• Title/Summary/Keyword: Sensitivity derivatives

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Phenyl substituent effect on the fungicidal activity of N-Phenyl-O-phenylthionocarbamate derivatives (N-Phenyl-O-phenylthionocarbamate 유도체의 항균활성에 미치는 phenyl 치환기의 효과)

  • Sung, Nack-Do;Soung, Min-Gyu
    • The Korean Journal of Pesticide Science
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    • v.3 no.1
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    • pp.29-36
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    • 1999
  • A series of N-phenyl-O-phenylthionocarbamate derivatives were synthesized and determinated fungicidal activities in vitro against gray mold (Botrytis cinerea) and capsicum phytophthora blight (Phytophthora capsici) which showed resistance and sensitivity to benomyl and metalaxyl as systemic fungicides, respectively. The structure-activity relationship (SAR) was investigated by Free-Wilson analysis method and Hansch method. From the basis on the findings, the N-phenyl(X) groups had more contributions than O-phenyl(Y) groups did and ortho-substituents on the N-phenyl group showed high fungicidal activities. Especially, 4-cyano substituent, 2 as X-group showed 50% inhibition($pI_{50}=5.50$) of hyphae growth at 0.8ppm against resistance P. capsici (RPC) And hydroxyl substituents, 12 and 23 displayed the highest fungicidal activity against resistant B. cinerea (RBC), sensitive B. cinerea (SBC), and sensitive P. capsici (SPC). Antifungal activities of SPC were dependent upon molar refractivity (MR) constant and those of others relied on hydrophobic parameters (${\sigma}$ and logP). For increasing fungicidal activity against RPC and SBC, the optimum values of the sigma (${\sigma}$) and field(F) constants as electron withdrawing groups were 0.32 and 0.18, respectively.

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Interaction of Barley Acetolactate Synthase with Triazolopyrimidine Inhibitors (Triazolopyrimidine계 저해제와 보리 Acetolactate Synthase와의 상호작용)

  • Lee, Jae Soeb;Chang, Soo Ik;Nam Goong, Sung Keon;Shin, Jung Hyu;Choi, Jung Do
    • Journal of the Korean Chemical Society
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    • v.42 no.3
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    • pp.306-314
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    • 1998
  • Acetolactate synthase (ALS) is the common enzyme in the biosynthesis of branched chain amino acids, Val, Leu, and Ile in bacteria, yeast, and higher plants. The enzyme is target site of several classes of structually diverse herbicides, including the sulfonylureas, the imidazolinones, the triazolopyrimidines, and the primidyl-oxy-benzoates. We have synthesized new triazolopyrimidine (TP) derivatives, and determined their inhibitory activities on barley ALS. $lC_{50}$ values for the active compounds were 3.2 nM-0.62 mM, and some of them appeared to be potent inhibitors. The progress curves for inhibition of ALS by TP4, a representative derivative, indicated that the extent of inhibition increased with incubation time. The inhibition of ALS by TP4 showed mixed-type inhibition with respect to pyruvate. Dual inhibition analyses of TP4 versus imidazolinone Cadre and feedback inhibitor Leu suggested that three different classes of inhibitors bind to ALS in a mutually exclusive manner. Chemical modification of tyrosyl residues of ALS decreased sensitivity of ALS to TP4, while modification of tryptophan and cysteine did not affect the sensitivity.

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Multi-Level Optimization of Framed Structures Using Automatic Differentiation (자동미분을 이용한 뼈대구조의 다단계 최적설계)

  • Cho, Hyo-Nam;Chung, Jee-Sung;Min, Dae-Hong;Lee, Kwang-Min
    • Journal of Korean Society of Steel Construction
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    • v.12 no.5 s.48
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    • pp.569-579
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    • 2000
  • An improved multi-level (IML) optimization algorithm using automatic differentiation (AD) of framed structures is proposed in this paper. For the efficiency of the proposed algorithm, multi-level optimization techniques using a decomposition method that separates both system-level and element-level optimizations, that utilizes and an artificial constraint deletion technique, are incorporated in the algorithm. And also to save the numerical efforts, an efficient reanalysis technique through approximated structural responses such as moments and frequencies with respect to intermediate variables is proposed in the paper. Sensitivity analysis of dynamic structural response is executed by AD that is a powerful technique for computing complex or implicit derivatives accurately and efficiently with minimal human effort. The efficiency and robustness of the IML algorithm, compared with a plain multi-level (PML) algorithm, is successfully demonstrated in the numerical examples.

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Development of Enzyme-Linked Immunosorbent Assay for Rapid and Sensitive Analysis of Biotin (Biotin의 분석을 위한 효소면역측정법(ELISA)의 개발)

  • 이경애;손동화;고영태
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.27 no.6
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    • pp.1152-1159
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    • 1998
  • In order to develop more rapid and reproducible analysis of biotin known as vitamin H, attempts were made to establish the condition for enzyme linked immunosorbent assay(ELISA) compared with traditional microbiological assay(MBA). Antibiotin and antiserum were obtained from the immunized rabbits injected with emulsion of biotin KLH conjugate and Freund's adjuvant. The antiserum showed cross reactivity on biocytin, a derivative of biotin, which is converted to biotin in intestine, at the rate of 177%(median inhibitory concentration(IC50)=12.58ppb), but not on other derivatives such as desthiobiotin, diaminobiotin and 2 imino biotin. Specific antibody for biotin was purified from the antiserum through protein A column and desalting column. The conditions of competitive direct ELISA (cdELISA) were established. Detection range of biotin concentration by cdELISA was 0.01∼300ng/ ml(ppb). In the spike test with milk, fruit flake and pine carrot juice, the correlation coefficient between two methods of MBA and ELISA was reliably consistent at the value of r=0.992. But detection of biotin by microbiological assay(MBA) was rather restricted in range and nonspecific. Detection range of biotin by MBA was 0.1∼0.5ng/ml(ppb). It showed cross reactivities on biocytin and desthiobiotin at the rate of 80.1% and 66.7%, respectively. In conclusion, ELISA revealed a significant improvement compared with MBA for the biotin detection in terms of sensitivity, detection range and cross reactivity. In addition, a variety of samples could be analyzed rapidly and conveniently at one time by using ELISA. These results strongly suggest that the ELISA is very promising for the practical application to detect biotin contents in a wide range of food stuffs.

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A Study on Measurement of Internal Defects of Pressure Vessel by Digital Shearography(I) (전자 전단 간섭법을 이용한 압력용기의 내부결함 측정에 관한 연구(I))

  • Kang, Young-June;Park, Nak-Kyu;Ryu, Won-Jae;Kim, Kyung-Suk
    • Journal of the Korean Society for Nondestructive Testing
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    • v.22 no.4
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    • pp.393-401
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    • 2002
  • Pipelines in power plants, nuclear facilities and chemical industries are often affected by corrosion effects. It is important to inspect the internal defects in pipelines in oder to guarantee safe operational condition. We have taken relatively much time, cost and manpower to use conventional NDT methods because these methods are contact measuring methods. In this paper, we used digital shearography, a laser-based optical method which allows full-field measurement of surface displacement derivatives. This method has many advantages in practical use, such as low sensitivity to environmental noise, simple optical configuration and real time measurement. The experiment was performed with pressure vessels which has different internal cracks and detected internal cracks in the pressure vessels at a real time using phase shifting method.

Quantitative Analysis of Pentachlorophenol in Paper Products (종이재 중의 Pentachlorophenol 정량 분석)

  • Hahn, Airan;Park, Jihye;Choi, Hyeongki;Hong, Sungyeap;Han, Hyechul;Jo, Byoungmuk;Oh, Jungsoo
    • Applied Chemistry for Engineering
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    • v.16 no.3
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    • pp.323-327
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    • 2005
  • Pentachlorophenol (PCP) is a representative compound of chlorophenol derivatives which are especially toxic and potentially carcinogenic compounds in the priority pollutant list of the EPA (Environmental Protection Agency, USA). The aim of this study was to investigate an analysis method of PCP in infinitesimal quantity retained in paper. PCP in paper was pretreated by solid phase extraction (SPE) in a phenyl cartridge. The extracted sample was acetylated or silylated and analyzed with GC/MS-SIM. The detection sensitivity of silylated PCP was improved significantly when compared with those of PCP itself and acetylated PCP. As a test specimen, an office paper and a wallpaper were used.

Chemical Modification and Feedback Inhibition of Arabidopsis thaliana Acetolactate Synthase (아라비돕시스 탈리아나 Acetolactate Synthase의 화학적 변형과 되먹임 방해)

  • Hong, Seong-Taek;Choi, Myung-Un;Shin, Jung-Hyu;Koh, Eun-Hie
    • Applied Biological Chemistry
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    • v.40 no.4
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    • pp.277-282
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    • 1997
  • Acetolactate synthase (ALS) was partially purified from Escherichia coli MF2000/pTATX containing Arabidopsis thaliana ALS gene. The partially purified ALS was examined for its sensitivity toward various modifying reagents such as iodoacetic acid, iodoacetamide, N-ethylmaleimide (NEM), 5,5'-dithiobis(2-nitrobenzoic acid) (DTNB), p-chloromercuribenzoic acid (PCMB), and phenylglyoxal. It was found that PCMB inhibited the enzyme activity most strongly followed by DTNB and NEM. Since iodoacetic acid did not compete with substrate pyruvate, it appeared that cysteine is not involved in the substrate binding site. On the other hand, the substrate protected the enzyme partly from inactivation by phenylglyoxal, which might indicate interaction of arginine residue with the substrate. The partially purified enzyme was inhibited by end products, valine and isoleucine, but not by leucine. However, the ALS modified with PCMB led to potentiate the feedback inhibition of all end products. Additionally, derivatives of pyrimidyl sulfur benzoate, a candidate for a new herbicide for ALS, were examined for their inhibitory effects.

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Enhanced Sensitivity to Gefitinib after Radiation in Non-Small Cell Lung Cancer Cells

  • Choi, Yun-Jung;Rho, Jin-Kyung;Back, Dae-Hyun;Kim, Hye-Ryoun;Lee, Jae-Cheol;Kim, Cheol-Hyeon
    • Tuberculosis and Respiratory Diseases
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    • v.71 no.4
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    • pp.259-265
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    • 2011
  • Background: Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, gefitinib and erlotinib, are effective therapies for non-small cell lung cancer (NSCLC) patients whose tumors harbor somatic mutations in EGFR. The mutations are, however, only found in about 30% of Asian NSCLC patients and all patients ultimately develop resistance to these agents. Ionizing radiation has been shown to induce autophosphorylation of EGFR and activate its downstream signaling pathways. In the present study, we have tested whether the effect of gefitinib treatment can be enhanced after ionizing radiation. Methods: We compared the PC-9 and A549 cell line with its radiation-resistant derivatives after gefitinib treatment with cell proliferation and apoptosis assay. We also analyzed the effect of gefitinib after ionizing radiation in PC-9, A549, and NCI-H460 cells. Cell proliferation was determined by MTT assay and induction of apoptosis was evaluated by flow cytometry. Caspase 3 activation and PARP cleavage were evaluated by western blot analysis. Results: PC-9 cells having mutated EGFR and their radiation-resistant cells showed no significant difference in cell viability. However, radiation-resistant A549 cells were more sensitive to gefitinib than were their parental cells. This was attributable to an increased induction of apoptosis. Gefitinib-induced apoptosis increased significantly after radiation in cells with wild type EGFR including A549 and NCI-H460, but not in PC-9 cells with mutated EGFR. Caspase 3 activation and PARP cleavage accompanied these findings. Conclusion: The data suggest that gefitinib-induced apoptosis could increase after radiation in cells with wild type EGFR, but not in cells with mutated EGFR.

Simultaneous Gas Chromatography-Mass Spectrometric Determination of Total and Individual Phthalic Esters Utilizing Alkaline Hydrolysis and Silyl Derivatization Technique

  • Kim, Min-Seon;Li, Dong-Hao;Shim, Won-Joon;Oh, Jae-Ryoung;Park, Jong-Man
    • Bulletin of the Korean Chemical Society
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    • v.28 no.3
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    • pp.432-438
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    • 2007
  • Environmentally important phthalic esters have been analyzed by GC-MS in terms of individual phthalic esters or total phthalic esters directly or after derivatization. Derivatization improves the chromatographic characteristics of the highly polar phthalic esters. This study focused on the GC-MS determination of the total phthalic esters and the individual phthalic esters simultaneously. The phthalic esters were hydrolyzed to phthalate and corresponding alcohols in 1 M NaOH solution at 90 oC for 30 min followed by extraction with ethyl acetate after acidifcation. The phthalic acid and alcohols were simultaneously silyl derivatized using bis(trimethylsilyl)trifluoroacetamide (BSTFA) to their corresponding silyl ester and ethers in the mixture of 60% acetone and 40% ethyl acetate at room temperature within 30 min. Because of the high reactivity of BSTFA with the phthalic acid and alcohols effective silyl derivatization was possible simultaneously. GC-MS analysis of the silyl derivatives of phthalic acid and alcohols was performed. The total phthalic ester content was estimated from the analytical result of phthalic silyl ester, while the individual phthalic ester was quantified from the analytical results of alcoholic silyl ethers. This technique was applied to spiked tab water and real seawater samples from the Lake Shihwa in Korea. The results were checked against the results from the direct GC-MS analysis of the phthalic esters and reasonable recoveries with high sensitivity were achieved. The recoveries were higher than 75% with low relative standard deviation (below 10%).

RETRIEVAL OF LOCAL INTERPLANETARY DUST EMISSIVITY BY ASTRO-F

  • HONG S. S.;KWON S. M.;PYO J.;UENO M.;ISHIGURO M.;USUI F.;WEINBERG J. L.
    • Journal of The Korean Astronomical Society
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    • v.37 no.4
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    • pp.159-169
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    • 2004
  • This is a proposal to probe local part of the interplanetary dust (IPD) cloud complex and retrieve mean volume emissivity of the local IPDs at mid-infrared wavelengths. This will be done by monitoring, with Infrared Camera (IRC) aboard the ASTRO-F, the annual modulation of the zodiacal emission. In pointing mode of the ASTRO-F mission the spacecraft can make attitude maneuvering over approximately ${\pm}1^{\circ}$ range centered at solar elongation $90^{\circ}$ in the ecliptic plane. The attitude maneuvering combined with high sensitivity of the IRC will provide us with a unique opportunity observationally to take derivatives of the zodiacal emission brightness with respect to the solar elongation. From the resulting differential of the brightness over the ${\pm}1^{\circ}$ range, one can directly determine the mean volume emissivity of the local IPDs with a sufficient accuracy to de-modulate the annual emissivity variations due to the Earth's elliptical motion and the dis-alignment of the maximum IPD density plane with respect to the ecliptic. The non-zero eccentricity ($e_{\oplus}$= 0.0167) of the Earth's orbit combined with the sensitive temperature dependence of the Planck function would bring modulations of amplitude at least $3.34\%$ to the zodiacal emission brightness at mid-infrared wavelengths, with which one may determine the IPD temperature T(r) and mean number density n(r) as functions of heliocentric distance r. This will in turn fix the power-law exponent $\delta$ in the relation $T(r) = T_o(r/r_o)^{-\delta}$ for the dust temperature and v in $n(r) = n_o(r/r_o)^-v$ for the density. We discuss how one may de-couple the notorious degeneracy of cross-section, density, reference temperature $T_o$ and exponent $\delta$.