• 제목/요약/키워드: K2

검색결과 337,364건 처리시간 0.165초

Synthesis, Cytotoxicity and Antitumor Activity of 2,3-Diarylcyclopent-2-ene-1-ones

  • Nam, Nguyen-Hai;Kim, Yong;You, Young-Jae;Hong, Dong-Ho;Kim, Hwan-Mook;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제25권5호
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    • pp.600-607
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    • 2002
  • Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a∼2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a∼3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

A Novel 3D Polypseudo-rotaxane Metal-organic Framework Based on a Flexible Bis-pyridyl-bis-amide Ligand

  • Wang, Xiu-Li;Han, Na;Lin, Hong-Yan;Xu, Chuang;Luan, Jian;Liu, Guo-Cheng
    • Bulletin of the Korean Chemical Society
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    • 제33권11호
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    • pp.3793-3796
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    • 2012
  • A novel 3D compound $\{[Cu(L)(H_2O)_4][Cu_2(SIP)_2(L)_2]\}{\cdot}2H_2O$ (1) (L = N,N-bis(4-pyridinecarboxamide)-1,4-butane, SIP = 5-sulfoisophthalate) is hydrothermally synthesized. X-ray diffraction analysis reveals that compound 1 is composed of 2D anionic $[Cu_2(SIP)_2(L)_2]_n{^{2n-}}$ double-layers and discrete 1D cationic $[CuL(H_2O)_4]_n{^{2n+}}$ polymeric chains, which represents a rare 3D polypseudo-rotaxane MOF from intercalation of 1D and 2D framework. In addition, the luminescent property and electrochemical behavior of compound 1 have been investigated.

Acute Effects of 2-Bromopropane and 1,2-Dibromopropane on Hepatotoxic and Immunotoxic Parameters in Female BALB/c Mice

  • Kim, Nam-Hee;Hyun, Sun-Hee;Jin, Chun-Hua;Lee, Sang-Kyu;Lee, Dong-Wook;Jean, Tae-Won;Park, Chang-Bon;Lee, Eung-Seok;Chae, Whigun;Jeong, Tae-Cheon
    • Archives of Pharmacal Research
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    • 제26권11호
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    • pp.943-950
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    • 2003
  • In the present studies, the acute toxic effects of 2-bromopropane (2-BP) and its analog, 1,2-dibromopropane (1,2-DBP), were investigated in female BALB/c mice. The mice were treated orally with either 2-BP at 2000 and 4000 mg/kg or 1,2-DBP at 300 and 600 mg/kg. Four days before necropsy, the mice were immunized intraperitoneally with sheep red blood cells (SRBCs). 1,2-DBP reduced the weights of the spleen and thymus weights and decreased the number of splenic cells. In addition, treatment with 1,2-DBP suppressed the antibody response to SRBCs. Meanwhile, only the antibody response was significantly suppressed by treatment with 2-BP. In the subsequent studies, the time course effects of 2-BP and 1 ,2-DBP on the hepatotoxic parameters were compared in female BALB/c mice. When mice were treated orally with either one of these chemicals for 6, 12, 24 and 48 h, the activities of serum alanine aminotransferase and aspartate aminotransferase elevated significantly only with 1,2-DBP 24 h after the treatment. The hepatic content of glutathione was reduced by 1,2-DBP. Meanwhile, these parameters were increased by 2-BP. The present results suggest that 1,2-DBP in the Solvent 5200 also contributes to the immnunotoxicity, although 2-BP is a major component.

The Role of the Hydrophobic Group on Ring A of Chalcones in the Inhibition of Interleukin-5

  • Yang, Hyun-Mo;Shin, Hye-Rim;Cho, Soo-Hyun;Song, Gyu-Yong;Lee, In-Jeong;Kim, Mi-Kyeong;Lee, Seung-Ho;Ryu, Jae-Chun;Kim, Young-Soo;Jung, Sang-Hun
    • Archives of Pharmacal Research
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    • 제29권11호
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    • pp.969-976
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    • 2006
  • Novel chalcones were found as potent inhibitors of interleukin-5 (II-5). 1-(6-Benzyloxy-2-hydroxyphenyl)-3-(4-hydroxyphenyl)propenone (2a, 78.8% inhibition at $50\;{\mu}M,\;IC_{50}=25.3\;{\mu}M$) was initially identified as a potent inhibitor of IL-5. This activity is comparable to that of budesonide or sophoricoside (1a). The benzyloxy group appears to be critical for the enhancement of the IL-5 inhibitory activity. To identify the role of this hydrophobic moiety, cyclohexyloxy (2d), cyclohexylmethoxy (2c), cyclohexylethoxy (2e), cyclohexylpropoxy (2f), 2-methylpropoxy (2g), 3-methylbutoxy (2h), 4-methylpentoxy (2i), and 2-ethylbutoxy (2j) analogs were prepared and tested for their effects on IL-5 bioactivity. Compounds 2c ($IC_{50}=12.6\;{\mu}M$), 2d ($IC_{50}=12.2\;{\mu}M$), and 2i ($IC_{50}=12.3\;{\mu}M$) exhibited the most potent activity. Considering the cLog P values of 2, the alkoxy group contributes to the cell permeability of 2 for the enhancement of activity, rather than playing a role in ligand motif binding to the receptor. The optimum alkoxy group in ring A of 2 should be one that provides the cLog P of 2 in the range of 4.22 to 4.67.

Synthesis and Characterization of the Large Single Crystal of Fully K+-exchanged Zeolite X (FAU), |K80|[Si112Al80O384]-FAU (Si/Al=1.41)

  • Lim, Woo-Taik;Jeong, Gyo-Cheol;Park, Chang-Kun;Park, Jong-Sam;Kim, Young-Hun
    • Bulletin of the Korean Chemical Society
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    • 제28권1호
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    • pp.41-48
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    • 2007
  • Large colorless single crystals of sodium zeolite X, stoichiometry |Na80 |[Si112Al80O384]-FAU, with diameters up to 200 μm and Si/Al = 1.41 have been synthesized from gels with the composition of 2.40SiO2 : 2.00NaAlO2 : 7.52NaOH : 454H2O : 5.00TEA. One of these, a colorless octahedron about 200 μm in cross-section has been treated with aqueous 0.1 M KNO3 for the preparation of K+-exchanged zeolite X. The crystal structure of |K80|[Si112Al80O384]-FAU per unit cell, a = 24.838(4) A, dehydrated at 673 K and 1 × 10-6 Torr, has been determined by single-crystal X-ray diffraction techniques in the cubic space group Fd at 294 K. The structure was refined using all intensities to the final error indices (using only the 707 reflections for which Fo > 4σ (Fo)) R1 = 0.075 (based on F) and R2 = 0.236 (based on F2). About 80 K+ ions per unit cell are found at an unusually large number of crystallographically distinct positions, eight. Eleven K+ ions are at the centers of double 6-rings (D6Rs, site I; K-O = 2.492(6) A and O-K-O (octahedral) = 88.45(22)o and 91.55(22)o). Site-I' position (in the sodalite cavities opposite D6Rs) is occupied by five K+ ions per unit cell; these K+ ions are recessed 1.92 A into the sodalite cavities from their 3-oxygen planes (K-O = 2.820(19) A, and O-K-O = 78.6(6)o). Twety-three K+ ions are found at three nonequivalent site II (in the supercage) with occupancies of 5, 9, and 9 ions; these K+ ions are recessed 0.43 A, 0.75 A, and 1.55 A, respectively, into the supercage from the three oxygens to which it is bound (K-O = 2.36(13) A, 2.45(13) A, and 2.710(13) A, O-K-O = 116.5(20)o, 110.1(17)o, and 90.4(6)o, respectively). The remaining sixteen, thirteen, and twelve K+ ions occupy three sites III' near triple 4-rings in the supercage (K-O = 2.64(3) A, 2.94(3) A, 2.73(5) A, 2.96(6) A, 3.06(4) A, and 3.08(3) A).

구조유도물질 18-crown-6 ether를 이용한 순수한 RHO 제올라이트 수열합성과 작은 가스 흡착 거동 (Structure direct agent-assisted hydrothermal synthesis and small gases adsorption behavior of pure RHO zeolite)

  • 김범주;;한문희;조철희
    • 에너지공학
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    • 제23권4호
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    • pp.141-149
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    • 2014
  • 본 연구에서는 구조유도물질인 18-crown-6 ether를 이용하여 순수한 RHO 제올라이트 입자를 합성하고, $N_2$, $CO_2$, $H_2$, $O_2$ 등 작은 기체 흡착 거동을 고찰하였다. 순수한 RHO 제올라이트 입자는 세슘이온이 함유된 알루미노실리케이트 겔로부터 합성되었으며, 직경 100-200 nm 크기의 일차입자로 구성된 약 $1.2{\mu}m$ 크기의 정육면체 모양의 이차입자이었다. 합성된 RHO 제올라이트 입자는 $600^{\circ}C$에서 3시간 하소 공정에서도 구조적으로 안정하였으며 수증기 흡착 실험으로부터 비표면적이 483.32 m2/g이고 마이크로 기공직경이 약 $4{\AA}$임을 확인할 수 있었다. RHO 제올라이트에 대한 $N_2$, $CO_2$, $H_2$, $O_2$ 흡착은 50-500 kPa의 압력 범위에서 이루어졌으며, $N_2$, $H_2$, $O_2$에 비하여 $CO_2$에 강한 흡착거동을 보였다. 특히, $CO_2$ 흡착은 모든 압력에서 시간 의존적이었으며 이는 기존에 알려진 RHO 제올라이트의 구조 변화로 설명할 수 있었다. 일정 압력에서 약 3시간 동안 유지하여 측정된 $CO_2$ 흡착량은 50 kPa과 500 kPa에서 각각 1.283 mmol/g과 3.357 mmol/g이었고, 500 kPa에서의 $CO_2/H_2$ 흡착 선택도는 15.77 이었다. 기존 가스 흡착제의 흡착 성능과 비교한 결과, 합성된 RHO 제올라이트는 $CO_2/H_2$ 분리에 유용할 것으로 판단되었다.

FGF-2 inhibits TNF-α mediated apoptosis through up-regulation of Bcl2-A1 and Bcl-xL in ATDC5 cells

  • Kim, Hey-Ryun;Heo, Youn-Moo;Jeong, Kyoung-Il;Kim, Yong-Min;Jang, Hae-Lan;Lee, Kwang-Yeol;Yeo, Chang-Yeol;Kim, Sung-Hoon;Lee, Hak-Kyo;Kim, Seung-Ryul;Kim, Eung-Gook;Choi, Joong-Kook
    • BMB Reports
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    • 제45권5호
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    • pp.287-292
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    • 2012
  • FGF-2 is involved in cell survival, proliferation, apoptosis, and angiogenesis in a wide variety of cells. FRGRs, PI3K and MAP kinases are well known mediators of FGF signaling. Despite its known roles during many developmental processes, including osteogenesis, there are few known targets of FGF-2. In the present study, we identified Bcl2-A1 and Bcl-xL as two prominent targets involved in promoting cell survival. Pretreatment of ATDC5 cells with FGF-2 increased cell survival, while siRNAs specific for Bcl2-A1 and Bcl-xL compromised the anti-apoptotic effect of FGF-2, sensitized the cells to apoptosis triggered by TNF-${\alpha}$. Chemical inhibition of FGFR, NFkB, and PI3K activity by PD173074, pyrrolidine dithiocarbamate, and LY294002 respectively abrogated the FGF-2-mediated induction of Bcl2-A1 and Bcl-xL expression. Taken together, our data demonstrate that a subset of Bcl2 family proteins are the targets of FGF-2 signaling that promotes the survival of ATDC5 cells.

Hydrogen Absorption at a Low Temperature by MgH2 after Reactive Mechanical Grinding

  • Song, Myoung Youp;Lee, Seong Ho;Kwak, Young Jun;Park, Hye Ryoung
    • 한국재료학회지
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    • 제24권3호
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    • pp.129-134
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    • 2014
  • Pure $MgH_2$ was milled under a hydrogen atmosphere (reactive mechanical grinding, RMG). The hydrogen storage properties of the prepared samples were studied at a relatively low temperature of 423 K and were compared with those of pure Mg. The hydriding rate of the Mg was extremely low (0.0008 wt% H/min at n = 4), and the $MgH_2$ after RMG had higher hydriding rates than that of Mg at 423 K under 12 bar $H_2$. The initial hydriding rate of $MgH_2$ after RMG at 423 K under 12 bar $H_2$ was the highest (0.08 wt% H/min) at n = 2. At n = 2, the $MgH_2$ after RMG absorbed 0.39 wt% H for 5 min, and 1.21 wt% H for 60 min at 423K under 12 bar $H_2$. At 573 K under 12 bar $H_2$, the $MgH_2$ after RMG absorbed 4.86 wt% H for 5 min, and 5.52 wt% H for 60 min at n = 2. At 573 K and 423 K under 1.0 bar $H_2$, the $MgH_2$ after RMG and the Mg did not release hydrogen. The decrease in particle size and creation of defects by reactive mechanical grinding are believed to have led to the increase in the hydriding rate of the $MgH_2$ after RMG at a relatively low temperature of 423 K.

Inhibition of Pacemaker Activity of Interstitial Cells of Cajal by Hydrogen Peroxide via Activating ATP-sensitive $K^+$ Channels

  • Choi Seok;Parajuli Shankar Prasad;Cheong Hyeon-Sook;Paudyal Dilli Parasad;Yeum Cheol-Ho;Yoon Pyung-Jin;Jun Jae-Yeoul
    • The Korean Journal of Physiology and Pharmacology
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    • 제11권1호
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    • pp.15-20
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    • 2007
  • To investigate whether hydrogen peroxide($H_2O_2$) affects intestinal motility, pacemaker currents and membrane potential were recorded in cultured interstitial cells of Cajal(ICC) from murine small intestine by using a whole-cell patch clamp. In whole cell patch technique at $30^{\circ}C$, ICC generated spontaneous pacemaker potential under current clamp mode(I=0) and inward currents(pacemaker currents) under voltage clamp mode at a holding potential of -70 mV. When ICC were treated with $H_2O_2$ in ICC, $H_2O_2$ hyperpolarized the membrane potential under currents clamp mode and decreased both the frequency and amplitude of pacemaker currents and increased the resting currents in outward direction under voltage clamp mode. Also, $H_2O_2$ inhibited the pacemaker currents in a dose-dependent manner. Because the properties of $H_2O_2$ action on pacemaker currents were same as the effects of pinacidil(ATP-sensitive $K^+$ channels opener), we tested the effects of glibenclamide(ATP-sensitive $K^+$ channels blocker) on $H_2O_2$ action in ICC, and found that the effects of $H_2O_2$ on pacemaker currents were blocked by co- or pre- treatment of glibenclamide. These results suggest that $H_2O_2$ inhibits pacemaker currents of ICC by activating ATP-sensitive $K^+$ channels.

$Li^{+}$ 이온 주입된 $Al_2O_3$의 결함 특성 (Defect center of $Li^{+}$ ion implanted $Al_2O_3$)

  • Kim, Tae-Kyu
    • 한국의학물리학회지:의학물리
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    • 제5권2호
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    • pp.13-20
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    • 1994
  • 본 연구에서는 감마선 조사, 전자선 조사방법에 의한 전자만의 주업 및 이온 주업 후 전자선조사 방법으로 전자들이 주입된 $\alpha$-$Al_2O_3$의 열자극 발광(Thermoluminescence : TL)에 관련된 결함 형태를 조사하였다. 감마선 조사된 $\alpha$-$Al_2O_3$의 열자극 발광 곡선은 380K, 415K, 440K, 460K 및 475K에서 TL peak가 나타났다. 광흡수 스펙트럼과 자외선 photobleaching 결과로부터 감마선 조사된 $\alpha$-$Al_2O_3$의 380K와 475K TL peak는 F center에, 415K TL peak는 $F^{+}$ center에 기인함을 알았다. 전자선 조사방법에 의하여 전자 주입된 $\alpha$-$Al_2O_3$의 열자극 발광 곡선은 380K, 415K, 440K 및 460K TL peak를 가졌고, $Li^{+}$ 이온 주입 후 전자선 조사방법으로 전자들이 주입된 $\alpha$-$Al_2O_3$는 440K에서 TL peak가 나타났다. 전자선 조사방법에 의한 전자만의 주입과 $Li^{+}$ 이온 주입 후 전자선 조사방법으로 전자들이 주입된 $\alpha$-$Al_2O_3$의 열자극 발광 특성은 380K TL peak는 F center에, 440K TL peak는 $F^{+}$ center에 기인함을 보였다.

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