• Title/Summary/Keyword: LB

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Antitumor Activity of LB42907, a Potent and Selective Farnesyltransferase Inhibitor: Synergistic Effect in Combination with Other Anticancer Drugs

  • Park, Ji-Hyun;Koo, Sun-Young;Kim, Dong-Myung;Kim, Kwi-Hwa;Jeong, Shin-Wu;Chung, Hyun-Ho;Cho, Heung-Soo;Park, Joong-Hoon;Yim, Hyeon-Joo;Lee, Jin-Ho;Koh, Jong-Sung;Kim, Se-Mi
    • Bulletin of the Korean Chemical Society
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    • v.29 no.7
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    • pp.1303-1310
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    • 2008
  • Inhibitors of farnesyltransferase (FT), a key enzyme in the post-translational modifications of Ras proteins, have been extensively studied as novel anticancer agents in the preclinical stages, some of which are currently in clinical development. Previously, it has been reported that a novel FT inhibitor LB42907 inhibits Ras farnesylation in the nanomolar range in vitro. The aim of this study was to assess the antitumor efficacy of LB42907 in vitro and in vivo. Anchorage-independent growth of various human tumor cell lines was potently inhibited by treatment with LB42907, comparable to other FT inhibitors in clinical development. In the nude mouse, oral administration of LB42907 demonstrated potent antitumor activity in several human tumor xenograft models including bladder, lung and pancreas origin. Interestingly, significant tumor regression in EJ (bladder) and A549 (lung) xenografts was induced by LB42907 treatment. The effectiveness of LB42907 was also investigated in simultaneous combination with paclitaxel, vincristine, cisplatin or gemcitabine against NCI-H460, A549, and HCT116 cells in vitro using median-effect analysis. LB42907 markedly synergized with most anticancer drugs tested in this study in NCI-H460 cell. In contrast, LB42907 displayed antagonism or partial synergism with these drugs in A549 and HCT116 cells, depending on the class of combined drugs and/ or the level of cytotoxicity. Our results demonstrate that LB42907 is an effective antitumor agent in vitro and in vivo and combination of LB42907 with other chemotherapeutic drugs results in synergistic or antagonistic effects mainly in a cell line-dependent manner. Further preclinical study is warranted.

A Study on the Stability of Langmuir-Blodgett(LB) Films of L-${\alpha}$-Phosphatidylethanolamine Monolayer (L-${\alpha}$-Phosphatidylethanolamine 단분자층 LB막의 안정성에 관한 연구)

  • Park, Keun-Ho
    • Journal of the Korean Applied Science and Technology
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    • v.31 no.1
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    • pp.44-49
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    • 2014
  • We were investigated by cyclic voltammetry to the stability through the electrochemical characteristics of phospholipid(L-${\alpha}$-phosphatidylethanolamine, LAPE) monolayer LB films. LAPE monolayer LB films was deposited by the LB method on the indium tin oxide(ITO) glass. The electrochemical properties was measured by cyclic voltammetry with a three-electrode system in 0.5 N, 1.0 N, 1.5 N and 2.0 N $KClO_4$ solution. The measuring range is continuously oxidized to 1650 mV, with an initial potential of -1350 mV was reduced. Scanning rates of 50, 100, 150, 200, and 250 mV/s was set. As a result, LB monolayer films of LAPE was appeared on irreversible processes by the oxidation current from the cyclic voltammogram. Diffusion coefficient (D) of LAPE was calculated 195, 15.9, 5.75, 1.38 and $0.754cm^2s^{-1}{\times}10^{-9}$ at 0.01 N, 0.05 N, 0.10 N, 0.15 N and 0.20 N $KClO_4$ solutions, respectively.

Protective Effects of Lespedeza bicolor Extract on B16/F10 Melanoma Cell Lines Damaged by Lead Acetate, Heavy Metal Compounds (중금속 화합물인 초산납으로 손상된 B16/F10 멜라닌세포주에 대한 싸리나무 추출물의 보호 효과)

  • Seo, Young-Mi
    • Korean Journal of Clinical Laboratory Science
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    • v.53 no.4
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    • pp.363-370
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    • 2021
  • This study was conducted to evaluate the dermal cytotoxicity of lead acetate (LA) and other heavy metal compounds, and the protective effect of Lespedeza bicolor (LB) extract on LA-induced cytotoxicity in cultured B16-/F10 melanoma cells. The study evaluated the antioxidative effects of LB due to its electron-donating ability (EDA), inhibitory effects on melanization and improving cell viability. LA significantly decreased cell viability in a dose-dependent manner, and the XTT50 value was determined at 52.7 µM in the studied cultures. Based on the Borenfreund and Puerner's toxicity criteria, LA was estimated to be highly cytotoxic. LA-induced cytotoxicity and cell damage was reversed by the antioxidant activity of kaempferol (KAE), thereby remarkably improving cell viability. A study of the protective effects of the LB extract on LA-induced cytotoxicity showed that the LB extract remarkably increased cell viability in the LA-treated group, and also inhibited the EDA and the total amount of melanin. The above results suggest oxidative stress-mediated cytotoxicity of LA. In the study, LB extract effectively prevented LA-induced cytotoxicity via its antioxidative activity and inhibition of melanization. In conclusion, natural resources like LB extracts may be useful agents for the prevention of oxidative stress-mediated cytotoxicity and melanization by heavy metallic compounds such as LA.

The Electro-Motive Force Generation in LB Insulating Films (LB 초박막의 기전력 발생)

  • Gwon, Yeong-Su;Gang, Do-Yeol;Guk, Sang-Hun
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 1993.05a
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    • pp.126-128
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    • 1993
  • It is well known that D.C voltage is generated at the element of MIM structure which is sandwiched between two electrode of Langmuir-Blodgett(LB) ultra-thin films. In this paper, the experiments are processed for the sample which is leaved at the atomosphere since it is fabricated in 1986. we measureed the same voltage as the time of fabricating in LB films.

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DLPC LB박막의 전기특성에 관한 연구

  • 이경섭;조수영;오재한;이우선;최충석
    • Proceedings of the Korean Society of Machine Tool Engineers Conference
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    • 1998.10a
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    • pp.97.1-100
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    • 1998
  • We studied on the ultra thin L- $\alpha$ -DLPC by LB method. The $\pi$ -A isotherm of the L- e -DLPC was measured at the air-water interface varying with the compressing speed and amounts of solutions for spreading. The molecular arrangement of deposited films were evaluated by measuring the absorption with the UV spectrometer. And we made structures of metal(Au)/L- $\alpha$ -DLPC/Metal(Au) and examined electron through L- $\alpha$ -DLPC LB films by means of current-voltage(I- V) measurement

Phenomena of voltage generation in langmuir-blodgett ultra-thin films (Langmuir-Blodgett 초박막의 전압발생현상)

  • ;;;;Taro Hino
    • Electrical & Electronic Materials
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    • v.6 no.3
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    • pp.228-231
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    • 1993
  • Langmuir-Blodgett(LB) 초박막 MIM구조의 소자에서 직류전압이 발생된다는 것은 이미 잘 알려져 있다. 발생전압의 원인은 LB막과 전극사이의 어떤 화학반응에 의한 것으로 보고되었다. 본 논문에서는 1986년에 제작되어 공기중에 방치된 LB 초박막 시료를 대상으로 실험한 결과, 제작 당시와 동일한 크기의 전압이 발생하고 있음을 확인할 수 있었다. 이때 LB막과 전극의 두께는 각각 20~30.angs. 및 2000.angs.정도이었다.

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Resistance and Frequency Properties Analysis of QCM Coated with LB Films (LB막이 누적된 QCM의 저항 및 주파수 특성해석)

  • 강현욱;진철남;김정명;권명수
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 1997.11a
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    • pp.465-467
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    • 1997
  • The oscillating properties of quartz Crystal Microbalance(QCM) were analyzed by electrical measurement. We tried to analyze the properties of quartz crystal coated with Langmuir-Bladgett(LB) films using the frequency and resistance at resonance in the electrical equivalent circuit. The resonant frequency was decreased linearly as to layers of LB films, however, there are some gap between theoretical values, Sauerbrey's equation and experimental values. The resistance was increase nonlinearly as to layers.

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Probiotic Properties of Lactic Acid Bacteria Isolated Traditional Fermented Foods (전통발효식품 유래 유산균의 프로바이오틱스 특성 연구)

  • Kim, Eun-Ji;Jo, Seung-Wha;Kim, Jin-Kyeong;Jeong, Do-Youn
    • Journal of Life Science
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    • v.29 no.6
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    • pp.697-704
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    • 2019
  • This study performed to investigate the probiotic properties of lactic acid bacteria 200 strains isolated from traditional fermented foods. Based on being higher tolerance to bile salts and showing higher acid resistance, 4 LAB Strains were selected in the screening experiment; Lactobacillus plantarum SRCM 102224, Lb. plantarum SRCM102227, Lb. paracasei SRCM102329, Lb. paracasei SRCM102343. Antibacterial activity against various pathogens, acid and bile salt tolerance, hemolytic phenomenon, cell surface hydrophobicity, and antibiotic resistance were examined. Among the tested strains, SRCM 102343 (95.9%) was highly observed hydrophobicity compared to Lb. rhmanosus GG (13.4%) as control. In this study, the in vitro adhesion properties of 4 strains of LAB was investigated using human intestinal caco-2 cell cultures. SRCM102329 and SRCM102343showed higher adherence to caco-2 cells than Lb. rhamnosus GG. The antibacterial activities of 4 strains LAB were investigated. the 3 strains showing strongly antimicrobial activity against Escherichia coli ATCC10798, Staphylococcus aureus KCCM11593, Listeria invanovii KCTC3444, Bacillus cereus ATCC11778 and S. enterica serovar. Typhi KCTC1926. These results suggest that selected strains have good probiotic potential for application in functional foods.

LB30057 Inhibits Platelet Aggregation and Vascular Relaxation Induced by Thrombin

  • Jung, Byoung-In;Kang, a-Kyu-Tae;Bae, Ok-Nam;Lee, Moo-Yeol;Chung, Seung-Min;Lee, Sang-Koo;Kim, In-Chul;Chung, Jin-Ho
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.879-884
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    • 2002
  • Previous study showed that an amidrazonophenylalanine derivative, LB30057, which has high water solubility, inhibited the catalytic activity of thrombin potently by interaction with the active site of thrombin. In the current investigation, we examined whether LB30057 inhibited platelet aggregation and vascular relaxation induced by thrombin. Treatment with LB30057 to plateletrich plasma (PRP) isolated from human blood resulted in a concentration-dependent inhibition of thrombin-induced aggregation. Values for $IC_{50}$ and $IC_{100}$ were $54{\pm}4$ nM and $96{\pm}3$ nM, respectively. This inhibition was agonist (thrombin) specific, since $IC_{50}$ values for collagen and ADP were \much greater than those for thrombin. In addition, concentration-dependent inhibitory effects were observed on the serotonin secretion induced by thrombin in PRP. Consistent with these findings, thrombin-induced increase in cytosolic calcium levels was inhibited in a concentration-dependent manner. When LB30057 was treated with aortic rings isolated from rats, LB30057 resulted in a concentration-dependent inhibition of thrombin-induced vascular relaxation. All these results suggest that LB30057 is a potent inhibitor of platelet aggregation and blood vessel relaxation induced by thrombin.

Changes in Nodule-Specific Proteins during Nodule Development of Canavalia lineata (해녀콩(Canavalia lineata)의 뿌리혹 발달 단계에 따른 뿌리혹 특이 단백질의 변화 양상)

  • 최성화
    • Journal of Plant Biology
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    • v.34 no.2
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    • pp.121-127
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    • 1991
  • Total soluble proteins from three developmental stages of induced root nodules of Canavalia lineata were compared with those of non-nodulated roots by SDS-PAGE and two dimensional (2-D) gel electrophoresis. Thirteen nodule-specific protein (nodulin) bands were identified by the former and 30 nodule specific protein spots were detected by the latter method respectively. Some of the nodulins were detected differentially depending on the nodule's developmental stages. For example, only three leghemoglobin (Lb)-like protein spots appeared at stage I (d<2 mm), but two additional Lb-like protein spots appeared at stage II (d <4-5 mm). pI value and molecular weight of nomomers of Lb-like protein were narrower and greater than those of soybean, ranging from 4.4 to 5.0 and 15.7 kd respectively. Northern blot hybridization of total RNAs from roots and root nodules using soybean Lb cDNA as a probe made it clear that Lb gene was expressed tissue-specifically only in the root nodules.odules.

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