• Title/Summary/Keyword: L-1210

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Cytotoxicity and Antimicrobial Effect of the Extract of Salvia plebeia (배암차즈기 추출물의 세포독성과 항균효과)

  • Shin, Min-Kyo;Kim, Seok-Keun;Lee, Sang-kon;Gang, Yeong-Seong;Kim, Seong-Su;Yang, Eun-Yeong;Lee, Hyun-Ok;Baek, Seung-Hwa
    • Korean Journal of Pharmacognosy
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    • v.32 no.1 s.124
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    • pp.55-60
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    • 2001
  • The comparison of $IC_{50}$ values of Salvia plebeia R. Br. extracts on L1210, $P388D_1$ cancer and Vero normal cell lines showed that the n-hexane soluble extract of S. plebeia R. Br. retains the most growth-inhibitory activity against tumor cell lines. The minimum inhibitory concentration (MIC) of the extract against microorganisms were also examined. Antimicrobial activity of amocla and ketoconazole as references was compared to those of other solvent extracts such as $H_2O$, n-hexane, chloroform, ethyl acetate and methanol. The antimicrobial activity of extract had growth inhibition activity against gramnegative bacteria, gram-positive bacteria and fungi $(MIC\;>\;200\;{\mu}g/ml)$ except for n-hexane extract. Seven bacterial strains were tested for in vitro susceptibility to the extract of S. plebeia R. Br. However the n-hexane extract of S. plebeia R. Br. inhibited the growth of several bacterial strains (MIC values between 100 and $200\;{\mu}g/ml$ for gram positive bacteria, $25\;{\mu}g/ml$ for P. putida).

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The search and development for antitumor compounds from the marine algae (해조류 유래의 항종양성 물질의 탐색과 개발)

  • 손병화
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.211-211
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    • 1994
  • 항종양성 화합물의 개발을 지향한 해양생물 유래의 생물활성 물질의 화학적 연구의 일환으로써 다양한 종류의 생물활성 (즉, 항균작용, 혈중콜레스테롤 저하작용)등을 나타내며, 구입수가 용이한 홍조 꼬시래기 (Gracilaria verrucosa) 및 갈조 지충이 (Sargassum thunbergii)의 아세톤 및 메탄올 엑스를 EtOAc 및 n-BuOH로 분획한후 각 분획을 SiO$_2$ column, TSK gel(Toyo pearl HW-40F), $\mu$-Bondapak column 및 HPLC등으로 분리 정제하여, 새로운 glyceroglycolipid(GV-5, -6, ST-6) 및 glycerylglycoside(GV-12)를 얻었다. 이렇게 분리된 화합물의 물리화학적 성질, 화학반응 및 분광학적 data를 종합 검토한 결과 GV-5, -6, -12, 및 ST-6은 각각 1,2-diacyl-3-0-($\alpha$-D-galactopyranosyl) glycerol (acyl : palmitate-oleate-arachidonate 4: 1 : 9) (1), 1,2-diacyl -3-0-〔$\alpha$-D-galactopyranosyl -(1 "$\longrightarrow$6')-0-$\beta$-D-galactopyranosyl〕 glycerol (acyl : palmitate-oleate-arachidonate(5:1:4)(3), 2-0-($\alpha$-D-galactopyranosyl) glycerol (5), 및 sodium salt of 1-acyl-3-0-(6'-sulfo-$\alpha$-D-quinovopyranosyl) glycerol(acyl:palmitate-oleate 96:4)(8) 이라는 것이 판명되었다. 그리고 GV-5 및 -6은 마우스 백혈병세포 (L1210)에 대한 세포독성 ($IC_{50}$/ of GV-5, and -6:8.0$\mu\textrm{g}$/ml and 10.8$\mu\textrm{g}$/ml )외에, 사람의 상피암세포에 대한 성장억제효과 [growth inhibitor(%) in 20$\mu\textrm{g}$/m1 :GV-5(39.9%), GV-6(16.7%)를 나타내었으며, 한편, GV-5, GV-6, -12 및 ST-6은 각각 쥐의 F9 기형암종 세포의 분화유도 활성을 나타내어 항종양제로의 개발에 많은 흥미가 기대된다.기대된다.

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새로운 nucleoside계 항암제, ara-CDP-DL-PCA.Na(BR-28702-2)의 약효연구 및 급성독성 시험.

  • 백우현;신원섭;채희상;노정구;강부연;차신우
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.169-169
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    • 1994
  • 항암 및 면역조절작용을 가지고 있으며 그 자체가 서방성 prodrug으로서 약효를 나타낼것으로 기대되는 ara-C와 etherphospholipid의 conjugate인 ara-CDP-DL-PCA.2Na, ara-CDP-DL-PBA.2Na, 및 ara-CDP-DL-PMA.2Na 3종의 BR-8702-2의 micellar soultion을 투여시료로 하여 제암력 평가를 실시하였다. DBA/2J 마우스(평균 체중 25g, 수컷)에 L$_{1210}$임파성 백혈병 세포를 이식한 후, 24시간 후 약물을 복강내에 투여하는 실험계 에서 400mg/kg/day, 단회투여 및 80 혹은 100mg/kg/day, 1~5일간 투여로 ILS%값이 229~543으로 우수한 제암력을 보였다. 또한 BDF$_1$ mice(15~20g)의 axillary region에 3㎣의 Lewis Lung Tumor를 피하로 이식한후 약물투여를 통한 제암효과를 관찰하였다. 100, 200, 300mg/kg/day의 단회 투여계 에서는 수명연장 효과가 없었다. 한편, 20, 40, 60mg/kg/day, 1~5일간의 투여계 에서는 ara-CDP-DL-PCA.2Na만이 효과가 있었는데 농도에 역순하여 저농도인 20mg/kg/day, 1~5일간의 투여계에서 가장 효과가 있었으며 그때의 ILS%는 32.3%였고 투여기간중의 체중변화는 거의 보이지 않았다. 한편 NICOM 370 Dynamic Light Scattering을 이용하여 투여시료로한 micellar solution의 입자도를 분석한 결과 ara-CDP-DL-PCA.2Na는 4.2nm size의 것이 99.48%를 차지하고 있었다. ara-CDP-DL-PCA.2Na의 ICR 마우스를 이용한 급성독성 시험에 있어서 경구투여에서의 LD$_{50}$값은 암,수컷 모두 5000mg/kg이상 이었고, 정맥내 투여 에서는 432mg/kg이었다. 실험과정중 생존동물의 일반적 이상소견등은 없었으나 정맥내 투여의 경우에서 체중증가 억제현상이 있었다.

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Studies on the Cytotoxicity and Antimicrobial Effects of the Extract of Ajuga multiflora Bunge (조개나물 추출물의 세포독성과 항균효과)

  • Ryu, Myeng-Hwan;Aeam, Yong-Dea;Byun, Jong-Ho;Cho, Hoon;Yang, Eun-Yeong;Kang, Kil-Ung;Shin, Min-Kyo;Baek, Seung-Hwa
    • Korean Journal of Pharmacognosy
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    • v.31 no.1
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    • pp.72-76
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    • 2000
  • This study was carried out to evaluate cytotoxic effects of Ajuga multiflora Bunge extracts on murine leukemia tumor $(P388D_1)$ cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The comparison of $IC_{50}$ values of Ajuga multiflora Bunge extracts in L1210 and $P388D_1$ cell lines showed that their susceptibility to these extracts decreased in the following order: Adriamycin>methanol extract>chloroform extract>ethyl acetate extract>hexane extract>water extract by the MTT assay. In order to develop an antimicrobial agent, dried Ajuga multiflora Bunge was extracted with several solvents, and then antimicrobial activity was investigated. The minimal inhibitory concentration (MIC) of the extract against microorganisms were also examined. Antimicrobial activities of amocla and ketoconazole as references were compared to those of extracts of $H_2O$, n-hexane, chloroform, ethyl acetate and methanol. The antimicrobial activity of all extracts from the sample had growth inhibition activity against gram-negative bacteria, gram-positive bacteria and fungi $(MIC>200\;{\mu}g/ml)$. These results suggest that the methanol soluble extract of Ajuga multiflora Bunge may be a valuable choice for the studies on the treatment of murine leukemia tumor cell lines.

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Naphthazarin Derivatives: Synthesis, Inhibition of DNA Topoisomerase-I and Antitumor Activity

  • Ahn, B-Z;Kim, Y;You, Y-J;Chung, S-K;Kim, K-S;Song, G-Y;Sok, D-E
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.109-109
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    • 1997
  • Inhibitory effect on DNA topoisomerase-I, rate of glutathione conjugation and cytotoxicity of naphthoquinone derivatives were correlated. During 5 min exposure of the derivatives to glutathione (GSH), it was found that 14% of 5,8-dimethoxy-1,4-naphthoquinone(DMNQ) was converted into a GSH-conjugate, whereas 5,8-dihydroxy-1,4-naphthoquinone(DHNQ) did not interact with GSH, implying that DMNQ exerted higher electrophilicity than DHNQ. However, DHNQ (IC$\_$50/, 0.15 ${\mu}$M) showed stronger cytotoxicity in L1210 cells than DMNQ(IC$\_$50/, 0.45 ${\mu}$M). The stronger cytotoxicity of DHNQ, compared to DMNQ, could be ascribed to more rapid redox cycling. Both naphthoquinones (IC$\_$50/, 60-65 ${\mu}$M) exhibiting about the same inhibitory effect on DNA topoisomerase-I were more potent than 1,4-naphthoquinone(1,4-NQ, IC$\_$50/, 134 ${\mu}$M). Thus, 5,8-oxy groups in the structure seem to be important for the inhibition of the enzyme. DMNQ showed a broader dose range while maintaining a good antitumor activity against S-180 fluid tumor. For these reasons, DMNQ was taken as useful pharmacophore for structural modification. Introduction of 1-hydroxyalkyl groups at C-2 of DMNQ lowered all of the activities mentioned above, while acetylation of 1-hydroxyalkyl moiety enhanced the activities by 4-5 times. Introduction of the same side chains at C-6 exhibited stronger activities than 2-substituted ones. Based on these results it was suggested that the quinonoid moiety in 6-substituted DMNQ was more exposed to cellular nucleophiles such as DNA, thiols of enzymes and so on. The synthesis of DHNQ or DMNQ derivatives are going on, and the corelationship between structure-activity will be discussed.

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Pichia pastoris: A Recombinant Microfactory for Antibodies and Human Membrane Proteins

  • Goncalves, A.M.;Pedro, A.Q.;Maia, C.;Sousa, F.;Queiroz, J.A.;Passarinha, L.A.
    • Journal of Microbiology and Biotechnology
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    • v.23 no.5
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    • pp.587-601
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    • 2013
  • During the last few decades, it has become evident that the compatibility of the yeast biochemical environment with the ability to process and translate the RNA transcript, along with its capacity to modify a translated protein, are relevant requirements for selecting this host cell for protein expression in several pharmaceutical and clinical applications. In particular, Pichia pastoris is used as an industrial host for recombinant protein and metabolite production, showing a powerful capacity to meet required biomolecular target production levels in high-throughput assays for functional genomics and drug screening. In addition, there is a great advantage to using P. pastoris for protein secretion, even at high molecular weights, since the recovery and purification steps are simplified owing to relatively low levels of endogenous proteins in the extracellular medium. Clearly, no single microexpression system can provide all of the desired properties for human protein production. Moreover, chemical and physical bioprocess parameters, including culture medium formulation, temperature, pH, agitation, aeration rates, induction, and feeding strategies, can highly influence product yield and quality. In order to benefit from the currently available wide range of biosynthesis strategies using P. pastoris, this mini review focuses on the developments and technological fermentation achievements, providing both a comparative and an overall integration analysis. The main aim is to highlight the relevance and versatility of the P. pastoris biosystem to the design of more cost-effective microfactories to meet the increasing demands for recombinant membrane proteins and clinical antibodies for several therapeutic applications.

Effect of Sintering Atmosphere and Carbon Addition on Sintered Density of M3/2 Grade High Speed Steel Powder (M3/2계 고속도 공구강 분말의 소결분위기와 탄소첨가가 소결밀도에 미치는 영향)

  • Ahn, Jin-Hwan;Heo, Jong-Seo;Joo, Dong-Won;Jung, Eun;Sung, Jang-Hyun
    • Journal of Powder Materials
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    • v.5 no.4
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    • pp.265-272
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    • 1998
  • For the purpose of investigating the effect of sintering atmosphere and carbon addition on sintered density and microstructural characteristics, the M3/2 grade high speed steel powders with the addition of carbon are sintered in vacuum and $20%H_2/79%N_2/l%CH_4$ gas atmosphere. With the addition of 0 wt%C, 0.45wt%C and 1.15 wt%C the optimum sintering temperatures decrease down to $1260^{\circ}C$, $1210^{\circ}C$ and $1150^{\circ}C$ respectively for the vacuum sintered specimen, and also decrease down to $1130^{\circ}C$, $1120^{\circ}C$ and $1115^{\circ}C$ for the gas sintered specimen. The threshold temperatures for full densification decrease steeply with increasing carbon content of the sintered specimen, while this temperatures are slowly decreased at high carbon content. The vacuum sintered specimen shows the primary carbides of MC and $M_6C$ type at the optimum sintering temperature, and eutectic carbides of $M_2C$ and Fe-Cr type are produced in the oversintered specimen. The gas sintered specimen exhibits M6C and Fe-Cr type primary carbides at the optimum sintering temperature. The eutectic carbides of $M_6C$ and Fe-Cr type and MX type carbonitride are shown for the oversintered specimen in the gas atmosphere. The hardness of gas sintered specimen shows high value of 830-860 Hv due to the increment of carbide precipitation.

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Purification of Materials Produced by Amylocolatosis sp. and Anticancer Effect in Oral Cancer Model (Amylocolatosis sp.가 생산하는 항암물질의 정제 및 구강암 모델에 미치는 항암 효과)

  • Kim, Jung;Park, Young-Min;Lim, Do-Seon
    • Journal of dental hygiene science
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    • v.3 no.1
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    • pp.11-14
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    • 2003
  • A methylotrophic Actinomycetes strain, which produce the anti-oral cancer activity compound, was isolated from soil and estimated as Amylocolatosis sp. based on taxonomic studies. A methanol didn't have influence on the production of the anticancer compounds. These compound were isolated by ethylacetate extract, silica gel column chromatography, sephadex LH-20 column and reverse phase HPLC. The compounds were very stable under heat ($121^{\circ}C$), acid(pH 2.0) and alkali(pH 11.0) treatment. The cytotoxic effect of isolated anticancer compounds on various cancer cell lines such as A549, SNU-1, KB, L1210, and Sarcoma 180 was investigated by MTT assay method. And these produced compounds also showed the broad antimicrobial spectrum to test strains such as bacteria and yeast.

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Influence of the degradation of MgO protective layer on the Surface profiles and discharge characteristics in AC-PDP.

  • Lee, Soo-Beom;Jeoung, J.M.;Ko, B.D.;Oh, P.Y.;Moon, M.W.;Lee, J.H.;Lim, J.E.;Lee, H.J.;Han, Y.G.;Yoo, N.L.;Jeoung, S.H.;Son, C.G.;Choi, E.H.
    • 한국정보디스플레이학회:학술대회논문집
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    • 2005.07b
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    • pp.1207-1210
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    • 2005
  • The MgO protective layer provides protection from the discharge, lowers the discharge voltage and prolongs the AC-PDP lifetime. We have investigated the characteristics of degradation of MgO protective layer, which correlates to the image-sticking[1] and the lifetime in AC-PDP. The degraded MgO have been changed the surface morphology of MgO. It was found that panel lifetime depended on degradation of MgO protective.

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Studies on the cytotoxicity and Antimicrobial Effects of the Extract of Houttuynia cordata (IV) (어성초 추출물의 세포독성과 향균효과 (IV))

  • Lee Jeong-Ho;Park Nang-Kyu;Yang Eun-Yeong;Lee Hyun-Ok;Han Dong-Min;Baek Seung-Hwa
    • Journal of Society of Preventive Korean Medicine
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    • v.4 no.1
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    • pp.144-151
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    • 2000
  • This study was carried out to evaluate cytotoxic effects of Houttuynia cordata Thunberg extracts on murine leukemia tumor cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazol iumbromide (MMT) assay. The comparison of $IC_{50}$ values of Houttuynia cordata Thunberg extracts on $L1210,\;P388D_1$ and Vero cell lines showed that the methanol extract of Houttuynia cordata Thunberg indicated the most antitumor activity in the MTT assay. In order to develop a antimicrobial agent, dried Houttuynia cordata Thunberg was extracted with several solvents, and then antimicrobial activity was investigated. The minimal inhibitory concentration (MIC) of the extracted substance against microorganisms were also examined. Antimicrobial activity of amocla and ketoconazole as references was compared to those of other solvent extracts such as $H_2O$, n-hexane, chloroform, ethyl acetate ethanol and methanol. The antimicrobial activity of all extracts from the sample had growth inhibition activity against gram-negative bacteria, yam-positive bacteria and fungi $(MIC,\;>\;200\;{\mu} g/ml)$. These results suggest that the methanol soluble extract of Houttuynia cordata Thunberg may be a valuable choice for the studies on the treaeent of murine leukemia tumor cell lines and antimicrobial agents.

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