• Title/Summary/Keyword: Activity Generation

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Studies on the Biological Activities of the Constituents of Ailanthi Cortex Radicis III - Antitumor activities of dichloromethane fration - (저근백피성분의 생리활성에 관한 연구(III) - 디클로드메탄분획의 항암작용 -)

  • Kim, Jong;Lee, Chung-Kyu
    • Korean Journal of Pharmacognosy
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    • v.28 no.1
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    • pp.54-58
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    • 1997
  • The cytotoxic activities of methanolic extract and its fractions of Ailanthi Cortex Radicis and column chromatographic eluates of its dichloromethane fraction (DCM fr.) were investigated. DCM fr. Showed the strongest cytotoxicity against hepatoma cells. Furthermore, the active equates 1-3, 8 and 9 were obtained. Effects on free radical generation and the growth of vascular endothelial cells were tested to elucidate the action mechanism of anticancer activity. Eluates 1-3 stimulated free radical generation, while eluates 8 and 9 showed no changes. Especially, eluates 8 and 9 efffectively inhibited the proliferation of vascular endothelial cells in a dose- dependant manner. It is speculated that the anticancer effects of eluates 1-3, 8 and 9 might be due to free radical generation and inhibition of endothelial cell growth, respectively.

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Antioxidant Effect of Salvia miltiorrhiza

  • Kang, Hye-Sook;Chung, Hae-Young;Jung, Jee-Hyung;Kang, Sam-Sik;Choi, Jae-Sue
    • Archives of Pharmacal Research
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    • v.20 no.5
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    • pp.496-500
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    • 1997
  • A strong antioxidant activity, which was measured by the radical scavenging effect on 1, 1-diphenyl-2-picrylhydrazyl(DPPH) radical, was detected in the methanol extract of Salvia miltiorrhiza Bunge (Labiatae). By activity-directed fractionation, compounds 1 and 2 were isolated as antioxidant principles of S. miltiorrhiza. Compounds 1 and 2 were identified as dimethyl lithospermate and 3-(3, 4-dihydroxyphenyl)lactamide, respectively, on the basis of spectral data. The radical scavenging effect of compounds 1 and 2 on DPPH radical exceeded that of L-ascorbic acid which is a well known antioxidant. These two compounds also showed prominent inhibitory activity against free radical generation in dichlorofluorescein (DCF) method and cytoprotective effect against t-BHP in cultured liver cell.

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A Study on Antimicrobial Activity of N-(fluorodichlomethylthio) Phthalimide-Ag Complex of Reclaimed Rubber Mat (리사이클 고무 매트의 N-(fluorodichlomethylthio) Phthalimide-Ag Complex에 관한 항미생물 활성 연구)

  • Kim, Ki-Jun;Lee, Joo-Youb;Park, Tae-Sul
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.4
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    • pp.491-496
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    • 2011
  • N-(fluorodichlomethylthio) phthalimide-silver complexes were prepared and investigated the antimicrobial activity on rubber mat manufactured with waste rubber. We are exposed to harmful bacteria and fungi all the time. We manufactured antimicrobial mat to be imposed to mats that it can prevent generation of bacteria and microorganisms, and restrict their reproduction. Infection of medical devices causes significant morbidity and mortality. For aim of this study, we measured the antimicrobial mat manufactured with N-(fluorodichlomethylthio) phthalimide-Ag complex by CCD, FT-IR and NMR. The effect of mole ratio of N-(fluorodichlomethylthio) phthalimide-Ag complex on antibacterial activity to bacteria and fungi is investigated. Reduction rate is evaluated using the Quinn method. Escherichia Coli is effectively inhibited than Staphylococcus aureus by antimicrobial mat.

A Brief Introduction to the Transduction of Neural Activity into Fos Signal

  • Chung, Leeyup
    • Development and Reproduction
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    • v.19 no.2
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    • pp.61-67
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    • 2015
  • The immediate early gene c-fos has long been known as a molecular marker of neural activity. The neuron's activity is transformed into intracellular calcium influx through NMDA receptors and L-type voltage sensitive calcium channels. For the transcription of c-fos, neural activity should be strong enough to activate mitogen-activated protein kinase (MAPK) signaling pathway which shows low calcium sensitivity. Upon translation, the auto-inhibition by Fos protein regulates basal Fos expression. The pattern of external stimuli and the valence of the stimulus to the animal change Fos signal, thus the signal reflects learning and memory aspects. Understanding the features of multiple components regulating Fos signaling is necessary for the optimal generation and interpretation of Fos signal.

Spontaneous Electrical Activity in Cerebellar Purkinje Neurons of Postnatal Rats

  • Nam, Sang-Chae
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.4
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    • pp.355-366
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    • 1997
  • Although cerebellar Purkinje cells display spontaneous electrical activity in vivo and in slice experiments, the mechanism of the spontaneous activity generation has not been clearly understood. The aim of this study was to investigate whether cerebellar Purkinje cells of postnatal rats generate spontaneous electrical activity without synaptic inputs. Dissociated cerebellar Purkinje cells were used for reducing synaptic inputs in the present study. Cerebellar Purkinje cells with dendrites were dissociated from postnatal rats using enzymatic treatment followed by mechanical trituration. Spontaneous electrical activities were recorded from dissociated cells without any stimulus using whole-cell patch clamp configuration. Two types, spontaneously firing or quiescent, of dissociated Purkinje cells were observed in postnatal rats. Both types of cells were identified as Purkinje cells using immunocytochemical staining technique with anti-calbindin after recording. Spontaneously active cells displayed two patterns of firing, repetitive and burst firings. Two thirds of dissociated Purkinje cells displayed repetitive firing and the rest of them did burst firing under same recording condition. Repetitive firing activities were maintained even after further isolation using either physical or pharmacological techniques. Neither high magnessium solution nor excitatory synaptic blockers, AP-5 and DNQX, block the spontaneous activity. These results demonstrate that spontaneous electrical activity of isolated cerebellar Purkinje cells in postnatal rats is generated by intrinsic membrane properties rather than synaptic inputs.

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In Vitro and Cellular Antioxidant Activity of a Water Extract of Saururus chinensis

  • Kim, Gyo-Nam;Lee, Jung-Sook;Jang, Hae-Dong
    • Food Science and Biotechnology
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    • v.17 no.6
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    • pp.1332-1336
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    • 2008
  • The water extract of Saururus chinensis was investigated for oxygen radical absorbance capacity (ORAC), reducing capacity, metal chelating activity, and intracellular antioxidant activity using HepG2 cell. When 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH) was used for the generation of peroxyl radicals in vitro, S. chinensis extract (SC-E) showed the strong and concentration-dependent scavenging activity through donating protons which could be explained by its reducing property. When hydroxyl radicals were generated in vitro through the addition of $Cu^{2+}$ and $H_2O_2$, SC-E demonstrated the antioxidant activity depending on its concentration. In HepG2 cell model, most of intracellular oxidative stress generated by AAPH was efficiently removed by SC-E. However, when $Cu^{2+}$ without $H_2O_2$ was used as an oxidant in the intracellular assay, SC-E partially reduced the oxidative stress caused by $Cu^{2+}$ in cellular antioxidant activity assay system. These results indicate that SC-E could be utilized for the development of functional foods as antioxidant resource in the near future.

Korean Red Ginseng Water Extract Restores Impaired Endothelial Function by Inhibiting Arginase Activity in Aged Mice

  • Choi, Kwanhoon;Yoon, Jeongyeon;Lim, Hyun Kyo;Ryoo, Sungwoo
    • The Korean Journal of Physiology and Pharmacology
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    • v.18 no.2
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    • pp.95-101
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    • 2014
  • Cardiovascular disease is the prime cause of morbidity and mortality and the population ages that may contribute to increase in the occurrence of cardiovascular disease. Arginase upregulation is associated with impaired endothelial function in aged vascular system and thus may contribute to cardiovascular disease. According to recent research, Korean Red Ginseng water extract (KRGE) may reduce cardiovascular disease risk by improving vascular system health. The purpose of this study was to examine mechanisms contributing to age-related vascular endothelial dysfunction and to determine whether KRGE improves these functions in aged mice. Young ($10{\pm}3$ weeks) and aged ($55{\pm}5$ weeks) male mice (C57BL/6J) were orally administered 0, 10, or 20 mg/mouse/day of KRGE for 4 weeks. Animals were sacrificed and the aortas were removed. Endothelial arginase activity, nitric oxide (NO) generation and reactive oxygen species (ROS) production, endothelial nitric oxide synthase (eNOS) coupling, vascular tension, and plasma peroxynitrite production were measured. KRGE attenuated arginase activity, restored nitric oxide (NO) generation, reduced ROS production, and enhanced eNOS coupling in aged mice. KRGE also improved vascular tension in aged vessels, as indicated by increased acetylcholine-induced vasorelaxation and improved phenylephrine-stimulated vasoconstriction. Furthermore, KRGE prevented plasma peroxynitrite formation in aged mice, indicating reduced lipid peroxidation. These results suggest KRGE exerts vasoprotective effects by inhibiting arginase activity and augmenting NO signaling and may be a useful treatment for age-dependent vascular diseases.

제3세대 백금착체 항암제 신약개발 1. Design, synthesis and antitumor activity of 3rd generation platinum complexes.

  • 김대기;김강혁;김종식;주상섭;김기협;김노경
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.73-73
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    • 1993
  • As part of a research program to develope 3rd generation anti tumor platinum complexes, a series of platinum complexes which have 4, 5-bis-(aminomethyl)- 1, 3-dioxolane derivatives as bidenate amine ligands, represented by the general structual formula was prepared. The R$_1$ and/or R$_2$ substituents in this series of platinum complexes can be hydrogen. alkyl, of jointly formed cyclohexane. Two Xs can be a bidenate leaving ligand such as 1, 1-cyclobutanedicarboxylate, malonate, dimethylmalonate, ethylmalonate, glycolate, L-lactate, or N-methyliminodiacetate. From based on the pharmacological and toxicological studies, we have chosen SKI 2053R, cis-malonato[(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) complex (NSC D644591) as a candidate for clinical evaluation. The antitumor activity of a new anti tumor platinum complex, cis-malonato [(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) (SKI 2053R, NSC D644591), was compared with those of cisplatin and carboplatin using murine tumors. We evaluated three platinum complexes against L1210/CPR, a subline of L1210 leukemia resistant to cisplatin for their abilities to overcome tumor resistance to cisplatin. The in vitro cytotoxicity of SKI 2053R to L1210 cell line was 2.5-fold less potent thann that of cisplatin, and was 10-fold more cytotoxic than that of carboplatin. SKI 2053R retained similar cytotoxic effect and anti tumor activity to L1210/CPR cell line, like the cytotoxicity of SKI 2053R to L1210 cell line, while either cisplatin or carboplatin had not property to overcome the acquired cisplatin-resistance. SKI 2053R exhibited greater or comparable antitumor activity than cisplatin or carboplatin in murine tumor models.

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Effects of Lubiprostone on Pacemaker Activity of Interstitial Cells of Cajal from the Mouse Colon

  • Jiao, Han-Yi;Kim, Dong Hyun;Ki, Jung Suk;Ryu, Kwon Ho;Choi, Seok;Jun, Jae Yeoul
    • The Korean Journal of Physiology and Pharmacology
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    • v.18 no.4
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    • pp.341-346
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    • 2014
  • Lubiprostone is a chloride ($Cl^-$) channel activator derived from prostaglandin $E_1$ and used for managing constipation. In addition, lubiprostone affects the activity of gastrointestinal smooth muscles. Interstitial cells of Cajal (ICCs) are pacemaker cells that generate slow-wave activity in smooth muscles. We studied the effects of lubiprostone on the pacemaker potentials of colonic ICCs. We used the whole-cell patch-clamp technique to determine the pacemaker activity in cultured colonic ICCs obtained from mice. Lubiprostone hyperpolarized the membrane and inhibited the generation of pacemaker potentials. Prostanoid $EP_1$, $EP_2$, $EP_3$, and $EP_4$ antagonists (SC-19220, PF-04418948, 6-methoxypyridine-2-boronc acid N-phenyldiethanolamine ester, and GW627368, respectively) did not block the response to lubiprostone. L-NG-nitroarginine methyl ester (L-NAME, an inhibitor of nitric oxide synthase) and 1H-[1,2,4]oxadiazolo[4,3,-a]quinoxalin-1-one (ODQ, an inhibitor of guanylate cyclase) did not block the response to lubiprostone. In addition, tetraethylammonium (TEA, a voltage-dependent potassium [$K^+$] channel blocker) and apamin (a calcium [$Ca^{2+}$]-dependent $K^+$ channel blocker) did not block the response to lubiprostone. However, glibenclamide (an ATP-sensitive $K^+$ channel blocker) blocked the response to lubiprostone. Similar to lubiprostone, pinacidil (an opener of ATP-sensitive $K^+$ channel) hyperpolarized the membrane and inhibited the generation of pacemaker potentials, and these effects were inhibited by glibenclamide. These results suggest that lubiprostone can modulate the pacemaker potentials of colonic ICCs via activation of ATP-sensitive $K^+$ channel through a prostanoid EP receptor-independent mechanism.

Volumetric 3-D Technologies: Current Status and a Road Map for Future Research

  • Blundell, Barry G.
    • 한국정보디스플레이학회:학술대회논문집
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    • 2009.10a
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    • pp.509-509
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    • 2009
  • In this presentation, the speaker draws upon his years of research into volumetric display systems. Key content from several books is used as a basis to discuss current activity and to provide a basis for discussion on the next generation of volumetric technologies.

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