• Archives of Pharmacal Research
• /
• v.23 no.3
• /
• pp.202-205
• /
• 2000

A convenient pathway for synthesis of trans-metanicotine analogues was developed. trans-Metanicotine, a subtype(${\alpha}4{\beta}2$)-selective ligand for neuronal nicotinic acetylcholine receptor, is under clinical phase for Alzheimer's disease. Zn-mediated allylation of allyl bromide and acetaldehyde followed by Heck reaction with 3-bromopyridine gave 5-pyridin-3-yl-pent-4-en-3-ol (2). Tosylation of 5-pyridin-3-yl-pent-4-en-3-ol followed by substitution reaction with methylamine in sealed tube gave methyl-(1-methyl-4-pyridin-3-yl-but-3-enyl)-amine (4) in good yields. Thus, trans-metanicotine analogues modified at the $\alpha$-position of the methylamino group with various functional groups can be obtained in 4 steps.

• Geomechanics and Engineering
• /
• v.19 no.4
• /
• pp.295-305
• /
• 2019

The present paper is concerned with the investigation of disturbances in orthotropic thermoelastic medium by using fractional order heat conduction equation with three phase lags due to thermomechanical sources. Laplace and Fourier transform techniques are used to solve the problem. The expressions for displacement components, stress components and temperature change are derived in transformed domain and further in physical domain using numerical inversion techniques. The effect of fractional parameter based on its conductivity i.e., ($0<{\alpha}<1$ for weak, ${\alpha}=1$ for normal, $1<{\alpha}{\leq}2$ for strong conductivity) is depicted graphically on various components.

• The Korean Journal of Food And Nutrition
• /
• v.23 no.4
• /
• pp.556-561
• /
• 2010

Tomato fruits(Lycoperisicon esculentum) synthesize the glycoalkaloids dehydrotomatine and ${\alpha}$-tomatine, possibly as defense against bacteria, fungi and insects. We developed a new effective method to prepare and purify dehydrotomatine and ${\alpha}$-tomatine that exists in tomato fruits using alumina column chromatography and high performance liquid chromatography (HPLC). The tomato glycoalkaloids(TGA) in tomato was extracted with 2% acetic acid, and then precipitated with ammonium hydroxide(pH=10.5). The dry precipitate substance was applied on alumina column, and then fractionated with water saturated n-butylalcohol. The TGA(Fr. No. 26~36) were collected and dried under reduced pressure. The TGA was performed on a reverse phase HPLC(Inertsil ODS-2, $5\;{\mu}m$), eluted with acetonitrile/20mM $KH_2PO_4$(24:76, v/v) at 208 nm. Two peaks were detected on HPLC, and individual peak was collected by repeating HPLC. Furthermore, to confirm the identity dehydrotomatine and ${\alpha}$-tomatine, each peak isolated was hydrolyzed with 1N HCl into sugar and aglycone tomatidine. The sugars were converted to trimethylsilyl ester derivatives. The nature and molar ratios of sugars were identified by gas-liquid chromatography(GLC) and the aglycone by high-performance liquid chromatography(HPLC). The first peak (Rt=17.5 min) eluted from HPLC was identified as dehydrotomatine, and second peak(Rt=21.0 min) was as ${\alpha}$-tomatine. This technique has been used effectively to prepare and isolate dehydrotomatine and ${\alpha}$-tomatine from tomato fruits.

• BMB Reports
• /
• v.39 no.3
• /
• pp.270-277
• /
• 2006

Helices 4 and 5 of the Bacillus thuringiensis Cry4Ba $\delta$-endotoxin have been shown to be important determinants for mosquito-larvicidal activity, likely being involved in membrane-pore formation. In this study, the Cry4Ba mutant protein containing an additional engineered tryptic cleavage site was used to produce the $\alpha4$-$\alpha5$ hairpin peptide by an efficient alternative strategy. Upon solubilization of toxin inclusions expressed in Escherichia coli and subsequent digestion with trypsin, the 130-kDa mutant protoxin was processed to protease-resistant fragments of ca. 47, 10 and 7 kDa. The 7-kDa fragment was identified as the $\alpha4$-loop-$\alpha5$ hairpin via N-terminal sequencing and mass spectrometry, and was successfully purified by size-exclusion FPLC and reversed-phase HPLC. Using circular dichroism spectroscopy, the 7-kDa peptide was found to exist predominantly as an $\alpha$-helical structure. Membrane perturbation studies by using fluorimetric calcein-release assays revealed that the 7-kDa helical hairpin is highly active against unilamellar liposomes compared with the 65-kDa activated full-length toxin. These results directly support the role of the $\alpha4$-loop-$\alpha5$ hairpin in membrane perturbation and pore formation of the full-length Cry4Ba toxin.

• Korean Journal of Materials Research
• /
• v.14 no.3
• /
• pp.218-223
• /
• 2004

P-type $\beta$-FeSi$_2$ with a nominal composition of $Fe_{0.92}Mn_{0.08}Si_2$ powders has been produced by mechanical alloying process. As-milled powders were spray dried and consolidated by atmospheric plasma thermal spraying as a rapid sintering process. As-milled powders were of metastable state and fully transformed to $\beta$-$FeSi_2$ phase by subsequent isothermal annealing. However, as-thermal sprayed $Fe_{0.92}Mn_{0.08}Si_2$ consisted of untransformed mixture of $\alpha$-$Fe_2Si_{5}$ and $\varepsilon$-FeSi phases. Isothermal annealing has been carried out to induce transformation to the thermoelectric semiconducting $\beta$-$FeSi_2$ phase. Isothermal annealing at $845^{\circ}C$ in vacuum gradually led to the thermoelectric semiconducting $\beta$-$FeSi_2$ phase transformation, but some residual metallic $\alpha$ and $\varepsilon$ phases were unavoidable even after prolonged annealing. Thermoelectric properties of $\beta$-$FeSi_2$ materials before and after isothermal annealing were evaluated. Seebeck coefficient increased and electric conductivity decreased with increasing annealing time due to the phase transition from metallic phases to semiconducting phases. Thermoelectric properties showed gradual increment, but overall properties appeared to be inferior to those of vacuum hot pressed specimens.

• Proceedings of the KIEE Conference
• /
• 2004.07c
• /
• pp.1588-1590
• /
• 2004

The composites were fabricated, respectively, using 61vol.% SiC - 39vol.% $TiB_2$ and using 61vol.% SiC 39vol.% WC powders with the liquid forming additives of 12wt% $Al_2O_3+Y_2O_3$ by pressureless annealing at 1800$^{\circ}C$ for 4 hours. Reactions between SiC and transition metal $TiB_2$, WC were not observed in this microstructure. The result of phase analysis of composites by XRD revealed SiC(6H), $TiB_2$ and YAG($Al_5Y_3O_{12}$) crystal phase on the SiC-$TiB_2$, and SiC(2H), WC and YAG($Al_5Y_3O_{12}$) crystal phase on the SiC-WC composites. ${\beta}{\rightarrow}{\alpha}$-SiC phase transformation was ocurred on the SiC-$TiB_2$, but ${\alpha}{\rightarrow}{\beta}$-SiC reverse transformation was not occurred on the SiC-WC composites. The relative density, the flexural strength showed respectively value of 96.2%, 310.19Mpa in SiC-WC composites. The electrical resistivity of the SiC-$TiB_2$ and the SiC-WC composites is all positive temperature cofficient resistance(PTCR) in the temperature ranges from 25$^{\circ}C$ to 500$^{\circ}C$.

• Advanced Composite Materials
• /
• v.18 no.4
• /
• pp.351-364
• /
• 2009

The thermal stability and elevated temperature mechanical properties of $SiC_P$/Al-11.7Fe-1.3V-1.7Si (Al-11.7Fe-1.3V-1.7Si reinforced with SiC particulates) composites sheets prepared by spray deposition (SD) $\rightarrow$ hot pressing $\rightarrow$ rolling process were investigated. The experimental results showed that the composite possessed high ${\sigma}_b$ (elevated temperature tensile strength), for instance, ${\sigma}_b$ was 315.8 MPa, which was tested at $315^{\circ}C$, meanwhile the figure was 232.6 MPa tested at $400^{\circ}C$, and the elongations were 2.5% and 1.4%, respectively. Furthermore, the composite sheets exhibited excellent thermal stability: the hardness showed no significant decline after annealing at $550^{\circ}C$ for 200 h or at $600^{\circ}C$ for 10 h. The good elevated temperature mechanical properties and excellent thermal stability should mainly be attributed to the formation of spherical ${\alpha}-Al_{12}(Fe,\;V)_3Si$ dispersed phase particulates in the aluminum matrix. Furthermore, the addition of SiC particles into the alloy is another important factor, which the following properties are responsible for. The resultant Si of the reaction between Al matrix and SiC particles diffused into Al matrix can stabilize ${\alpha}-Al_{12}(Fe,\;V)_3Si$ dispersed phase; in addition, the interface (Si layer) improved the wettability of Al/$SiC_P$, hence, elevated the bonding between them. Furthermore, the fine $Al_4C_3$ phase also strengthened the matrix as a dispersion-strengthened phase. Meanwhile, load is transferred from Al matrix to SiC particles, which increased the cooling rate of the melt droplets and improved the solution strengthening and dispersion strengthening.

• Journal of the Korean Electrochemical Society
• /
• v.3 no.2
• /
• pp.72-75
• /
• 2000

For the purpose of developing the non-stoichiometric Zr-based Laves phase alloy with higher capacity and better performance for electrochemical application, extensive work has been carried out in KAIST. After careful alloy design of $ZrMn_2-based$ hydrogen storage alloys through varing their stoichiometry while susbstituting or adding some alloying elements, the $Zr-Ti-(Lh-V-Ni)_{2.2},\;Zr-Ti-(Mn-V-Cr-Ni)_{1.8\pm0.1}$ with high capacity and better performance was developed. Consequently the $Zr-Ti-(Mn-V-Ni)_{2.2}$ alloy has a high discharge capacity of 394mAh/g and shows a high rate capability equaling to that of commercialized $AB_5$ type alloys. On the other hand, in order to develop the hydrogen storage alloy with higher discharge capacity, the hypo-stoichiometric $Zr(Mn-V-Ni)_{2-\alpha}$ alloys substituted by Ti are under developing. As the result of competitive roles of Ti and $stocihiometry({\alpha})$, the discharge capacity of $Zr-Ti-(Mn-V-Cr-Ni)_{l.8\pm0.1}$ alloys is about 400mAh/g(410 mAh/g, which shows the highest level of performance in the Zr-based alloy developed. Our sequential endeavor is improving the shortcoming of Zr-based Laves phase alloy for commercialization, i.e., poor activation property and low rate capability, etc. It is therefore believed that the commercialization of Zr-based Laves phase hydrogen storage alloy for Ni-MH rechargeable battery is in near future.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1996.04a
• /
• pp.243-243
• /
• 1996

백금착물 항암제 후보물질로서 합성된 KBP31705-Cl27, KBP30603-901을 기존 화합물인 cisplatin 및 carboplatin과 pharmacokinetic profile을 비교 검토하였다. 웅성 Sprague-Dawley rat을 sodium pentobarbital 마취하에서 방광 및 대퇴동맥과 정맥에 polyethylene tubing을 사용하여 catheterization시켰다. Urine 배출이 안정화되었을 때 대퇴정맥내로 cisplatin과 KBP31705-Cl27은 2 mg/kg, carboplatin과 KBP 30603-901은 20mg/kg 용량으로 주사한 후 2, 4, 6, 8, 10, 15, 20, 30, 45, 60, 120 분에 대퇴동맥으로부터 혈액을 채취하였으며 urine은 약물투여 후 1시간 간격으로 4시간동안 채취하였다. Plasma와 urine중의 platinum농도는 inductively coupled plasma-mass spectrometer를 사용하여 측정하였고, pharmacokinetic parameters는 non-linear least square computer Program인 PCNONLIN을 이용하여 산출되었다. 혈중 platinum농도와 시간의 관계에서 KBP31705-Cl27은 cisplatin과 비교하여 alpha-phase에서 혈중 농도는 낮지만 비슷한 양상을 나타내었고, beta-phase에서는 비교적 느리게 소실됨을 보였다. Urine으로 4시간동안 배출된 platinum양은 각각 투여량의 52, 56%로서 두 약물에서 비슷하였다. 또한 KBP30603-901은 carboplatin과 비교하여 alpha-phase는 거의 비슷한 패턴을 나타내었으나, beta-phase는 훨씬 느리게 감소하여 반감기가 길다는 것을 보여 주었으며 또한 이것은 urine으로 4시간동안 배출된 platinum양이 KBP30603-901의 경우 투여량의 46%로서 carboplatin의 59%보다 적게 배출된다는 data와도 일관됨을 보여주었다. 이상의 결과로 볼 때 KBP30603-901이 다른 백금착물 항암제보다 체내에 머무르는 시간이 길어 혈중에서 보다 오랜 시간동안 머물러 높은 유효농도를 유지할 수 있을 것으로 사료된다.

• Journal of Powder Materials
• /
• v.12 no.6 s.53
• /
• pp.422-427
• /
• 2005

The $Al_2O_3$ with various phases were prepared by simple ex-situ hydrolysis and spark plasma sintering (SPS) process of Al powder. The nano bayerite $(\beta-Al(OH)_3)$ phase was derived by hydrolysis of commercial powder of Al with micrometer size, whereas the bohemite (AlO(OH)) phase was obtained by hydrolysis of nano Al powder synthesized by pulsed wire evaporation (PWE) method. Compaction as well as dehydration of both nano bayerite and bohemite was carried out simultaneously by SPS method, which is used to fabricate dense powder compacts with a rapid heating rate of $100^{\circ}C$ per min. under the pressure of 50MPa. After compaction treatment in the temperature ranges from $100^{\circ}C\;to\; 1100^{\circ}C$, the bayerite and bohemite phases change into various alumina phases depending on the compaction temperatures. The bayerite shows phase transition of $Al(OH)_3{\to}{\eta}-Al_2O_3{\to}{\theta}-Al_2O_3{\to}\alpha-Al_2O_3$ sequences. On the other hand, the bohemite experiences the phase transition from AlO(OH) to ${\gamma}-Al_2O_3\;at\;350^{\circ}C.$ It shows AlO(OH) ${\gamma}-Al_2O_3{\to}{\delta}-Al_2O_3{\to}{\alpha}-Al_2O_3$ sequences. The ${\gamma}-Al_2O_3$ compacted at $550^{\circ}C$ shows a high surface area $(138m^2/g)$.