• Title/Summary/Keyword: Analogs

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Effect of impression coping and implant angulation on the accuracy of implant impressions: an in vitro study

  • Jo, Si-Hoon;Kim, Kyoung-Il;Seo, Jae-Min;Song, Kwang-Yeob;Park, Ju-Mi;Ahn, Seung-Geun
    • The Journal of Advanced Prosthodontics
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    • v.2 no.4
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    • pp.128-133
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    • 2010
  • PURPOSE. The purpose of this study was to compare the accuracy of the implant master cast according to the type (pick-up, transfer) and the length (long, short) of the impression copings. MATERIALS AND METHODS. The metal master cast was fabricated with three internal connection type implant analogs (Osstem GS III analog), embedded parallel and with $10^{\circ}$ of mesial angulation to the center analog. Four types of impression coping were prepared with different combinations of types (transfer, pick-up) and lengths (long, short) of the coping. The impressions were made using vinyl polysiloxane (one step, heavy + light body) with an individual tray, and 10 impressions were made for each group. Eventually, 40 experimental casts were produced. Then, the difference in the distance between the master cast and the experimental cast were measured, and the error rate was determined. The analysis of variance was performed using the SPSS (v 12.0) program (${\alpha}$= .05), and the statistical significance was set at P < .05. RESULTS. The ANOVA showed that the pick-up type impression coping exhibited a significantly lower error rate than the transfer type. However, no significant difference was observed with respect to the length of the impression coping. Additionally, no significant difference was observed between the parallel and mesial angulated groups. CONCLUSION. Within the limitations of this study, the pick-up type impression coping exhibited a more accurate implant master cast than the transfer type in parallel group. The accuracy of the implant master cast did not differ for different lengths of impression coping of at least 11 mm. Additionally, the accuracy of the implant cast was not different for the parallel and $10^{\circ}$ mesial angulated groups.

Nuclear Imaging of Cellular Proliferation (핵의학적 세포증식 영상)

  • Yeo, Jeong-Seok
    • The Korean Journal of Nuclear Medicine
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    • v.38 no.2
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    • pp.198-204
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    • 2004
  • Tumor cell proliferation is considered to be a useful prognostic indicator of tumor aggressiveness and tumor response to therapy but in vitro measurement of individual proliferation is complex and tedious work. PET imaging provides a noninvasive approach to measure tumor growth rate in situ. Early approaches have used $^{18}F$-FDG or methionine to monitor proliferation status. These 2 tracers detect changes in glucose and amino acid metabolism, respectively, and therefore provide only an indirect measure of proliferation status. More recent studies have focused on DNA synthesis itself as a marker of cell proliferation. Cell lines and tissues with a high proliferation rate require high rates of DNA synthesis. $[^{11}C]Thymidine$ was the first radiotracer for noninvasive imaging of tumor proliferation. The short half-life of $^{11}C$ and rapid metabolism of $[^{11}C]Thymidine$ in vivo make the radiotracer less suitable for routing use. Halogenated thymidine analogs such as 5-iodo-2-deoxyuridine (IUdR) can be successfully used as cell proliferation markers for in vitro studies because these compounds are rapidly incorporated into newly synthesized DNA. IUdR has been evaluated as a potential in vivo tracer in nuclear medicing but the image qualify and the calculation of proliferation rates are impaired by its rapid in vivo degradation. Hence, the thymidine analog $3'-deoxy-3'-^{18}F-fluorothymidine$ (FLT) was recently introduced as a stable proliferation marker with a suitable nuclide half-life and stable in vivo. $[^{18}F]FLT$ is phosphorylated to 3-fluorothymidine monophosphate by thymidine kinase 1 and reflects thymidine kinase 1 activity in proliferating cell. $[^{18}F]FLT$ PET is feasible in clincal use and well correlates with cellular proliferation. Choline is a precursor for the biosynthesis of phospholipids (in particular, phosphatidylcholine), which is the essential component of all eukaryotic cell membranes and $[^{11}C]choline$, which is a new marker for cellular proliferation.

Stereochemistry of the Degradation Product of (-)-α-Narcotine and Its Analogs with Ethyl Chloroformate ((-)-α-Narcotine과 유사화합물을 ethyl chloroformate로 반응시 생성된 분해물의 입체화학)

  • Lee Dong-Ung
    • Journal of Life Science
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    • v.15 no.1 s.68
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    • pp.147-151
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    • 2005
  • A$(-)-\alpha$-narcotine from Papaver sommiferum was refluxed with ethyl chloroformate to give the diastereomeric chloro-carbamate mixture and the Z/E-enol lactones as Z:E=1:1.1 ratio in HPLC analysis. After photoisomerization with UV (254 nm), the Z/E ratio was drastically changed to Z:E=7:1, which may indicate that the E-isomer was easily converted to the Z-isomer due to photoisomerization. The photoisomerization of the Z/E-enol lactones and the different stereochemistry of the degradation product of $\beta-narcotine$, deuterated $\beta-narcotine$ and $\beta-narcotine$ with ethyl chloroformate will also be discussed.

NMR Studies on Turn Mimetic Analogs Derived from Melanocyte-stimulating Hormones

  • Cho, Min-Kyu;Kim, Sung-Soo;Lee, Myung-Ryul;Shin, Joon;Lee, Ji-Yong;Lim, Sung-Kil;Baik, Ja-Hyun;Yoon, Chang-Ju;Shin, In-Jae;Lee, Weon-Tae
    • BMB Reports
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    • v.36 no.6
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    • pp.552-557
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    • 2003
  • Oligomers with $\alpha$-aminooxy acids are reported to form very stable turn and helix structures, and they are supposed to be useful peptidomimetics for drug design. A recent report suggested that homochiral oxa-peptides form a strong eight-member-ring structure by a hydrogen bond between adjacent aminooxy-acid residues in a $CDCl_3$ solution. In order to design an $\alpha$-MSH analog with a stable turn conformation, we synthesized four tetramers and one pentamer, based on $\alpha$-MSH sequence, and determined the solution structures of the molecules by two-dimensional NMR spectroscopy and simulated annealing calculations. The solution conformations of the three peptidomimetic molecules (TLV, TDV, and TLL) in DMSO-$d_6$ contain a stable 7-membered-ring structure that is similar to a $\gamma$-turn in normal peptides. Newly-designed tetramer TDF and pentamer PDF have a ball-type rigid structure that is induced by strong hydrogen bonds between adjacent amide protons and carbonyl oxygens. In conclusion, the aminooxy acids, easily prepared from natural or unnatural amino acids, can be employed to prepare peptidomimetic analogues with well-defined turn structures for pharmaceutical interest.

Topographical Changes and Textural Characteristics in the Areas Around the Saemangeum Dyke (새만금방조제 축조에 따른 지형 및 입도특성의 변화)

  • Lee, Hee-Jun;Jo, Hyung-Rae;Kim, Min-Ji
    • Ocean and Polar Research
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    • v.28 no.3
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    • pp.293-303
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    • 2006
  • The topography of the sea floor and textural characteristics of surface sediments are documented in areas off sectors 1,2, and 4 of the Saemangeum dyke and inside the dyke. These were investigated during the years 2002 to 2005, when the dyke construction almost came to an end, and were compared with natural topographic analogs before the dyke construction from the maritime maps of 1982 and 1994. Along and across the dyke are a number of erosional troughs formed by intensified currents during the dyke construction. The sea floor off sector 4 has undergone gradual accumulation of sands moving from the north by currents varying in direction from normal to parallel to the dyke. This is in a strong contrast with a slight erosional environment prevailing over the sea floor before dyke construction. off sectors 1 and 2, a topography with an alterative pattern of erosional troughs and sand shoals develops normal to the dyke. Eroded materials from the troughs seem to have added to the sand shoals. As a result, the troughs, former natural tidal channels, have become increasingly deeper, whereas the sand shoals have become somewhat shallower. The sea floor inside the dyke has also been remarkably shallower with expanding tidal flats due to trapping by the dyke of continuous sediment input from the Dongjin and Mangyeong rivers. Sands, all of which are considered to have originated originally from the two rivers, dominate the entire Saemangeum area.

Optimization of Physical Conditions for Caviar Analog Preparation Using Calcium-alginate Gel Capsules

  • Ji, Cheong-Il;Cho, Sueng-Mock;Yun, Young-Soo;Kim, Seon-Bong
    • Fisheries and Aquatic Sciences
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    • v.10 no.3
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    • pp.103-112
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    • 2007
  • High prices, overfishing, and contamination have limited the availability of natural caviar as a food product. We attempted to apply encapsulation by calcium-alginate gel membranes to caviar analog preparation in an effort to produce a high-quality replacement for natural caviar. Physical conditions of stirring speed $(X_1,\;rpm)$ and gelation time $(X_2,\;min)$ as the independent variables for gelation were optimized by response surface methodology. Sphericity $(Y_1,\;%)$, diameter $(Y_2,\;mm)$, membrane thickness $(Y_3,\;mm)$, rupture strength $(Y_4,\;g)$, and rupturing deformation $(Y_5,\;mm)$ were used as the dependent variables to compare characteristics of the capsules for caviar analogs with natural caviar. The values of the independent variables as evaluated by multiple response optimization were $X_1=-0.1271 (278 rpm) and $X_2=0.4436$ (12.2 min), respectively. Predicted values of the four dependent variables were $Y_1=97.7%,\;Y_2=2.97mm,\;Y_4=1,465g,\;and\;Y_5=1.15mm$. Membrane thickness $(Y_3)$ was eliminated from the dependent variables for multiple response optimization because it could not be measured with an image analyzer. The experimental values prepared under the optimal conditions for verification nearly coincided with the predicted values and satisfied the conditions of natural caviar.

Mechanisms Underlying Relaxations Caused by Angiotensin II and Its Analogs in Isolated Rabbit Mesenteric Artery

  • Hong, Ki-Whan;Park, Ji-Young;Kim, Chi-Dae;Lee, Won-Suk;Rhim, Byung-Yong;Yoo, Sung-Eun
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.4
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    • pp.393-402
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    • 1997
  • In the present study, we characterized the angiotensin II (AII)-induced relaxations in the phenylephrine-precontracted rabbit mesenteric arteries with endothelium. 1) AII-induced relaxation was consistently observed in the rabbit mesenteric arteries with and without endothelium, but not in the aortic segment with endothelium. 2) AII-induced endothelium-dependent relaxation was markedly inhibited by $N^w-nitro-L-arginine$ (L-NNA, $100\;{\mu}M$), methylene blue ($10\;{\mu}M$) and LY83583 ($10\;{\mu}M$), respectively. 3) Inhibition of cyclooxygenase with indomethacin ($10\;{\mu}M$) strongly decreased the vasorelaxant response to AII irrespective of the presence of endothelium. 4) 7-Ethoxyresorufin ($1\;{\mu}M$) and clotrimazole ($1\;{\mu}M$), inhibitors of cytochrome P-450-dependent arachidonic acid metabolism, greatly attenuated the vasodilator response to AII. 5) Carbacyclin, arachidonic acid and prostaglandin $F_{2{\alpha}}$ ($PGF_{2{\alpha}}$) caused concentration-dependent relaxations in the mesenteric artery with endothelium, which were inhibited by L-NNA and methylene blue. 6) AII and $PGF_{2{\alpha}}$ significantly stimulated cyclic GMP formation in the mesenteric arteries with endothelium, which was inhibited by L-NNA and methylene blue, respectively. 7) AII enhanced synthesis of $PGF_{2{\alpha}}$ and 6-keto $PGF_{1{\alpha}}$ from the arterial segments with endothelium, which was inhibitable by indomethacin, but not by L-NNA. In conclusion, the vasorelaxant responses to AII of the rabbit mesenteric artery with endothelium are subserved by arachidonic acid and its metabolites produced via activation of cyclooxygenase and cytochrome P-450 enzyme as well as by nitric oxide.

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Pharmacology of enantiomers of higenamine and related tetrahydroisoquinolines

  • Park, Min-Kyu;Huh, Ja-Myung;Lee, Young-Soo;Kang, Young-Jin;Seo, Han-Geuk;Lee, Jae-Heun;Park, Hye-Sook-Yun-;Lee, Duck-Hyung;Chang, Ki-Churl
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2004.04a
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    • pp.3-10
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    • 2004
  • Oxidative stress is a constant threat to all living organisms and an immense repertoire of cellular defense systems is being employed by most pro- and eukaryotic systems to eliminate or to attenuate oxidative stress. Ischemia and reperfusion is characterized by both a significant oxidative stress and characteristic changes in the antioxidant defense. Heme oxigenase-l (HO-l) is up-regulated by various stimuli including oxidative stress so that it is thought to participate in general cellular defense mechanisms against ischemic injury in mammalian cells. Higenamine, an active ingredient of Aconite tuber, has been shown to have antioxidant activity along with inhibitory action of inducible nitric oxide synthase (iNOS) expression in various cells. In the present study, we investigated whether higenamine and related analogs protect cells from oxidative cellular injuries by modulating antioxidant enzymes, such as HO-l, MnSOD etc. R-form of YS-51 was the most potent inducer of HO-l in bovine endothelial cells, which inhibited apoptotic cell death by H$_2$O$_2$. HO-1 induction by YS 51 was mediated by PI3 kinase activation in which PKA- as well as PKG pathway is considered as important regulators. YS-51 also induced Mn-SOD mRNA expression by activating c-jun N-terminal kinase in endothelial cells and Hela cells. In ROS 17/2.1 cells, higenamine and enetiomers of related compounds inhibited iNOS expression by cytokine mixtures. Taken together, higenamine and related compounds can be developed as possible protective agents from oxidative cell injury or death.

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Targeting Nrf2-Mediated Gene Transcription by Triterpenoids and Their Derivatives

  • Loboda, Agnieszka;Rojczyk-Golebiewska, Ewa;Bednarczyk-Cwynar, Barbara;Zaprutko, Lucjusz;Jozkowicz, Alicja;Dulak, Jozef
    • Biomolecules & Therapeutics
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    • v.20 no.6
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    • pp.499-505
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    • 2012
  • Chemoprevention represents a strategy designed to protect cells or tissues against various carcinogens and carcinogenic metabolites derived from exogenous or endogenous sources. Recent studies indicate that plant-derived triterpenoids, like oleanolic acid, may exert cytoprotective functions via regulation of the activity of different transcription factors. The chemopreventive effects may be mediated through induction of the nuclear factor erythroid 2-related factor 2 (Nrf2) transcription factor. Activation of Nrf2 by triterpenoids induces the expression of phase 2 detoxifying and antioxidant enzymes such as NAD(P)H quinone oxidoreductase 1 (NQO1) and heme oxygenase-1 (HO-1) - proteins which can protect cells or tissues against various toxic metabolites. On the other hand, inhibition of other transcription factors, like NF-${\kappa}B$ leads to the decrease in the pro-inflammatory gene expression. Moreover, the modulation of microRNAs activity may constitute a new mechanism responsible for valuable effects of triterpenoids. Recently, based on the structure of naturally occurring triterpenoids and with involvement of bioinformatics and computational chemistry, many synthetic analogs with improved biological properties have been obtained. Data from in vitro and in vivo experiments strongly suggest synthetic derivatives as promising candidates in the chemopreventive and chemotherapeutic strategies.

Function of the Tethered rec-eCG in Rat and Equine Receptors

  • Park, Jong-Ju;Jargal, Naidansuren;Yoon, Jong-Taek;Min, Kwan-Sik
    • Reproductive and Developmental Biology
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    • v.33 no.4
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    • pp.229-236
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    • 2009
  • The glycoprotein hormone family represents a class of heterodimers, that includes the placental hormone equine chorionic gonadotropin (eCG) and the anterior pituitary hormones- follitropin (FSH), lutropin (LH), and thyrotropin (TSH). The 4 hormones are heterodimers, with a common $\alpha$-subunit and unique $\beta$-subunits. eCG is the most heavily glycosylated of the known pituitary and placental glycoprotein hormones. Recent observations using single chain glycoprotein hormone analogs in which, the $\beta$-and $\alpha$-subunits are linked, implied that heterodimeric-like quaternary configuration is not a prerequisite for receptor/signal transduction. To study the function and signal transduction of tethered rec-eCG, a single chain eCG molecule was constructed and rec-eCG protein was produced. Molecular mass of the single chain is about 45 kDa. All mice were ovulated by tethered rec-eCG treatment. The dual activity of tethered rec-eCG was determined in receptor cell lines of nonequid species; in fact, this dual activity was proven in species other than horse. Tethered rec-eCG in equids does not bind to FSH receptors, suggesting that eCG is primarily an LH-like hormone in the horse. Taken together, these data suggest that tethered rec-eCG has dual activity in nonequid species in vitro. However, it has only LH-like activity in equid species in vitro.