• Title/Summary/Keyword: $\mu$-Synthesis

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Synthesis and Evaluation of Antitumor Activity

  • Jin, Guang-Zhu;Song, Gyu-Yong;Zheng, Xiang-Guo;Kim, Yong;Sok, Dai-Eun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.21 no.2
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    • pp.198-206
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    • 1998
  • Fourty eight derivatives of 2-(1-oxyalkyl)-1,4-dioxy-9,10-anthraquinone were synthesized, and their antitumor activity was evaluated. On the whole, 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones (DHAQ=1,4-dihydroxy-9,10-anthraquinone) showed stronger cytotoxic activity against L1210 cells than 2-(l-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones(DMAQ =1,4-dimethoxy-9,10-anthraquinone), implying that free hydroxy groups at C-1 and C-4 of the anthraquinone structure are necessary for the cytotoxic activity. The bioactivity of 2-(lhydroxyalkyl)-DHAQ derivatives differed according to the size of alkyl group at C-1;while the elongation of alkyl group over 7 carbon atoms failed to enhance the bioactivity, the derivatives possessing alkyl moiety of 1-6 carbon atoms showed an increase in the cytotoxicity and the antitumor activity in Sarcoma-180; 2-hydroxymethyl-DHAQ ($ED_{50}$, $15\mu\textrm{g}$/ml; T/C, 125%), 2-(1 -hydroxyethyl)-DHAQ($1.9{\mu}g/ml;139.2%)$;, 2-(1-hydroxypropyl)-DHAQ ($7.2{\mu}g$/ml; 135.1%), 2-(1-hydroxybutyl)-DHAQ ($10.2{\mu}g/ml; 125.3%)$, 2-(1-hydroxypentyl)-DHAQ ($23.7{\mu}g/ml; 110.1%$). and 2-(1-hydroxyhexyl)-DHAQ ($58{\mu}g/ml;108%$). Next, 2-(1-Hydroxyalkyl)-DHAQ derivatives were acetylated to produce 2-(1-acetoxyalkyl)-DHAQ analogues. Although the acetylation somewhat enhanced the cytotoxicity, but not the antitumor action. In addition, the presence of phenyl group at $C-1^{l}$ enhanced the cytotoxicity and the T/C value, compared to alkyl groups of same size; 2-(1-hydroxy-1-phenyl)-DHAQ ($ED_{50}$, $5.6{\mu}g$, T/C, 137%).

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Study on Pharmacological Activity of Sipjeondaebotang by Difference in Component Ratio between Astragali Radix and Cinnamomi Cortex (십전대보탕에서 황기.육계의 함량 변화에 따른 약리활성 비교 연구)

  • Lee, Ho-Young;Ha, Hye-Kyung;Jung, Da-Young;Choi, Ji-Yoon;Lee, Nam-Hun;Ma, Jin-Yeul;Yu, Young-Beob;Shin, Hyeun-Kyoo
    • The Journal of Korean Medicine
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    • v.29 no.1
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    • pp.156-166
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    • 2008
  • Objective : Pamooltang (PM) and Sipjeondaebotang (SC) are used in Korea to treat many diseases such as sterility, menstrual disorder, and general prostration. We made a comparative study of PM and SC which are different in component ratio between Astragalus membranaceus BUNGE (AC) and Cinnamomum cassia PRESL. (CC). Methods : Anti-oxidation was studied by 1.1.-diphenyl-2-picrylhydrazyl (DPPH) assay and anti-inflammation was investigated by prostaglandin $E_2\;(PGE_2)$ and nitric oxide (NO) inhibition assay. For immune response activities, this study used NO synthesis on RAW 264.7 cells and splenocyte proliferation. Results : The results showed that PM and SC components had no significant effect of anti-oxidation or anti-inflammation. However, we observed their effects upon inducible NO synthesis in Raw 264.7 cells. The SC2 stimulated NO synthesis $11.42\pm1.36{\mu}M$ (control; $0.89\pm0.00{\mu}M$). PM and SC components had the effect of immune response which in a dose-dependent manner significantly induced the splenocyte proliferation. The splenocyte proliferation induced by SC2 was higher than others at the concentration of 1, 10, 100, 1000 and 2000 ${\mu}g/ml$. The SC8 was shown to up-regulate IgG, 100 ${\mu}g/ml$ 3.3 times, 1000 ${\mu}g/ml$ 2.6 times as a control. Conclusions : These results may have important implications for our understanding of the ratios of AC and CC in SC.

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INFLUENCE OF PHENYLALANINE IN THE MEDIUM ON PROTEIN SYNTHESIS OF CHICKEN EMBRYO FIBROBLASTS

  • Kita, K.;Miyazaki, M.;Okumura, J.
    • Asian-Australasian Journal of Animal Sciences
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    • v.9 no.6
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    • pp.701-703
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    • 1996
  • The influence of phenylalanine (Phe) in the medium on protein synthesis of chicken embryo fibroblasts (CEF) was examined. CEF was derived from 9-d-old embryos by trypsin-EDTA digestion. To examine the deficiency of Phe in the medium, CEF was cultured in Dulbecco's modified Eagle's medium (DMEM) with or without Phe. CEF was also cultured in Dulbecco's phosphate buffered saline (PBS ($Ca^{2+}$, $Mg^{2+}$)) with or without $400{\mu}m$ Phe in order to examine the effect of Phe supplementation. All media were supplemented with 10% (v/v) fetal calf serum. After incubation for 6, 30 and 54 h, protein synthesis was measured by the incorporation of L-[2, $6-^{3}H$] Phe into CEF for further 18 h. Protein synthesis of CEF cultured in DMEM was higher than that in PBS ($Ca^{2+}$, $Mg^{2+}$). High specific radioactivity of Phe due to the low concentration of Phe in the medium resulted in the apparent increase in protein synthesis of CEF. Protein synthesis cultured in PBS ($Ca^{2+}$, $Mg^{2+}$) with Phe did not increase during 72 h of cell culture.

Isolation and Characterization of a Cephalosporin C Resistant and 7-Aminocephalosporanic Acid Sensitive Strain (Cephalosporin C 내성과 7-Aminocephalosporanic Acid 감수성을 지닌 균주의 선발 및 특성)

  • Kim, Ook-Hyun;Park, Yong-Chjun;Lim, Jai-Yun;Kim, Young-Chang
    • Microbiology and Biotechnology Letters
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    • v.23 no.5
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    • pp.556-558
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    • 1995
  • A strain which showed cephalosporin C resistance and 7-aminocephalosporanic acid sensitivity was isolated from nature. Among the isolates, SS5 was sensitive to cephalosporin C, penicillin G, ampicillin, 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxy cephatosporanic acid at concentrations of 1,000 $\mu $g/ml, 2,000 $\mu $g/ml, 3,000 $\mu $g/ml, 30 $\mu $g/ml 100 $\mu $g/ml and 100 $\mu $g/ml, respectively. But SS5 was sensitive at very low concentration of chloramphenicol, kanamycin, neomycin, streptomycin and tetracycline. Since SS5 was sensitive to 7-ACA (30 $\mu $g/ml) and didn't have $\beta $-lactamase activity on the cephalosporin C, SS5 could be useful as an indicator strain for the production of 7-ACA, which is an important precursor for the synthesis of many semisynthetic cephalosporins.

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Study on Antiestrogenic Effects of Tamoxifen in Immature Rat Uterus: II. Effects on Synthesis of Ribonucleic Acid and Protein (미성숙 쥐 자궁에서 Tamoxifen의 Antiestrogen 효과에 관한 연구 : II. Ribonucleic Acid 및 단백질 합성능력에 관하여)

  • Lee, Hyo-jong;Jo, Choong-ho;Park, Moo-hyun
    • Korean Journal of Veterinary Research
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    • v.26 no.1
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    • pp.31-37
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    • 1986
  • The present study has been carried out to elucidate the antiestrogenic effects of tamoxifen on RNA and protein synthesis in uteri of immature rats. Immature female Sprague-Dawley rats were allocated into 4 groups and injected with $5{\mu}g$ of estradiol-$17{\beta}$, $50{\mu}g$ of tamoxifen, a combination of both, or vehicle only subcutaneously three times with an interval of 24 hours respectively. The specific activities of $^3H$-uridine incorporation into uterine RNA and those of $^3H$-leucine incorporation into uterine protein were measured before and 1, 3, 6, 12, 24, 48 and 72 hours after the above treatments. The results obtained were summarized as follows; 1. Tamoxifen itself increased RNA synthesis an hour after treatment(169.18% of control), but it's specific activity was reduced to control level after 3 hours. Tamoxifen inhibited significantly (p<0.01) the activity of RNA synthesis of estradiol-$17{\beta}$. 2. The increasing rate of protein synthesis was lower in tamoxifen treated group than that in estradiol-$17{\beta}$ treated group. While the rate was steadily increased up to 357.4% of control by estradiol-$17{\beta}$ in 72 hours, tamoxifen itself failed to increase the rate after 24 hours and significantly (p<0.01) inhibited the activity of estradiol-$17{\beta}$(-167.4%).

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Synthesis of FAU(Faujasite)-type Zeolite with Variation of Synthesis Condition (합성조건의 변화에 따른 FAU(Faujasite)형 제올라이트의 합성)

  • 임형미;김봉영;남중희;안병길;오성근;정상진
    • Journal of the Korean Ceramic Society
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    • v.40 no.2
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    • pp.132-138
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    • 2003
  • The effect of synthesis condition, type of starting materials, mole ratio, mixing. aging, and crystallization temperature and time, on the size of FAU-type zeolite has been studied. Different mixing route may lead to the different phase of zeolite even with the same starting materials. In general, the size of particles is smaller after aging, especially at lower aging temperature. Two step mixture gel preparation method resulted to not only the reduction of crystallization time but also that of particle size, but without the aging of two mixture gels before the preparation of the overall gel in the second step, only the crystallization time was reduced, not the particle size. The FAU-type zeolite with average particle size 0.4$\mu$m and BET surface area 838 $m^2$/g was obtained from starting materials of liquid sodium silicate, sodium aluminate, and sodium hydroxide with two step preparation of mixture gel, aging of the mixture gels in two steps, which effectively reduced the crystallization time and particle size.

Role of cAMP, EGF, IGF-I and Protein Phosphorylation in Mammary Development I. Effect of EGF, IGF-I and Photoreactive Cyclic AMP on DNA Synthesis of Mammary Epithelial Cell (유선발달에 있어서 cAMP, EGF, IGF-I 및 단백질 인산화 작용의 역할 I. EGF, IGF-I 및 Photoreactive Cyclic AMP가 유선상피세포의 DNA합성에 미치는 효과)

  • 여인서;박춘근;홍병주
    • Korean Journal of Animal Reproduction
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    • v.17 no.1
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    • pp.49-56
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    • 1993
  • Mouse mammary epithelial cells(NMuMG) were plated onto 24 well phates(100,000 cells/well), in DMEM supplemented with 10% fetal calf serum. After serum starvation for 24 hours, EGF)0~100ng/ml) was added simultaneously with IGF-I(10ng/ml), 1$\mu$M photoreactive cAMP(4,5-dimethoxy-2-nitrobenzyl adenosine-3',5' cyclic monophosphate, DMNB) or IGF-I plus DMNB. After 2 hours, the cells were expposed to UV light(300nm, 3 second pulse0 in order to activate DMNB which induces a rapid transient increase in intracellular cAMP upon UV irradiation. DNA synthesis was estimated as incorporation of 3H-thymidine into DNA(1 hour pulse with 1$\mu$Ci/ml, 18~19 hours after UV exposure). Without IGF-I or DMNB, EGF(10 or 100ng/ml) increased DNA synthesis from 8,362 dpm/well in control to 16,345 or 18,684 dpm/well with EGF(pooled SE=1,239 dpm/well, P<0.05). IGF-I or IGF-I plus DMNB alone increased DNA synthesis from 8,362 dpm/well in control to 17,307 or 20,427 dpm/well, respectively(P<0.05). Addition of IGF-I, DMNB or IGF-I plus DMNB into 0~100ng/ml EGF did not significantly change the shape of dose response curve of EGF alone. In other experiment, EGF or IGF-I plus DMNB into 10ng/ml EGF group exhibited interaction effect in DNAsynthesis [EGF(10ng/ml)=18,497; IGF-I+EGF=22,837; DMNB+EGF=20,658 ; IGF-I+DMNB+EGF=29,658, pooled SE=1,055, P<0.05]. These results indicate that simultaneous activation of EGF, IGF-I and intracellular cAMP interact in DNA synthesis of mouse mammary epithelial cells.

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Semiconductor Capacitive Fingerprint Sensor and Image Synthesis Technique (반도체 capacitive 지문 센서 및 이미지 합성 방법)

  • Lee, Jeong-Woo;Min, Dong-Jin;Kim, Won-Chan
    • Journal of the Korean Institute of Telematics and Electronics D
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    • v.36D no.2
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    • pp.62-70
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    • 1999
  • This paper introduces a possibility of a low-cost, high-resolution fingerprint sensor chip. The test chip is composed of $64{\times}256$ sensing cells(chip size : $2.7mm{\times}10.8mm$). A new detection circuit of charge sharing is proposed, which eliminates the influences of internal parasitic copacitances. This the reduced sensing-capacitor size enables a high resolution of 600dpi, using even conventional 0.6${\mu}m$ CMOS process. The partial fingerprint image captured therefrom are synthesized into a full fingerprint image with a image synthesis algorithm. The problems and possibilities of image synthesis technique are also analyzed and discussed.

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Neurotoxicity of Sodium Salicylate on Spinal Sensory Neurons in Culture (배양 척수감각신경세포에 대한 살리실산 나트륨의 신경독성에 관한 연구)

  • Lee, Kang-Chang;Choi, Yu-Sun;Park, Seung-Taeck
    • The Korean Journal of Pain
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    • v.14 no.2
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    • pp.136-141
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    • 2001
  • Background: Sodium salicylate (SS) is a nonsteroidal anti-inflammatory drug (NSAID) for the treatment of neuralgia or pain from rheumatoid arthritis. When abused or used in excess, SS can induce cytotoxicity. The present study examined whether SS has a neurotoxic effect. Methods: Cell viability was examined by MTT [3-(4,5-dimethylthiazol-2,5-dipheny ltetrazolium bromide] assay and Sulforhodamine (SRB) assay after cultivating dorsal root ganglion (DRG) neurons derived from neonatal mouse. These cells were treated with various concentrations of SS for 24 hours. In addition, the amount of protein synthesis against SS was measured in these cultures. Results: Cell viability (20, $40{\mu}g/ml$ SS) significantly decreased in a dose-dependent manner. Additionally, SS inhibited protein synthesis after the exposure of cultured mouse DRG neurons to $30{\mu}g/ml$ of SS for 24 hours. Conclusions: The present study suggests that SS is toxic in cultured DRG neurons derived from neonatal mouse by decreasing cell viability and the amount of protein synthesis.

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