• 제목/요약/키워드: Biological Synthesis

검색결과 1,250건 처리시간 0.023초

핵산계 화학요법제의 합성 및 생물활성에 관한 연구 (A study on the Synthesis and Biological Activity of Nucleoside Chemotherapeutic Agents)

  • 강신원;김경희;신정희;이봉헌;장태식
    • 미생물학회지
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    • 제29권6호
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    • pp.353-360
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    • 1991
  • 5-substituted uridine(I,Br,Cl), 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate-fatty acid detrivatives were chemically synthesized. Their biological activities were determined as MIC and IC/sub 50/ unit against various pathogenic microorganisms in vitro. 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(23), 5-iodo-5'-amino-deoxyuridine-penicillin G(26) were the most efficient; their IC/sub 50/ against L5178Y murine lymphoma cell was 6.5 h/ml, MIC against S. aureus (+) and E. coli (-) was 6.25 g/ml. MIC of 5-bromo-2', 3'-O-isopropylideneuridine(6) against Trichophyton rubrum was 0.2 g/ml. And 5'-monophosphate derivatives are more active than simple uridine derivatives, suggesting other modified nucleoside 5'-phosphate may be worthwhile examing further as a new prodrugs.

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Synthesis and Evaluation of Benzoquinolinone Derivatives as SARS-CoV 3CL Protease Inhibitors

  • Ahn, Tae-Young;Kuo, Chih-Jung;Liu, Hun-Ge;Ha, Deok-Chan;Liang, Po-Huang;Jung, Young-Sik
    • Bulletin of the Korean Chemical Society
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    • 제31권1호
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    • pp.87-91
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    • 2010
  • For the discovery of new antivirals against Severe Acute Respiratory Syndrome-coronavirus (SARS-CoV), we prepared and evaluated several benzoquinoline compounds as its 3C-like protease (3CLpro) inhibitors. Based on the computer modeling study that each of the two rigid benzoquinolinone and N-phenoltetrazole moieties of the compound 1 is bound to the S1 and S2 sites, respectively, of the SARS protease by forming H-bonds and hydrophobic interactions, we designed and synthesized alkylated benzoquinolines at both the sites of the hydroxyl groups. We found that the compound 2a showed five times higher inhibiting activity against the 3CLpro compared to the compound 1.

Cloning and Expression of a cDNA AAPT3 Encoding Aminoalcoholphosphotransferase Isoform from Chinese Cabbage

  • Kim, Kwang-Soo;Park, Jong-Ho;Cho, Sung-Ho
    • Animal cells and systems
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    • 제8권2호
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    • pp.105-109
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    • 2004
  • Aminoalcoholphosphotransferase catalyzes the synthesis of phosphatidylcholine and phosphatidylethanolamine from diacylglycerol plus a CDP-aminoalcohol such as CDP-choline or CDP-ethanolamine. Previously we suggested the presence of possible isoforms of this enzyme from Chinese cabbage roots and now report the cDNA cloning and expression analysis of AAPT3 encoding a third isoform of aminoalcoholphosphotransferase (AAPT3). AAPT3 contains an open reading frame of 1,176 bp coding for a protein of 392 amino acids. It shares 96 and 95% identity with Chinese cabbage AAPT1 and AAPT2, respectively, at the deduced amino acid level. The results from reverse transcriptase-polymerase chain reaction analysis indicate that expression of AAPT3 is up-regulated by low temperature as well as AAPT1 and AAPT2.

Expression of Recombinant HBV Pol Proteins in HepG2 Cells

  • Cho, Ginam;Na, Seun-Gon;Suh, Se-Won;Jung, Gu-Hung
    • BMB Reports
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    • 제33권6호
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    • pp.440-447
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    • 2000
  • In this study HepG2 cells were used to express and purify HBV pol proteins. In order to facilitate purification of HBV pol proteins, HBV pol and its deletion mutants were fused to MBP (Maltose Binding Protein). As a result we successfully expressed and partially purified both wild type and mutant recombinant HBV pol proteins by using an amylose resin and anti-MBP antibody. In the case of wild type, the anti-MBP antibody detected three bands. One was full-length and the others were generated by proteolysis of the terminal domain region. The expressed MBP/POL proteins were localized both in the cytoplasm and in the perinuclear region. The purified proteins had polymerase activity toward an exogenous homo-polymer template. The MBP/POL protein also had DNA synthesis activity in vivo, since the MBP/POL expression construct was able to complement a HBV polymerase mutant in trans.

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Chiral Pool Synthesis of N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine from L-Malic acid

  • Hao, Bao-Yu;Liu, Jin-Qiang;Zhang, Wei-Han;Chen, Xin-Zhi
    • Bulletin of the Korean Chemical Society
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    • 제34권5호
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    • pp.1371-1377
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    • 2013
  • A new synthetic route to N-Cbz-cis-(3R,4R)-3-methylamino-4-methylpiperidine, key intermediate for CP-690,550, was disclosed with L-malic acid as the chiral pool starting material. The title compound was obtained in 16 steps with a total yield of 26% and more than 98% ee.

Analysis of Erythropoietin Glycoform Produced by Recombinant CHO Cells Using the Lectin-Blotting Technique

  • Chang, Kern-Hee;Kim, Kyung-Soo;Kim, Jung-Hoe
    • Biotechnology and Bioprocess Engineering:BBE
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    • 제3권1호
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    • pp.40-43
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    • 1998
  • The glycosylation pattern of Erythropoietin (EPO), produced by recombinant CHO cells, was studied using the simple and rapid technique of 'Lectin-blotting'. In this experiment we used three different kinds of lectins, MAA(Maackia amurensis agglutinine), RCA(Ricinus communis agglutinine), and DSA(Datura stramonium agglutinine), which bind to the terminal sialic acid, galactose, and the N-acetyllactosamine chain respectively. The lectin-blotting technique was used to analyze the carbohydrate structure of EPO produced in the presence of two physiologically active chemical compounds, ammonium and chloroquine. The effect of the ammonium ion on the glycosylation of EPO was studied because it accumulated in the medium mainly as a by-product of glutamine matabolism. Ammonium chloride significantly inhibited the sialylation of the terminal galactose residue at concentrations of 8mM or more. Chloroquine, a potent inhibitor of glycosylation, inhibited terminal sialylation at concentrations of 100 and 200 $\mu$M, and at a concentration of 300 $\mu$M, also inhibited Nacetyllactosamine chain synthesis.

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Synthesis and Biological Studies of Catechol Ether Type Derivatives as Potential Phosphodiesterase (PDE) IV Inhibitors

  • Rhee, Chung K.;Kim, Jong-Hoon;Suh, Byung-Chul;Xiang, Myung-Xik;Youn, Yong-Sik;Bang, Won-Young;Kim, Eui-Kyung;Shin, Jae-Kyu;Lee, Youn-Ha
    • Archives of Pharmacal Research
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    • 제22권2호
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    • pp.202-207
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    • 1999
  • New series of catechol ether type derivatives 5, 6 have been synthesized and applied to biological tests. Even though it is ap preliminary data, some of our target molecules show the promising result against PDE IV inhibition. SAR and biological studies with studies with synthetic compounds will be discussed in detail.

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Structural and Morphological Alterations of Candida albicans Cells after Treatment with Atratoxin $B_1$ from Holothuria atra (Jaeger)

  • Long, K.L.;Darah, I.;Ibrahim, C.O.
    • Natural Product Sciences
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    • 제4권3호
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    • pp.136-142
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    • 1998
  • Atratoxin $B_1$ which was found to inhibit the growth of Candida albicans caused structural and morphological alteration of the cells. Increased accumulation of vesicles and membranous bodies in the cytoplasm, and alterations of the cell membrane and cell wall were most obvious. Sequential lytic events of the cells eventually resulted in complete disintegration of the cytoplasmic structures. These results suggested that atratoxin $B_1$ functioned by either blocking the biosynthetic step during cell wall synthesis, altering cell wall metabolism or dissolution of the cell organelles. These changes caused a progressive destruction of the cell wall leading to cell lysis.

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화장품 소재로써의 딱지꽃(Potentilla chinensis) 뿌리 추출물의 효과 (The Effect of Roots Extract from Potentilla chinensis as Cosmeceutical Material)

  • 유재천;정해수;김형식;이정훈;모상현
    • Journal of Applied Biological Chemistry
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    • 제59권1호
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    • pp.13-17
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    • 2016
  • 천연물을 이용한 산업이 증가됨에 따라 전통약재식물들의 화장품소재로 사용하려는 관심이 높아지고 있다. 다양한 약재식물 중 딱지꽃(Potentilla chinensis) 역시도 다양한 약리 활성이 알려짐에 따라 관심이 높아지고 있다. 그러나 다양한 약리활성을 지닌 반면 딱지꽃(Potentilla chinensis) 을 이용한 산업적 응용은 거의 이루어지지 않고 있다. 본 연구에서는 화장품소재로서의 딱지꽃 뿌리 추출물에 관현 연구를 수행하였다. 그 이유는 딱지꽃의 뿌리 부분이 다른 부분보다 더 많은 약리활성을 지녔다는 보고들이 있었기 때문이다. 딱지꽃 뿌리 추출물을 얻어낸 뒤 항염증, 주름개선, 보습 그리고 미백 효과를 확인함에 따라 딱지꽃 뿌리 추출물을 화장품 소재로 응용가능한지 확인하였다. 그 결과 elastin과 aquaporin-3 증가 효과를 확인할 수 있었고, cyclooxygenase-2, metallopeptidase-1 그리고 melanin 합성 억제효과를 확인할 수 있었다.