the PRP immunization was challenged with either Hib with iron dextran (Hib/) or with a combination of mucin and hemoglobin (Hibmh) as a VEF. The me­dium lethal dose $(LD_{50})$ for Hibmh and Hibiwas measured as 10 CFU (Colony Forming Unit) and $2.5{\times}10^{8}$ CFU respectively. Each immunized animal was challenged with five or ten times the $LD_{50}$ level of bacteria with a VEF. A significant difference in mortality between the immunized and control mice (P> 0.01) was observed with the Hibmh challenge inoculation but not with the Hibi challenge inoculation. These results show that a combination of mucin and hemoglobin was able to enhance the virulence of Hib in BALB/c mice to cause a lethal infection, thus suggesting that BALB/c mice introduced to this method can be an effective model animal for testing the protective efficacy of H. influenzae conjugate vaccines.

Kinetics and Hydrolysis Mechanism of Herbicidal N-(2,6-dimethoxypyrimidin-2-yl)aminocarbonyl-2-(1-hyd roxy-2-fluoroethyl)benzenesulfonamide Derivatives (제초성, N-(2,6-dimethoxypyrimidin-2-yl)aminocarbonyl-2-치환(Z)-6-(1-hyd roxy-2-fluoroethyl)benzenesulfonamide 유도체의 가수분해 반응 메카니즘)

  • Lee, Chan-Bog;Ryu, Jae-Wook;Kim, Dae-Whang;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.38 no.5
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    • pp.455-462
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    • 1995
  • The new six herbicidal N-[(pyrimidin-2-yl)aminocarbonyl]-2-substituted-6-(1-hydroxy-2-fluoroethyl)benzenesulfonamide derivatives(S) were synthesized and rate constants for the hydrolysis of thier in the range of pH $1.0{\sim}10.0$ have been studied in 15%(v/v) aqueous acetonitrile solution at $45^{\circ}C$. From the basis of the results, pH-effect, solvent effect, ortho-substituent effect, thermodynamic parameters(${\Delta}H^{\neq}$ & ${\Delta}S^{\neq}$), pKa constant(4.80), rate equation, analysis of hydrolysis products(2-(1-hydroxy-2-fluoroethyl)benzenesulfonamide & 4,6-dimethoxyaminopyrimidine), it may be concluded that the general acid catalyzed hydrolysis through $A-S_E2$ mechanism and specific acid catalyzed hydrolysis through A-2 type(or $A_{AC}2$) mechanism proceeds via conjugate acid($SH^+$) and tetrahedral intermediate(I) below pH 8.0, whereas, above pH 9.0, the general base catalyzed hydrolysis by water molecules(B) through $(E_1)_{anion}$ mechanism proceeds via conjugate base(CB). In the range between $pH\;7.0{\sim}pH\;9.0$, these two reactions occur competitively.

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Synthesis and characterization of transferrin-polyethylenimine conjugate for targeted gene delivery

  • Lee, Kyung-Man;Kim, In-Sook;Shin, Sang-Chul;Oh, In-Joon
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.315.2-316
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    • 2003
  • Polyethylenimine (PEI) has been used as a non-viral gene delivery carrier. To improve the efficacy of transfection, transferrin was incorporated by covalent linkage to PEI. As a model plasmid DNA, pHME185/b-gal, a mammalian expression vector was used. The transferrin-polyethylenimine (TfPEI) was synthesized by conjugate PEI with transferrin using sodium periodateand and characterized by FT-IR and 1H-NMR. (omitted)

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On a Reverse of the Slightly Sharper Hilbert-type Inequality

  • Zhong, Jianhua
    • Kyungpook Mathematical Journal
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    • v.49 no.4
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    • pp.731-742
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    • 2009
  • In this paper, by introducing parameters ${\lambda}$, ${\alpha}$and two pairs of conjugate exponents (p, q), (r, s) and applying the improved Euler-Maclaurin's summation formula, we establish a reverse of the slightly sharper Hilbert-type inequality. As applications, the strengthened version and the equivalent form are given.

Self-starting vector phase conjugate laser oscillator in inverted Nd:YAG

  • Kim, D.H.;Udaiyan, D.;Green, R.P.M.;Crofts, G.J.;Damzen, M.J.
    • Journal of the Optical Society of Korea
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    • v.1 no.1
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    • pp.41-43
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    • 1997
  • We report the operation of a self-adaptive vector phase conjugate laser (VPCL) oscillator which compensates intracavity polarization distortion and wavefront aberration simultaneously. The VPCL in Nd:YAG gain media produce an output with energy of 125mJ in a 20ns single-longitudinal-mode pulse at 10Hz, which is unaffected by intracavity polarization distortion.

A Study on Poisson-lognormal Model (포아송-로그정규분포 모형에 관한 연구)

  • 김용철
    • The Korean Journal of Applied Statistics
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    • v.13 no.1
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    • pp.189-196
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    • 2000
  • Conjugate prior density families were motivated by considerations of tractability in implementing the Bayesian paradigm. But we consider problem that the conjugate prior p($\Theta$) cannot be used in restriction of the parameter $\Theta$. This article considers the nonconjugate prior problem of hierarchical Poisson model. We demonstrate the use of latent variables for sampling non-standard densities which arise in the context of the Bayesian analysis of non-conjugate by using a Gibbs sampler.

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COMPARISON OF FINITE ELEMENT SOLUTIONS WITH THOSE OF ANSYS-FLUENT IN A CONJUGATE HEAT TRANSFER PROBLEM (복합 열전달 해석에서 유한요소 해와 Ansys-Fluent 해의 비교)

  • Jeon, B.J.;Choi, H.G.;Lee, D.H.;Ha, J.P.
    • 한국전산유체공학회:학술대회논문집
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    • 2011.05a
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    • pp.86-87
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    • 2011
  • In this paper, a conjugate heat transfer around cylinder with heat generation was investigated. Both forced convection and conduction was considered in the present finite element simulation. A finite element formulation based on SIMPLE type algorithm was adopted for the solution of the incompressible Navier-Stokes equations. We compared the finite element solution with that of Ansys fluent 12.0, in which finite volume method was employed for spatial discretization. It was found that the finite element method gave more accurate solution than Ansys fluent 12.0. Further, it was found that the maximum temperature inside cylinder is positioned at the rear side due to the flow separation.

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The Efficacy of 9-($\beta$-D-Arabinofuranosyl)adenine and its Conjugate of Prednisone (BR-8702-AP) in the Treatment of Herpes simplex Virus Type 1 Encephalitis in Mice (단순 포진 바이러스 감염 생쥐에 대한 아데닌 아라비노사이드와 그의 프레드니손 결합화합물인 BR-8702-AP의 항바이러스 효과)

  • 채희상;신원섭;신현종;백우현
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.98-102
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    • 1993
  • The therapeutic effectiveness of adenine arabinoside(tora-A) and its conjugate of prednisone(BR-8702-AP) was compared in Herpes simplex Virus Type 1 (HSV-1) infected BALB/C mice. The BALB/C mouse was infected with HSV-1(700 PFU/mouse) intranasally. Among mice infected intranasally with virus, a mortality rate of 100% was observed. On the oral administration of non-toxic doses of ara-A or BR-8702-AP(125 mg /kg/day) for 5 consecutive days 2 hours after virus infection, the tora-A was highly effective in reducing mortality to 0% (P<0.001) and BR-8702-AP was also effective in reducing mortality to 15% (P<0.01). In this model infection, the virus was first replicated in the lung and transmitted to the brain. Both arts-A and BR-8702-AP did not inhibit the viral replication in the lung, but they inhibited the viral transmission to the brain. However, the BR-8702-AP was less effective than the aria-A to prevent transmission of virus to brain. Therefore, the reduced mortality due to tora-A or BR-8702-AP therapy was associated with inhibition of viral transmission to brain.

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