• Archives of Pharmacal Research
• /
• v.20 no.1
• /
• pp.53-57
• /
• 1997

For the purpose of defining the effects of the N-substituted alkyl groups on the anticonvulsant activities of N-Cbz-.alpha.-aminosuccinimides, various (R)- and (S)-N-alkyl substituted N-Cbz-.alpha.-aminosuccinimides (1 and 2) were prepared from the corresponding (R)- and (S)-N-Cbz-aspartic acid by using known reaction and were evaluated the anticonvulsant activies in the MES and PTZ tests, including their neurotoxicities. The most active compound in the MES test was (R)N-Cbz-.alpha.-amino-N-methylsuccinimide (1b) $(ED_{50}=52.5 mg/kg, Pl=3.2)$. And in case of the PTZ test, (R)-N-Cbz-.alpha.-amino-N-ethylsuccinimide (1c) was the most active compound $(ED_{50}/=32.5mg/kg, Pl=3.1)$. The order of anticonvulsant activities of these compounds against the MES test, as judged from the ED_50values for the R series (1), was N-methyl > N-isobutyl > non-substituted > N-ethyl, N-allyl > N-benzyl compound; for the S series (2) N-methyl > N-altyl > non-substituted > N-isobutyl > N-ethyl > N-benzyl compound. The anticonvulsant activities in the PTZ tests of these compounds exhibited somewhat different pattern ; for the R series (1) Nethyl > N-methyl > N-isobutyl> non-substituted > N-allyl > N-benzyl compound in order of decreasing activity; for S series (2) N-ethyl > N-allyl, non-substituted > N-isobutyl > N-methyl > N-benzyl compound in order of decreasing activity.

• Geotechnical Engineering
• /
• v.10 no.1
• /
• pp.63-70
• /
• 1994

In-situ soil is anisotropically consolidated at rest, and the coefficient of earth pressure at rest $K_0$ is dependent on the properties of soil and stress history. In order to estimate roughly the in-situ undrained shear strength of a $K_0$-anisotropically normally consolidated clay from isotropic consolidated undrained test, consolidated undrained shear testy with four different consolidation pressure ratios ($K={\sigma}'_{3c}/{\sigma}'_{1c}$) were performed and test results showed K-$\alpha$ relationship, representing the strength ratio $\alpha$ as ($S_u/{\sigma}'_{1c})_{CKU}=\alpha(S_u/{\sigma}'_{1c})_{CIU}$. Strength ratio u increases with increasing consolidation pressure ratio. And the angle of internal friction $\Phi'$and angle ratio $\Phi'_{CKU}/\Phi'_{CIU}/$ are increased with the increament of K-value.

• Journal of applied mathematics & informatics
• /
• v.26 no.1_2
• /
• pp.15-27
• /
• 2008

We present and discuss an algorithm for the numerical solution of initial value problems of the form $D_*^\alpha$y(t) = f(t, y(t)), y(0) = y0, where $D_*^\alpha$y is the derivative of y of order $\alpha$ in the sense of Caputo and 0<${\alpha}{\leq}1$. The algorithm is based on the fractional Euler's method which can be seen as a generalization of the classical Euler's method. Numerical examples are given and the results show that the present algorithm is very effective and convenient.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.41 no.2
• /
• pp.143-150
• /
• 2015

This study demonstrates an effective one-pot regioselective synthesis of 3,7-diarylpyrazolo [1,5-${\alpha}$]pyrimidines. Moreover, the derivatives obtained were effective CB1R antagonists. These pyrazolo [1,5-${\alpha}$]pyrimidines with diaryl groups at the 3,7-positions are potential pharmacophores for CB1R candidates.

• Journal of agriculture & life science
• /
• v.44 no.5
• /
• pp.29-33
• /
• 2010

Soybean (Glycine max (L.) Merr.) seed is the main source of protein and oil for human and animal. The use of soybean protein has been expanded in the food industry due to their excellent nutritional benefits. But, antinutritional and allergenic factors are exist in the raw mature soybean. Lipoxygenase, Kunitz trypsin inhibitor (KTI) protein, and ${\alpha}^{\prime}-subunit$ of 7S globulin are main antinutritional factors in soybean seed. Breeding of a new soybean strain with lacking these components is needed. The objective of this research was to select new soybean line with lipoxygenase-free, KTI-free, and ${\alpha}^{\prime}-subunit$ free (lx1lx1lx2lx2lx3lx3titicgy1cgy1 genotype). Total 434 $F_2$seeds were obtained from the cross of cultivar, "Gaechuck#2" and PI506876. Presence and absence of lipoxygenase, KTI protein, and ${\alpha}^{\prime}-subunit$ of 7S globulin was tested by SDS electrophoresis using a partial seed of each $F_2$seed. Only one $F_2$seed with lacking these three components was selected and was planted to $F_2$plant. Absence of lipoxygenase, KTI, and ${\alpha}^{\prime}-subunit$ protein was confirmed on the $F_3$seeds harvested. Selected line with lx1lx1lx2lx2lx3lx3titicgy1cgy1 genotype might be useful for soybean breeding.

• Bulletin of the Korean Chemical Society
• /
• v.2 no.3
• /
• pp.96-104
• /
• 1981

(1) The flow data of f (stress) and ${\dot{s}$ (strain rate) for Fe and Ti alloys were plotted in the form of f vs. -ln ${\dot{s}$ by using the literature values. (2) The plot showed two distinct patterns A and B; Pattern A is a straight line with a negative slope, and Pattern B is a curve of concave upward. (3) According to Kim and Ree's generalized theory of plastic deformation, pattern A & B belong to Case 1 and 2, respectively; in Case 1, only one kind of flow units acts in the deformation, and in Case 2, two kinds flow units act, and stress is expressed by $f={X_1f_1}+{X_2f_2}$where $f_1\;and\;f_2$ are the stresses acting on the flow units of kind 1 and 2, respectively, and $X_1,\;X_2$ are the fractions of the surface area occupied by the two kinds of flow units; $f_j=(1/{\alpha}_j) sinh^{-1}\;{\beta}_j{{\dot{s}}\;(j=1\;or\;2)$, where $1/{\alpha}_j\;and\;{\beta}_j$ are proportional to the shear modulus and relaxation time, respectively. (4) We found that grain-boundary flow units only act in the deformation of Fe and Ti alloys whereas dislocation flow units do not show any appreciable contribution. (5) The deformations of Fe and Ti alloys belong generally to pattern A (Case 1) and B (Case 2), respectively. (6) By applying the equations, f=$(1/{\alpha}_{g1}) sinh^-1({\beta}_{g1}{\dot{s}}$) and $f=(X_{g1}/{\alpha}_{g1})sinh^{-1}({\beta}_{g1}{\dot{s}})+ (X_{g2}/{\alpha}_{g2})\;shih^{-1}({\beta}_{g2}{\dot{s}})$ to the flow data of Fe and Ti alloys, the parametric values of $x_{gj}/{\alpha}_{gj}\;and\;{\beta}_{gs}(j=1\;or\;2)$ were determined, here the subscript g signifies a grain-boundary flow unit. (7) From the values of ($({\beta}_gj)^{-1}$) at different temperatures, the activation enthalpy ${\Delta}H_{gj}^{\neq}$ of deformation due to flow unit gj was determined, ($({\beta}_gj)^{-1}$) being proportional to , the jumping frequency (the rate constant) of flow unit gj. The ${\Delta}H_{gj}\;^{\neq}$ agreed very well with ${\Delta}H_{gj}\;^{\neq}$ (self-diff) of the element j whose diffusion in the sample is a critical step for the deformation as proposed by Kim-Ree's theory (Refer to Tables 3 and 4). (8) The fact, ${\Delta}H_{gj}\;^{\neq}={\Delta}H_{j}\;^{\neq}$ (self-diff), justifies the Kim-Ree theory and their method for determining activation enthalpies for deformation. (9) A linear relation between ${\beta}^{-1}$ and carbon content [C] in hot-rolled steel was observed, i.e., In ${\beta}^{-1}$ = -50.2 [C] - 40.3. This equation explains very well the experimental facts observed with regard to the deformation of hot-rolled steel..

• Reproductive and Developmental Biology
• /
• v.39 no.3
• /
• pp.59-67
• /
• 2015

Galactose-${\alpha}1,3$-galactose (${\alpha}1,3$-Gal) epitope is synthesized at a high concentration on the surface of pig cells by ${\alpha}1,3$-galactosyltransferase gene (GGTA1). The ${\alpha}1,3$-Gal is responsible for hyperacute rejection in pig-to-human xenotransplantation. The generation of transgenic pigs as organ donors for humans is necessary to eliminate the GGTA1 gene that synthesize $Gal{\alpha}$(1,3)Gal. To prevent hyperacute graft rejection in pig-to-human xenotransplantation, previously, we developed ${\alpha}1,3$-galactosyltransferase gene-knock-out somatic cell by homologous recombination. In this study, we established cell lines of ${\alpha}1,3$-GT knock-out expressing hDAF and hHT gene from minipig fibroblasts to apply somatic cell nuclear transfer. The hDAF and hHT mRNA were expressed in the knock-in somatic cells and ${\alpha}1,3$-GT mRNA was suppressed. However, the knock-in somatic cells were increased resistance to human serum-mediated cytolysis.

• Entomological Research
• /
• v.48 no.5
• /
• pp.390-399
• /
• 2018

In order to precisely assess gene expression levels, the suitable internal reference genes must be served to quantify real-time reverse transcription polymerase chain reaction (RT-qPCR) data. For armyworm, Mythimna separata, which reference genes are suitable for assessing the level of transcriptional expression of target genes have yet to be explored. In this study, eight common reference genes, including ${\beta}$-actin (${\beta}$-ACT), 18 s ribosomal (18S), 28S ribosomal (28S), glyceraldehyde-3-phosphate (GAPDH), elongation fator-alpha ($EF1{\alpha}$), TATA box binding protein (TBP), ribosomal protein L7 (RPL7), and alpha-tubulin (${\alpha}$-TUB) that in different developmental stages, tissues and insecticide treatments of M. separata were evaluated. To further explore whether these genes were suitable to serve as endogenous controls, three software-based approaches (geNorm, BestKeeper, and NormFinder), the delta Ct method, and one web-based comprehensive tool (RefFinder) were employed to analyze and rank the tested genes. The optimal number of reference genes was determined using the geNorm program, and the suitability of particular reference genes was empirically validated according to normalized HSP70, and MsepCYP321A10 gene expression data. We found that the most suitable reference genes for the different experimental conditions. For developmental stages, 28S/RPL7 were the optimal reference genes, both $RPL7/EF1{\alpha}$ were suitable for experiments of different tissues, whereas for insecticide treatments, $28S/{\alpha}-TUB$ were suitable for normalizations of expression data. In addition, $28S/{\alpha}-TUB$ were the suitable reference genes because they have the most stable expression among different developmental stages, tissues and insecticide treatments. Our work is the first report on reference gene selection in M. separata, and might serve as a precedent for future gene expression studies.

• Molecules and Cells
• /
• v.27 no.4
• /
• pp.493-496
• /
• 2009

Hypoxia-inducible factor $1{\alpha}$ ($HIF1{\alpha}$) is a transcription factor that plays a key role in the adaptation of cells to low oxygen stress and oxygen homeostasis. The oxygen-dependent degradation (ODD) domain of $HIF1{\alpha}$ responsible for the negative regulation of $HIF1{\alpha}$ in normoxia is intrinsically unfolded. Here, we carried out the backbone $^1H$, $^{15}N$, and $^{13}C$ resonance assignment of a proteolysis-resistant fragment (residues 404-477) in the $HIF1{\alpha}$ ODD domain using NMR spectroscopy. About 98% (344/352) of all the $^1HN$, $^{15}N$, $^{13}C{\alpha}$, $^{13}C{\beta}$, and $^{13}CO$ resonances were unambiguously assigned. The results will be useful for further investigation of the structural and dynamic states of the $HIF1{\alpha}$ ODD domain and its interaction with binding partners.

• Journal of Oriental Neuropsychiatry
• /
• v.19 no.2
• /
• pp.77-93
• /
• 2008

Objective : This experiment was designed to investigate the effect of the CBD hot water extract & ultra-fine Powder on Alzheimer's Disease Model Induced by ${\beta}A$. Method : The effects of the CBD hot water extract on expression of interleukin-1 beta($IL-1{\beta}$), $TNF-{\alpha}$ mRNA and production of IL-6, $TNF-{\alpha}$ in BV2 microglial cell line treated by lipopolysacchaide(LPS). The effects of the CBD hot water extract & ultra-fine powder on (1) the behavior (2) expression of $IL-1{\beta}$, tumor necrosis factor-alpha($TNF-{\alpha}$), (3) the infarction area of the hippocampus in Alzheimer's diseased mice induced with ${\beta}A$ were investigated. Result : The CBD hot water extract suppressed the expression of $IL-1{\beta}$, $TNF-{\alpha}$ mRNA in BV2 microglia cell line treated with LPS. The CBD hot water extract significantly suppressed the production of $IL-1{\beta}$, $TNF-{\alpha}$ in BV2 microglial cell line treated with LPS. The CBD hot water extract & ultra-fine powder a significant inhibitory effect on the memory deficit was shown for the mice with Alzheimer's disease induced by ${\beta}A$ in the Morris water maze experiment, which measured step-through latency and distance movement-through latency. The CBD hot water extract & ultra-fine powder significantly suppressed the expression of $IL-l{\beta}$ and $TNF-{\alpha}$ protein in the microglial cell of mice with Alzheimer's disease induced by ${\beta}A$. The CBD hot water extract & ultra-fine powder suppressed the over-expression of AChE activity in the serum of the mice with Alzheimer's disease induced by ${\beta}A$. The CBD hot water extract & ultra-fine powder reduced infarction area of hippocampus, in the mice with Alzheimer's disease induced by ${\beta}A$. Conclusions : These results suggest that the CBD hot water extract & ultra-fine powder may be effective for the prevention and treatment of Alzheimer's disease. Investigation into the clinical use of the CBD hot water extract & ultra-fine powder for Alzheimer's disease is suggested for future research.