Synthesis and evaluation of a radioiodinated trisaccharide derivative as a synthetic substrate for a sensitive N-acetylglucosaminyltransferase V radioassay.

N-acetylglucosaminyltransferase V (GnT-V) is one of the most relevant glycosyltransferases to tumor invasion and metastasis. Based on previous findings of molecular recognition between GnT-V and synthetic substrates, we designed and synthesized a p-iodophenyl-derivatized trisaccharide, 2-(4-iodophenyl)ethyl 6-O-[2-O-(2-acetamido-2-deoxy-β-d-glucopyranosyl)-α-d-mannopyranosyl]-β-d-glucopyranoside (IPGMG, 1) and its radiolabeled form, [(125)I]IPGMG ([(125)I]1), for use in assays of GnT-V activity in vitro. The tributyltin derivative, 2-[4-(n-tributylstannyl)phenyl]ethyl 6-O-[2-O-(3, 4, 6-tri-O-acetyl-2-acetamido-2-deoxy-β-d-glucopyranosyl)-3, 4, 6-tri-O-acetyl-α-d-mannopyranosyl]-2, 3, 4-tri-O-acetyl-β-d-glucopyranoside (21), was synthesized as a precursor for the preparation of [(125)I]1. The iododestannylation of 21 using hydrogen peroxide as an oxidant followed by deacetylation yielded [(125)I]1. When [(125)I]1 was incubated in GnT-V-expressing cells with a UDP-GlcNAc donor, the production of β1-6GlcNAc-bearing IPGMG (IPGGMG, 2) was confirmed by radio-HPLC. In kinetic analysis, 1 was found to be a good substrate with a K(m) of 23.7μM and a V(max) of 159pmol/h. μg protein. [(125)I]1 would therefore be a useful synthetic substrate for the quantitative determination of GnT-V activity

Absorbed dose simulation of meta-211At-astato-benzylguanidine using pharmacokinetics of 131I-MIBG, and the novel dose conversion method, RAP

Objective We aimed to estimate in vivo 211At-labeled meta-benzylguanidine (211At-MABG) absorbed doses by the two dose conversion methods, using 131I-MIBG biodistribution data from a previously reported neuroblastoma xenograft model. Additionally, we examined the effects of different cell lines and time limitations using data from two other works.Methods We used the framework of the Monte Carlo method to create 3200 virtual experimental data sets of activity concentrations (kBq/g) to get the statistical information. Time activity concentration curves were produced using the fitting method of a genetic algorithm. The basic method was that absorbed doses of 211At-MABG were calculated based on the medical internal radiation dose formalism with the conversion of the physical half-life time of 131I to that of 211At. We have further improved the basic method, that is a novel dose conversion method, RAP (RAtio of Pharmacokinetics), using percent injected dose/g.Results Virtual experiments showed that 211At-MABG and 131I-MIBG had similar properties of initial activity concentrations and biological components, but the basic method did not simulate the 211At-MABG dose. Simulated 211At-MABG doses from 131I-MIBG using the RAP method were in agreement with those from 211At-MABG, so that their boxes overlapped in the box plots. The RAP method showed applicability to the different cell lines, but it was difficult to predict long-term doses from short-term experimental data.Conclusions The present RAP dose conversion method could estimate 211At-MABG absorbed doses from the pharmacokinetics of 131I-MIBG with some limitations. The RAP method would be applicable to a large number of subjects for targeted nuclide therapy

Nonclinical study and applicability of the absorbed dose conversion method with a single biodistribution measurement for targeted alpha-nuclide therapy

We derived a new formalism of the RAP dose conversion method at time t. In addition, we acquired a formula to determine the optimal timing of a single measurement of the percent injected dose/g, assuming the one-compartment model for biological clearance.　We investigated the new formalism’s performance using a representative RAP coefficient with radioactive-decay weighting. Dose conversions by representative RAP coefficients predicted the true [211At]MABG absorbed doses with an error of 10% or less. The inverses of the representative RAP coefficients plotted at 4 h post-injection, which was the optimal timing reported in the previous work, were very close to the new inverses of the RAP coefficients 4 h post-injection. Next, the behavior of the optimal timing was analyzed by radiolabeled compounds with physical half-lives of 7.2 h and 10 d on various biological clearance half-lives. Behavior maps of optimal timing showed a tendency to converge to a constant value as the biological clearance half-life of a target increased. The areas of optimal timing for both compounds within a 5% or 10% prediction error were distributed around the optimal timing when the biological clearance half-life of a target was equal to that of the reference. Finally, an example of RAP dose conversion was demonstrated for [211At]MABG

Numerical Analysis of One-Dimensional Plasma Flow with MHD Interaction (Constant-velocity, constant-temperature and constant-pessure conditions)

In this study some of the numerical analyses of one-dimensional compressible flow with magnetohydrodynamic (MHD) interaction have been carried out. A detailed study of this type of flow is vital for an understanding of many practical devices, such as the MHD generator, accelerator and pump. The steady conservation equations, coupled with the generalized Ohm\u27s law, were solved. Numerical results for channels with flows of constant velocity, temperature and pressure, respectively, could be obtained, but a rather peculiar area variation is required. As in the case of a constant velocity flow, the channel can be classified into a total of three possible types dependent on the load factor, and the flow Mach number decreases with an increase in the load factor. On the other hand, in the case of a constant temperature flow, the flow Mach number increases with an increase in the load factor. There is some precise set of initial flow properties that flow velocity reaches sonic and smooth acceleration or deceleration through sonic condition occurs

Numerical Analysis of Plasma Flow in Constant-area Channel with MHD Interaction

Numerical analysis has been carried out to explain and predict MHD effects, the choking phenomena and the occurrence of a shock wave in plasma flow with MHD interaction. This study is intended to provide one of data bases for a large scale flow with MHD interaction. The steady one-dimensional conservation equation, coupled the generalized Ohm’s law are solved. It was shown that, on account of the effect of the Joule heating and Lorentz force attractive possibilities was found for controlled acceleration or deceleration of plasma at subsonic and supersonic speeds, even in constant-area channe1. The behavior of the flow is characteristically different in different regimes of Mach Number and flow speed relative to certain significant speeds that are dependent on load factor

Visual Study of Supersonic Plasma Flow in Constant Area MHD Channel

The purpose of the present paper is to report the results of visual studies of the supersonic plasma flow in the Faraday type MHD generator with constant area channel. The plasma for MHD generator is produced using a shock tube. In order to obtain a clear and sharp image of the supersonic plasma flow in MHD generator channel, the color schlieren method has been employed. The experimental results show clearly shock waves and Prantle-Meyer fans in MHD channel. In the case of the flush mounted electrode channel, the adjusting wave is formed at the end of channel and moves to upstream. The pressure increases smoothly and the flow Mach number decreases from supersonic to subsonic through the adjusting wave. The plasma flow in a channel with protruded electrodes is also investigated, and the characteristics of the multiple shock wave which appear between electrodes are discussed

MHD 相互作用を伴うプラズマ流れの数値解析（等速，等温及び等圧条件の場合）

In this study some of the numerical analyses of one-dimensional compressible flow with magnetohydrodynamic (MHD) interaction have been carried out. A detailed study of this type of flow is vital for an understanding of many practical devices, such as the MHD generator, accelerator and pump. The steady conservation equations, coupled with the generalized Ohm's law, were solved. Numerical results for channels with flows of constant velocity, temperature and pressure, respectively, could be obtained, but a rather peculiar area variation is required. As in the case of a constant velocity flow, the channel can be classified into a total of three possible types dependent on the load factor, and the flow Mach number decreases with an increase in the load factor. On the other hand, in the case of a constant temperature flow, the flow Mach number increases with an increase in the load factor. There is some precise set of initial flow properties that flow velocity reaches sonic and smooth acceleration or deceleration through sonic condition occurs

断面積一定流路におけるMHD相互作用を伴うプラズマ流れの数値解析

Numerical analysis has been carried out to explain and predict MHD effects, the choking phenomena and the occurrence of a shock wave in plasma flow with MHD interaction. This study is intended to provide one of data bases for a large scale flow with MHD interaction. The steady one-dimensional conservation equation, coupled the generalized Ohm’s law are solved. It was shown that, on account of the effect of the Joule heating and Lorentz force attractive possibilities was found for controlled acceleration or deceleration of plasma at subsonic and supersonic speeds, even in constant-area channe1. The behavior of the flow is characteristically different in different regimes of Mach Number and flow speed relative to certain significant speeds that are dependent on load factor

Assessment Report of Doctoral Theses

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