• Title/Summary/Keyword: biphenyl

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Cytotoxicity of Trichoderma spp. Cultural Filtrate Against Human Cervical and Breast Cancer Cell Lines

  • El-Rahman, Atef Abd El-Mohsen Abd;El-Shafei, Sally Mohamed Abd El-Aziz;Ivanova, Elena Vladimirovna;Fattakhova, Alfia Nurlimanovna;Pankova, Anna Victorovna;El-Shafei, Mohamed Abd El-Aziz;El-Morsi, El-Morsi Abu El-Fotouh;Alimova, Farida Kashifovna
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.17
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    • pp.7229-7234
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    • 2014
  • Trichoderma spp. are known as a rich source of secondary metabolites with biological activity belonging to a variety of classes of chemical compounds. These fungi also are well known for their ability to produce a wide range of antibiotic substances and to parasitize other fungi. In search for new substances, which might act as anticancer agents, the overall objective of this study was to investigate the cytotoxic effects of Trichoderma harzianum and Trichoderma asperellum cultural filtrates against human cervical and breast cancer cell lines (HeLa and MCF-7 cells respectively). To achieve this objective, cells were exposed to 20, 40, 60, 80 and 100 mg/ml of both T. harzianum cultural filtrate (ThCF) and T. asperellum cultural filtrate (TaCF) for 24h, then the cell viability and the cytotoxic responses were assessed by using trypan blue and 3-(4,5-dimethylthiazol-2yl)-2,5-biphenyl tetrazolium bromide (MTT) assays. Morphological changes in cells were investigated by phase contrast inverted microscopy. The results showed that ThCF and TaCF significantly reduce the cell viability, have cytotoxic effects and alter the cellular morphology of HeLa and MCF-7 cells in a concentration dependent manner. A concentration of 80 and 100mg/ml of ThCF resulted in a sharp decline in the cell viability percent of HeLa and MCF-7 respectively (25.2%, 26.5%) which was recorded by trypan blue assay. The half-maximal inhibitory concentrations ($IC_{50}$) of ThCF and TaCF in HeLa and MCF-7 were recorded as 16.6, 12.0, 19.6 and 0.70mg/ml respectively by MTT assay. These results revealed that ThCF and TaCF have a substantial ability to reduce the viability and proliferation of human cervical and breast cancer cells.

Ceriporia sp. ZLY-2010 in Biodegradation of Polychlorinated Biphenyls : Extracellular Enzymes Production and Effects of Cytochrome P450 Monooxygenase (Ceriporia sp. ZLY-2010에 의한 폴리염화비페닐류의 생분해 : 균체 외 효소활성 및 cytochrome P450 monooxygenase 영향)

  • Hong, Chang-Young;Gwak, Ki-Seob;Lee, Su-Yeon;Kim, Seon-Hong;Jeong, Han-Seob;Choi, In-Gyu
    • Journal of the Korean Wood Science and Technology
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    • v.39 no.6
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    • pp.469-480
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    • 2011
  • In this study, to determine the ligninase activity related to the PCBs degradation of Ceriporia sp. ZLY-2010, the protein contents and manganese peroxidase (MnP) and laccase activities during cultivation on shallow stationary culture (SSC) medium were observed. 4 PCB congeners were selected depending on the number of chlorine substituted on biphenyl. Furthermore, to examine the effects of cytochrome P450 monooxygenase, the inhibition of cytochrome P450 monooxygenase was evaluated by measuring the biodegradation rate when inhibitor such as 1-aminobenzotriazole was added. The extracellular protein contents were affected by PCB congeners in culture media. The total protein in the culture medium showed the biggest differences between the samples containing 2,2',4,4',5,5'-hexachlorobiphenyl and the control. On the other hand, MnP and laccase activity showed dominant increases within samples containing 4,4'-dichlorobiphenyl and 2,3',4',5-tetrachlorobiphenyl. Cytochrome P450 monooxygenase was inhibited by adding inhibitor, 1-aminobenzotriazole in low concentration. Only 2.73% of 2,3',4',5-tetrachlorobiphenyl was degraed on day 1, and biodegradation of 2,2',4,4',5,5'-hexachlorobiphenyl was inhibited as well, showing about 20% of biodegradation rate.

Selection of White Rot Fungi for Biodegradation of Polychlorinated Biphenyl, and Analysis of Its Biodegradation Rate (폴리염화비페닐류의 생분해 우수 백색부후균 선발 및 분해율 분석)

  • Hong, Chang-Young;Gwak, Ki-Seob;Lee, Su-Yeon;Kim, Seon-Hong;Choi, In-Gyu
    • Journal of the Korean Wood Science and Technology
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    • v.38 no.6
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    • pp.568-578
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    • 2010
  • In this study, the possibility of biodegradation of polychlorinated biphenyls (PCBs) by various white rot fungi was evaluated, and outstanding white rot fungi for the degradation of PCBs were selected. Seven white rot fungi were used to degrade Aroclor 1254 and 1260, which are widely considered to be toxic and difficult to degrade. And the degradation rates of Aroclors by selected white rot fungi were performed by GC analysis. Through the resistance test of white rot fungi on different concentrations of PCBs, the inhibition of mycelial growth of Cystidodontia isubellina was much less than that of others, and this fungus grew faster than others, relatively. Based on this result, it was considered that C. isubellina was selected as degrading fungus for Aroclors. As a result of biodegradation rate of Aroclors by Cystidodontia isubellina, the degradation rate of Arolor 1254 was reached to 57.57% in 13 days, which showed very high degradation rate. Also the degradation rate of Aroclor 1260 by C. isubellina had a tendency of increasing along with increasing incubation day. Maximal degradation rate of Aroclor 1260 was 49.43% at 13 days. Based on this results, it indicated that in comparison with a previous study, high degradation rate was obtained by C. isubellina.

Pharmacological Characterization of KR-31125, a Novel Nonpeptide AT1 Receptor Antagonist (안지오텐신 수용체 길항제 KR-31125의 특성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.6
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    • pp.831-837
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    • 2010
  • KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) is a potent inhibitor of angiotensin II type 1 ($AT_1$) receptors in human recombinant $AT_1$ receptors and rabbit aorta. These in vitro studies revealed that KR-31125 inhibited specific [$^{125}I$] [$Sar^1$, $Ile^8$]-angiotensin II binding to human recombinant $AT_1$ receptors in a concentration dependent manner with an $IC_{50}$ value of $19.72{\pm}2.65$ nM. However, no interaction with $AT_2$ receptors was detected as displayed by the competition binding of [$^{125}I$] CGP 42112A to human recombinant $AT_2$ receptor. The binding action was also confirmed as a competitive mode that was identical to the previously studied compound, losartan. In addition, KR-31125 caused a nonparallel shift to the right in the concentration response curves to angiotensin II with a 30-80% decrease in the maximum contractile responses ($pK_B$: 7.63). Compared to the previous studies with losartan that showed a parallel right shift in the maximum contractile responses to AII ($pA_2$: 7.59), KR-31125 presented a different mode of action with a similar potency to losartan. These results demonstrate that KR-31125 is a highly potent and $AT_1$ selective angiotensin II receptor antagonist that can be applied to the fields of new diagnostic and research tools with upcoming in vivo study results.

A Study on Pollution Levels and Source of Polychlorinated Biphenyl (PCB) in the Ambient Air of Korea and Japan (한국과 일본의 환경대기 중 폴리염화비페닐(PCB)의 농도수준 및 발생원 해석에 관한 연구)

  • Kim, Kyoung-Soo;Song, Byung-Joo;Kim, Jong-Guk;Kim, Kyeo-Keun
    • Journal of Korean Society of Environmental Engineers
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    • v.27 no.2
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    • pp.170-176
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    • 2005
  • This study was conducted to investigate the level of PCBs and distribution of PCB congeners in the ambient air of Korea and Japan. The source of PCBs were also studied by a statistical method. The TEQ concentration of PCB in the ambient air of Korea and Japan were between 0.003 and $1.01\;pgTEQ/m^3$(mean value : $0.22\;pgTEQ/m^3$) and between 0.002 and $0.014\;pgTEQ/m^3$ (mean value: $0.007\;pgTEQ/m^3$), respectively. The ambient air of industrial area of Korea showed a fluctuation in PCB concentration than other sampling area. The isomer distribution patterns in the ambient air was more or less similar in all sampling places. In addition, highly chlorinated homologues ($7{\sim}10CB$) were detected in the only Korea industrial area. This observation suggests that there is a possibility of specific source of PCBs in the industrial area. The source identification of PCB in ambient air was performed using multivariate statistical analysis(principal component analysis). As a result, it is estimated that the Korean ambient air was more influenced by combustion process than the ambient air of Japan and also the effect of PCB commercial products was relatively a small.

Impedance Characteristics of 3 Layered Green Fluorescent OLED (3층 구조 녹색 형광 OLED의 임피던스 특성)

  • Gong, Do-Hun;Im, Ji-Hyeon;Choe, Seong-U;Park, Yun-Su;Lee, Gwan-Hyeong;Ju, Seong-Hu
    • Proceedings of the Korean Institute of Surface Engineering Conference
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    • 2016.11a
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    • pp.140-140
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    • 2016
  • 유기전계발광소자 (Organic Light Emitting Diode : OLED)는 보조광원이 필요 없고 천연색 표현이 가능하며, 낮은 소비 전력 및 저전압 구동 등의 장점으로 이상적인 디스플레이 구현이 가능하여 차세대 디스플레이로써 많은 이목을 끌고 있으나 제한된 수명과 안정성의 문제점을 안고 있다. 따라서 OLED의 열화 원인을 분석하고 수명을 연장하기 위한 체계적인 방법과 기술 개발이 중요하다. Impedance Spectroscopy는 이온, 반도체, 절연체 등의 벌크 또는 계면 영역의 전하 이동을 조사하는데 사용될 수 있어, OLED에서도 Impedance Spectroscopy를 이용하여 전하수송과 전자주입 메커니즘 등 폭넓은 전기적 정보를 얻을 수 있다. 본 연구에서는 Impedance Spectroscopy를 이용하여 경과시간에 따른 OLED의 임피던스 특성을 측정하여 열화 메커니즘을 분석하였다. 본 연구에서 OLED는 ITO / 2-TNATA (4,4,4-tris2-naphthylphenyl-aminotriphenylamine) / NPB (N,N'-bis-(1-naphyl)-N, N'-diphenyl-1,1'- biphenyl-4,4'-diamine) / Alq3 (tris(quinolin-8-olato) aluminum) / Liq / Al으로 구성된 녹색 형광 OLED를 제작하였다. OLED의 전계 발광 특성을 측정하기 위한 전원 인가장치로 Keithley 2400을 사용하여 전압과 전류를 인가하였고, 소자에서 발광된 휘도 및 발광 스펙트럼은 Photo Research사의 PR-650 Spectrascan을 사용하여 암실 환경에서 측정하였다. 임피던스 스펙트럼은 컴퓨터 제어 프로그래밍이 가능한 KEYSIGHT사의 E4990A를 사용하여 측정하였다. 임피던스 측정 전압은 0 V부터 2 V 간격으로 8 V까지, 주파수는 20 Hz에서 2 kHz의 범위로 설정하여 측정하였다. I-V-L과 임피던스 특성은 24 시간의 간격을 두고 실온에서 측정하였다. 그림은 경과시간에 따른 녹색 형광 OLED의 인가전압 2 V, 6 V의 Cole-Cole plot을 나타낸 것이다. 문턱전압 미만인 인가전압 2 V에서는 소자를 통하여 전류가 흐르지 않아 큰 반원 형태를 나타내었고, 시간이 경과함에 따라 소자 제작 직후엔 실수 임피던스의 최댓값이 $8982.6{\Omega}$에서 480 시간 경과 후엔 $9840{\Omega}$으로 약간 증가하였다. 문턱전압 이상인 인가전압 6 V에서는 소자 제작 직후 실수 임피던스의 최댓값이 $108.2{\Omega}$으로 작은 반원 형태를 나타내나 시간이 경과함에 따라 방사형으로 증가하는 것을 확인 할 수 있었고, 672 시간 경과 후엔 실수 임피던스의 최댓값이 $9126.9{\Omega}$으로 문턱 전압 미만 일 때와 유사한 결과를 나타내었다. 이러한 임피던스의 증가 현상은 시간이 경과함에 따라 OLED의 열화에 의한 것으로 판단된다.

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Pharmacological Profile of KR-31125, an Orally Active AT1 Receptor Antagonist (안지오텐신 수용체 리간드 KR-31125의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.7
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    • pp.969-976
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    • 2010
  • In vivo studies of KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) were performed in pithed rats, conscious angiotensin II (AII) challenged normotensive rats, renal hypertensive rats (RHRs) and furosemide-treated beagle dogs. KR-31125 induced a non-parallel right shift in the dose-pressor response curve to AII ($ID_{50}$: 0.095 mg/kg) with a dose-dependent reduction in the maximum responses in pithed rats. Compared to losartan, this antagonistic effect was about 18 times more potent, presenting competitive antagonism. Other agonists such as norepinephrine and vasopressin did not alter the responses induced by KR-31125. Orally administered KR-31125 had no agonistic effect and dose-dependently inhibited the pressor response to AII with a slightly weaker potency ($ID_{50}$: 0.25 and 0.47 mg/kg, respectively) in the AII-challenged normotensive rat model, but with a more rapid onset of action than losartan (time to $E_{max}$: 30 min for KR-31125 and 6 hr for losartan). KR-31125 produced a dose-dependent antihypertensive effect with a higher potency than losartan in RHRs, and these effects were confirmed in furosemide-treated dogs where they presented a dose-dependent and long-lasting (>8 hr) antihypertensive effect with a rapid onset of action (time to $E_{max}$: 2-4 hr), as well as a 20-fold greater potency than losartan. These results suggest that KR-31125 is a potent, orally active $AT_1$ receptor antagonist that can be applied to the development of new diagnostic and research tools as an added exploratory potential of $AT_1$ receptor antagonist.

TM-25659-Induced Activation of FGF21 Level Decreases Insulin Resistance and Inflammation in Skeletal Muscle via GCN2 Pathways

  • Jung, Jong Gab;Yi, Sang-A;Choi, Sung-E;Kang, Yup;Kim, Tae Ho;Jeon, Ja Young;Bae, Myung Ae;Ahn, Jin Hee;Jeong, Hana;Hwang, Eun Sook;Lee, Kwan-Woo
    • Molecules and Cells
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    • v.38 no.12
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    • pp.1037-1043
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    • 2015
  • The TAZ activator 2-butyl-5-methyl-6-(pyridine-3-yl)-3-[2'-(1H-tetrazole-5-yl)-biphenyl-4-ylmethyl]-3H-imidazo[4,5-b]pyridine] (TM-25659) inhibits adipocyte differentiation by interacting with peroxisome proliferator-activated receptor gamma. 1 TM-25659 was previously shown to decrease weight gain in a high fat (HF) diet-induced obesity (DIO) mouse model. However, the fundamental mechanisms underlying the effects of TM-25659 remain unknown. Therefore, we investigated the effects of TM-25659 on skeletal muscle functions in C2 myotubes and C57BL/6J mice. We studied the molecular mechanisms underlying the contribution of TM-25659 to palmitate (PA)-induced insulin resistance in C2 myotubes. TM-25659 improved PA-induced insulin resistance and inflammation in C2 myotubes. In addition, TM-25659 increased FGF21 mRNA expression, protein levels, and FGF21 secretion in C2 myotubes via activation of GCN2 pathways (GCN2-$phosphoelF2{\alpha}$-ATF4 and FGF21). This beneficial effect of TM-25659 was diminished by FGF21 siRNA. C57BL/6J mice were fed a HF diet for 30 weeks. The HF-diet group was randomly divided into two groups for the next 14 days: the HF-diet and HF-diet + TM-25659 groups. The HF diet + TM-25659-treated mice showed improvements in their fasting blood glucose levels, insulin sensitivity, insulin-stimulated Akt phosphorylation, and inflammation, but neither body weight nor food intake was affected. The HF diet + TM-25659-treated mice also exhibited increased expression of both FGF21 mRNA and protein. These data indicate that TM-25659 may be beneficial for treating insulin resistance by inducing FGF21 in models of PA-induced insulin resistance and HF diet-induced insulin resistance.

Fabrication and Characterization of High Luminance WOLED Using Single Host and Three Color Dopants (단일 호스트와 3색 도펀트를 이용한 고휘도 백색 유기발광다이오드 제작과 특성 평가)

  • Kim, Min Young;Lee, Jun Ho;Jang, Ji Geun
    • Korean Journal of Materials Research
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    • v.26 no.3
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    • pp.117-122
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    • 2016
  • White organic light-emitting diodes with a structure of indium-tin-oxide [ITO]/N,N-diphenyl-N,N-bis-[4-(phenylm-tolvlamino)-phenyl]-biphenyl-4,4-diamine [DNTPD]/[2,3-f:2, 2-h]quinoxaline-2,3,6,7,10,11-hexacarbonitrile [HATCN]/1,1-bis(di-4-poly-aminophenyl) cyclo -hexane [TAPC]/emission layers doped with three color dopants/4,7-diphenyl-1,10-phenanthroline [Bphen]/$Cs_2CO_3$/Al were fabricated and evaluated. In the emission layer [EML], N,N-dicarbazolyl-3,5-benzene [mCP] was used as a single host and bis(2-phenyl quinolinato)-acetylacetonate iridium(III) [Ir(pq)2acac]/fac-tris(2-phenylpyridinato) iridium(III) $[Ir(ppy)_3]$/iridium(III) bis[(4,6-di-fluoropheny)-pyridinato-N,C2] picolinate [FIrpic] were used as red/green/blue dopants, respectively. The fabricated devices were divided into five types (D1, D2, D3, D4, D5) according to the structure of the emission layer. The electroluminescence spectra showed three peak emissions at the wavelengths of blue (472~473 nm), green (495~500 nm), and red (589~595 nm). Among the fabricated devices, the device of D1 doped in a mixed fashion with a single emission layer showed the highest values of luminance and quantum efficiency at the given voltage. However, the emission color of D1 was not pure white but orange, with Commission Internationale de L'Eclairage [CIE] coordinates of (x = 0.41~0.45, y = 0.41) depending on the applied voltages. On the other hand, device D5, with a double emission layer of $mCP:[Ir(pq)_2acac(3%)+Ir(ppy)_3(0.5%)]$/mCP:[FIrpic(10%)], showed a nearly pure white color with CIE coordinates of (x = 0.34~0.35, y = 0.35~0.37) under applied voltage in the range of 6~10 V. The luminance and quantum efficiency of D5 were $17,160cd/m^2$ and 3.8% at 10 V, respectively.

Thermotropic Liquid Crystalline Behavior of [4-{4'-(Nitrophenylazo)phenoxycarbonyl}]alkanoated Celluloses ([4-{4'-(니트로페닐아조)펜옥시카보닐}]알카노화 셀룰로오스들의 열방성 액정 거동)

  • Jeong, Seung-Yong;Ma, Yung-Dae
    • Polymer(Korea)
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    • v.33 no.1
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    • pp.58-66
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    • 2009
  • The thermotropic liquid crystalline behavior of the homologous series of cellulose tri[4-{4'-(nitrophenylazo) phenoxycarbonyl}] alkanoates (NACEn, n=2$\sim$8, 10, the number of methylene units in the spacer) have been investigated. All of the homologoues formed monotropic nematic phases. The isotropic-nematic transition temperature ($T_{iN}$) decreased when n is increased up to 7, but it became almost constant when n is more than 7. The plot of transition entropy at $T_{iN}$ against n had a sharp negative inflection at n=7. The sharp change at n=7 may be attributed to the difference in arrangement of the side groups. The melting temperature ($T_m$) and associated entropy change at $T_m$, in contrast with $T_{iN}$ and associated entropy change at $T_{iN}$, exhibited a distinct odd-even effect, suggesting that the average shape of the side chains in the crystalline phase is different from that in the nematic phase. The thermal stability and degree of order of the nematic phase observed for NACEn were significantly different from those reported for the homologous series of side-chain and combined type liquid crystal polymers bearing azobenzene or biphenyl units in the side chains. The results were discussed in terms of the differences in the chemical structure, the flexibility of the main chain, the mode of chemical linkage of the side group with the main chain, and the number of the mesogenic units per repeating unit.