• Title/Summary/Keyword: ${\mu}$ Synthesis

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Synthesis and Biological Evaluation of Phosphonate Analogues of 1 $\alpha$, 25-Dihydroxyvitamin $D_3$

  • Han, Gyoon-hee
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.206-210
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    • 2000
  • A new series of phosphonate side chain analogues of 1$\alpha$,25-dihydroxyvitamin $D_3$ (1) have been synthesized. Antiproliferative activities of theses analogues (8a,b and 9a,b) using human keratinocyte cell shows that analogues which have natural A-ring show higher activity than unnatural A-ring series and almost equally active to 1 $\alpha$,25-Dihydroxyvitamin $D_3$(1) at 1 $\mu$M level.

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Differential inhibitory effects of alpha-viniferin, resveratrol trimer on inflammatory mediators

  • Chung, Eun-Yong;Min, Kyung-Rak;Kim, Young-Soo
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.213.1-213.1
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    • 2003
  • Alpha-viniferin was isolated from Carex humilis (Cyperaceae), and showed anti-inflammatory effects on carrageenin or histamine-induced paw edema in mice. To understand mode of the anti-inflammatory action. effects of alpha-viniferin on cyclooxygenase (COX)-2, iNOS, oxygen radicals and proinflammatory cytokines have been analyzed. Alpha-viniferin showed selective inhibitory effect with an IC50 value of 5 $\mu\textrm{m}$ on COX-2 activity but showed weak inhibitory effect on the synthesis of COX-2 transcript which was identified by RT-PCR. (omitted)

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5-Arylidene-2(5H)-furanone Derivatives: Synthesis and Structure-Activity Relationship toward Cytotoxicity

  • Bang, Seong-Cheol;Kim, Yong;Yun, Mi-Young;Kim, Dong-Hee;Ahn, Byung-Zun
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.343.2-343.2
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    • 2002
  • Ranunculin (RAN). isolated from Ranunculaceae. exhibited significant cytotoxic activity against KB and Bel-7402 cells with ED$_{50}$ values of 0.21 and 0.35).${\mu}4M respectively. Under physiological condition. the ranunculin was deglycosylated to be protoanemonin. an active form containing ${\alpha}{\beta}$-unsaturated ketone moiety. which successively dimerized to be anemonin inactive form. (omitted)

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Stereoselective synthesis of novel 4′$\alpha$-C-methyl branched novel carbocyclic nucleosides

  • Kim, Ji-Hee;Ko, Ok-Hyun;Hong, Joon-Hee
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.345.2-345.2
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    • 2002
  • Recently. 4'${\alpha}$-C homologated furanose nucleosides. especially alkyl branches. are molecules of considerable current interest. One of reasons for this prominence arises from the notable biological activities as antiviral and antitumor agents. as shown in 4'${\alpha}$-C-methyl-2-deoxythymidine (EC$_{50}$ = 7.2$\mu$M against HIV in MT-4 cell), 4'${\alpha}$-C-fluoromethyl-2-deoxycytidine. 4'${\alpha}$-C-hydroxymethylthymidine and 4'${\alpha}$- -C-azidomethyl-thymidine. (omitted)omitted)

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Effects of Nicotine on the Expression of Cell Cycle Regulatory Proteins of Human Gingival Fibroblasts (니코틴이 치은섬유아세포의 세포주기 조절 단백질 발현에 미치는 영향)

  • Kim, Tak;Kim, Jae-ho;Pi, Sung-Hee;Kim, Eun-Cheol;You, Yong-Ouk;You, Hyung-Keun;Shin, Hyung-Shik
    • Journal of Periodontal and Implant Science
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    • v.31 no.3
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    • pp.597-610
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    • 2001
  • Normal gingival fibroblasts functioning is fundamental for the maintenance of periodontal connective tissue as well as wound healing. Nicotine have been found to affect DNA synthesis and cell proliferation, which appear to depend on the type of cells. This in vitro study was done to determine the effects of nicotine, a major component of tobacco, on cell proliferation, viability, activity, cell cycle distribution, and expression of cell cycle regulatory proteins in human gingival fibroblasts. Nicotine has been tested for 2 days or 4 days in 5 different concentrations; $0.1{\mu}g/ml$; $1{\mu}g/ml$; $10{\mu}g/ml$; $100{\mu}g/ml$; $1000{\mu}g/ml$. To assess cell proliferation and viability, viable and non-viable cells were counted by hemocytometer; to evaluate cellular activity, MTT assay was employed; to analyze cell cycle distribution, fluorescent propidium iodide-DNA complex were measured using fluorocytometer; to determine the expression of cell cycle regulatory proteins, western blot analysis was performed. After 2 days and 4 days incubation respectively, at concentrations of $1{\mu}g/ml$ - $1000{\mu}g/ml$, nicotine significantly inhibited proliferation comparing to non-supplemented controls. The cell viability was significantly decreased after 2 days and 4 days at concentrations of $1{\mu}g/ml$ - $1000{\mu}g/ml$ and at $10{\mu}g/ml$ - $1000{\mu}g/ml$ respectively. After 2 days and 4 days, the cellular activity was significantly decreased at concentrations of $10{\mu}g/ml$ - $1000{\mu}g/ml$. Treatment with $100{\mu}g/ml$ nicotine for 48 hours caused an increase in the proportion of G1-phase cells (from 46.41% to 53.46%) and a decrease in the proportion of S-phase cells (from 17.80% to 14.27%). The levels of cyclin $D_1$ and CDK 4 proteins in nicotine-treated fibroblasts were lower than that of controls, whereas the levels of p16 and pRB were higher than that of controls. These results suggest that the decrease of cell proliferation and lengthened Gap phases (G1) by nicotine may due to the increased expression of p16 and pRB as well as decreased expression of cyclin $D_1$ and CDK 4 in human gingival fibroblasts.

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Determination of the Period of the Formation and Size of Sieve Element Area and Sieve Pore (Streptanthus tortus 조직배양 세포에서 사공의 형성시기와 사공 영역과 사공의 크기 결정)

  • Cho, Bong-Heuy
    • Journal of Plant Biotechnology
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    • v.29 no.1
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    • pp.41-44
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    • 2002
  • During the phloem development from parenchyma cells in a suspension culture of Streptanthus induced sucrose carrier and glucose carrier disappeared. Sieve element area and sieve pore induced suspension culture of Streptanthus were formed almost at the last period of the synthesis of sieve endoplasmic reticulum (SER) and p-protein. The new synthesized cell wall begann to digeste only after the new cell wall was surrounded by SER. The digested region of the cell wall and the formed region of sieve pore were regular comparatively. The completed sieve pore was an oval form, and the outer portion of sieve pore varied, ca 1.2 ${\mu}{\textrm}{m}$~1.6 ${\mu}{\textrm}{m}$ in longitudinal, 0.8 ${\mu}{\textrm}{m}$~1.3 ${\mu}{\textrm}{m}$ in tangential, and the inner size of sieve pore was irregular form of a star-like shape. The number of sieve pore between sieve cells was ca 2~7 per ${\mu}{\textrm}{m}$$^2$ and the sieve pore wall with callose was 0.05 ${\mu}{\textrm}{m}$~0.07 ${\mu}{\textrm}{m}$ in thickness. The energy for the formation of sieve element area and sieve pore might be supplied by mitochondria near the new cell wall and the role of SER remains to be illucidated.

Whitening Effect of Hizikia fusiformis Ethanol Extract and Its Fractions (톳(Hizikia fusiformis) 에탄올 추출물 및 분획물의 미백활성)

  • Jeon, Myong-Je;Kim, Mi-Hyang;Jang, Hye-Ji;Lee, Seung-Woo;Kim, Jae-Hoon;Kim, Hyung-Suk;Lee, Sang-Hyeon
    • Journal of Life Science
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    • v.22 no.7
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    • pp.889-896
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    • 2012
  • Melanin synthesis is catalyzed by tyrosinase. To investigate the whitening effect of Hizikia fusiformis, fractions from ethanol extract of H. fusiformis were prepared by a systematic fractionation procedure with solvents such as methanol, hexane, butanol, and $H_2O$. The ethanol extract and its fractions were then subjected to evaluate the inhibitory effects on the tyrosinase activity and melanin synthesis in murine B16F10 melanoma cells. The ethanol extract and aqueous fraction exhibited a whitening effect with no cytotoxicity. The ethanol extract showed the highest whitening effect among the samples. The inhibitory effect of $100{\mu}g/ml$ of ethanol extract was higher than that of $10{\mu}g/ml$ of arbutin, but it was lower than that of $10{\mu}g/ml$ of kojic acid. Furthermore, the inhibitory effects of $100{\mu}g/ml$ of methanol, hexane, butanol, and aqueous fractions were similar to those of $10{\mu}g/ml$ of arbutin. The antioxidant activities were examined by comparing the results with that of ascorbic acid as a positive control. The ethanol extract and aqueous fraction showed relatively higher DPPH radical-scavenging activities compared with the other samples. Furthermore, $500{\mu}g/ml$ of ethanol extract and aqueous fraction diminished LPS-induced iNOS expression to 82 and 80%, respectively. These results suggest that ethanol extract and aqueous fraction of H. fusiformis could be used as cosmetic ingredients for whitening and skin protection effects.

The Effects of Nifedipine on Cellular Activity of Human Gingival Fibroblast (Nifedipine이 건강 치은 조직의 치은 섬유모세포에 미치는 영향)

  • Shin, Hyung-Shik;Han, Hee-Ran;Kim, Myung-Eun
    • Journal of Periodontal and Implant Science
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    • v.26 no.3
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    • pp.669-679
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    • 1996
  • Gingival overgrowth is a well known side effect of several drugs, including nifedipine, phenytoin, cyclosporin, dilitiazem, verapamil. A number of studies have been performed to investigate the mechanism by which nifedipine(a calcium channel blocking agent) affects the gingival tissue. The aim of the present work was to investigate the effect of nifedipine on healthy gingival fibroblasts with special emphasis on determining the changes in cellular proliferation and protein and collagen synthesis. Gingival fibroblasts were obtained from the explants of healthy gingiva of extracted 3rd molars or premolar teeth extracted from the patients for orthodontic treatment. To evaluate the effect of nifedipine on cell proliferation, the cells were seeded at a cell density of $1{\times}10^4$cells/well in 24-well culture plates and treated with 100 and 200ng/ml of nifedipine for 10days. After trypsinization, the cells were counted with a haemocytometer on 1st, 3rd, 5th, 7th and 10th days. Then, MTT assay was carried out. For total protein and percent collagen synthesis, $3{\mu}Ci/ml$ $^3H-proline$ was added to each well for the final 4 hours of the incubation period. The results indicate that nifedipine does not influence cell proliferation in healthy gingival fibroblast in vitro and has a specific effect in reducing total protein and percent collagen synthesis. On the above the findings, exogenous nifedipine does not influence on healthy human gingival fibroblast proliferation and protein and collagen synthesis.

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Effects of Abscisic acid and Temperature on the Anthocyanin Accumulation in Seedlings of Arabidopsis thaliana

  • Song Ju-Yeun;Kim Tae-Yun;Hong Jung-Hee
    • Journal of Environmental Science International
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    • v.14 no.12
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    • pp.1093-1102
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    • 2005
  • Effects of abscisic acid(ABA) and temperature on the anthocyanin accumulation and phenylalanine ammonia Iyase(PAL) activity were investigated in seedlings of Arabidopsis thaliana. In time course study, exogenous application of ABA $(50-1000\;{\mu}M)$ led to a noticeable increase in anthocyanin pigments which persisted over the following 5 days. Anthocyanins increased in concert with the chlorophyll loss. The activity of PAL, a key enzyme in the phenylpropanoid pathway, increased on exposure to ABA and reached maximum on the 4th day, This result shows that anthocyanin synthesis and PAL activity have a close physiological relationships. In the effects of temperatures ($10^{\circ}C,\;17^{\circ}C,\;25^{\circ}C$and $30^{\circ}C$) on anthocyanin accumulation and PAL activity in seedlings, a moderate-low temperatures ($17^{\circ}C$) enhanced both anthocyanin content and PAL activity, whereas elevated temperatures ($30^{\circ}C$) showed low levels of anthocyanin and PAL activity, suggesting a correlation between temperature-induced anthocyanin synthesis and the accumulation of PAL mRNA. Simultaneous application of ABA with temperatures Induced higher anthocyanin synthesis and PAL activity in seedlings than ABA or temperature stress alone. Moderate-low temperature with ABA exposure elicited the maximal induction of anthocyanin synthesis and PAL activity. Therefore, ABA treatment significantly increased thermotolerance in .A. thalinan seedlings. Ethephon and ABA showed similar mode of action in physiological effects on anthocyanin accumulation and PAL activity. Our data support that anthocyanins may be protective in preventing damage caused by environmental stresses and play an important role in the acquisition of freezing tolerance.

GTP Induces S-phase Cell-cycle Arrest and Inhibits DNA Synthesis in K562 Cells But Not in Normal Human Peripheral Lymphocytes

  • Moosavi, Mohammad Amin;Yazdanparast, Razieh;Lotfi, Abbas
    • BMB Reports
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    • v.39 no.5
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    • pp.492-501
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    • 2006
  • Since differentiation therapy is one of the promising strategies for treatment of leukemia, universal efforts have been focused on finding new differentiating agents. In that respect, we used guanosine 5'-triphosphate (GTP) to study its effects on K562 cell line. GTP, at concentrations between 25-200 ${\mu}M$, inhibited proliferation (3-90%) and induced 5-78% increase in benzidine-positive cells after 6-days of treatments of K562 cells. Flow cytometric analyses of glycophorine A (GPA) showed that GTP can induce expression of this marker in more mature erythroid cells in a time- and dose-dependent manner. These effects of GTP were also accompanied with inhibition of DNA synthesis (measured by [$^3H$]-thymidine incorporation) and early S-phase cell cycle arrest by 96 h of exposure. In contrast, no detectable effects were observed when GTP administered to unstimulated human peripheral blood lymphocytes (PBL). However, GTP induced an increase in proliferation, DNA synthesis and viability of mitogen-stimulated PBL cells. In addition, growth inhibition and differentiating effects of GTP were also induced by its corresponding nucleotides GDP, GMP and guanosine (Guo). In heat-inactivated medium, where rapid degradation of GTP via extracellular nucleotidases is slow, the anti-proliferative and differentiating effects of all type of guanine nucleotides (except Guo) were significantly decreased. Moreover, adenosine, as an inhibitor of Guo transporter system, markedly reduced the GTP effects in K562 cells, suggesting that the extracellulr degradation of GTP or its final conversion to Guo may account for the mechanism of GTP effects. This view is further supported by the fact that GTP and Guo are both capable of impeding the effects of mycophenolic acid. In conclusion, our data will hopefully have important impact on pharmaceutical evaluation of guanine nucleotides for leukemia treatments.