• Title/Summary/Keyword: K-7174

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A Straightforward Synthesis of K-7174, a GATA-Specific Inhibitor

  • Majik, Mahesh S.;Yu, Jin-Ha;Jeong, Lak-Shin
    • Bulletin of the Korean Chemical Society
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    • v.33 no.9
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    • pp.2903-2906
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    • 2012
  • K-7174, a GATA-specific inhibitor, is a putative anti-inflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. An expeditious four-step synthesis of K-7174 is described in this paper. The route employs Wittig olefination and bis-alkylation of homopiperazine as the key reactions. The iodine-catalyzed isomerization of the Z-isomer results in complete conversion to the E-isomer is the highlight of our synthetic endeavors.

Variation of Disease Severity by Mixed Inoculation of Compatible and Incompatible Races of Bacterial Blight in Rice (비친화적 및 친화적 레이스의 혼합접종에 따른 벼흰잎마름병 발병도의 변화)

  • Kim, Bo-Ra;Lee, Eun-Jeong;Choi, Jae-Eul
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.52 no.2
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    • pp.162-168
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    • 2007
  • Compatible and incompatible interactions of near-isogenic lines containing one of Xa1, Xa3, and Xa7 resistance genes with Japanese bacterial blight isolates (T7174, T7147, and T7133) were examined in order to determine the variation of bacterial blight resistance and the stability of resistance gene. IRBB 101 line having a Xal gene was compatible (host susceptible) with T7147 and T7133 isolates but incompatible (host resistant) with T7174 isolate at all the tested rice growth stages. IRBB 103 line having a Xa3 gene was susceptible or moderately resistant to the three isolates at seedling and maximum tillering stage but resistant at heading stage. IRBB 101 line having a Xa7 gene was semi-compatible with the three isolates at seedling stage but incompatible at the other growth stages. Overall there were clear differences between compatible and incompatible interactions of rice with Xanthomonas oryzae pv. oryzae races. In the mixed inoculations of compatible and incompatible isolates, the lesion length from near-isogenic lines decreased as the ratios of incompatible races increased. When the distinction between compatible and incompatible isolates was unclear, there was almost no variation of lesion length regardless of mixed ratios. The pathogenicity of the mixed races in the incompatible Interactions increased rather than the individual inoculation whereas the lesion length of compatible interactions was similar to that of the individual inoculation. These data indicate the incompatible races inhibit the virulence of a compatible race but compatible races increase the disease occurrence due to incompatible races. Furthermore, IRBB 107 line that showed resistance to all the isolates at all the tested growth stages was considered as a good parent f3r breeding of resistant variety.

Quantitative Analysis of t-Cinnamaldehyde of Cinnamomum cassia by $^1H-NMR$ Spectrometry ($^1H-NMR$을 이용한 계피의 t-cinnamaldehyde 정량분석)

  • Song, Myoung-Chong;Yoo, Jong-Su;Baek, Nam-In
    • Applied Biological Chemistry
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    • v.48 no.3
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    • pp.267-272
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    • 2005
  • trans-Cinnamaldehyde, a major component of Cinnamomum cassia, was quantitatively analyzed using the $^1H-NMR$ spectrometry. Applicability of this method was confirmed through observing the variation of chemical shift in the $^1H-NMR$ spectrum of t-cinnamaldehyde and the integration value according to various sample concentrations or running temperatures. When the $^1H-NMR$ spectrometry was run for t-cinnamaldehyde (7.1429 mg/ml) at 19, 25, 30, 40 and $50^{\circ}C$, the chemical shifts of the doublet methine signal due to an aldehyde group were observed at 9.7202, 9.7184, 9.7169, 9.7142 and 9.7124 ppm, respectively, to imply that the running temperature had no significant variation in the chemical shift of the signal. The integration values of the signal were $1.37\;(19^{\circ}C),\;1.37\;(25^{\circ}C),\;1.37\;(30^{\circ}C),\;1.37(40^{\circ}C)$ and $1.37(50^{\circ}C)$, respectively, to also indicate running temperature gave no effect on the integration value. When the sample solutions with various concentrations such as 0.4464, 0.8929, 1.7857, 3.5714, 7.1429 and 14.286 mg/ml were respectively measured for the $^1H-NMR$ at $25^{\circ}C$, the chemical shifts of the aldehyde group were observed at 9.7206, 9.7201, 9.7196, 9.7192, 9.7185 and 9.7174 ppm. Even though the signal was slightly shifted to the high field in proportion to the increase of sample concentration, the alteration was not significant enough to applicate this method. The calibration curve for integration values of the doublet methine signal due to the aldehyde group vs the sample concentration was linear and showed very high regression rate ($r^2=1.0000$). Meantime, the $^1H-NMR$ spectra (7.1429 mg/ml $CDCl_3,\;25^{\circ}C$) of t-cinnamaldehyde and t-2-methoxycinnamaldehyde, another constituent of Cinnamomum cassia, showed the chemical shifts of the aldehyde group as ${\delta}_H$ 9.7174 (9.7078, 9.7270) for the former compound and ${\delta}_H$ 9.6936 (9.6839, 9.7032) for the latter one. The difference of the chemical shift between two compounds was big enough to be distinguished using the NMR spectrometer with 0.45 Hz of resolution. The contents of cinnamaldehyde in Cinnamomum cassia, which were respectively extracted with n-hexane, $CHCl_3$, and EtOAc, were determiend as 94.2 \;mg/g (0.94%), 137.6 mg/g (1.38%) and 140.1 mg/g(1.40%) t-cinnamaldehyde in each extract, respectively, by using the above method.

Lack of Association of the NPAS2 Gene Ala394Thr Polymorphism (rs2305160:G>A) with Risk of Chronic Lymphocytic Leukemia

  • Rana, Sobia;Shahid, Adeela;Ullah, Hafeez;Mahmood, Saqib
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.17
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    • pp.7169-7174
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    • 2014
  • Background: NPAS2 is a product of the circadian clock gene. It acts as a putative tumor suppressor by playing an important role in DNA damage responses, cell cycle control and apoptosis. Chronic lymphocytic leukemia (CLL) appears to be an apoptosis related disorder and alteration in the NPAS2 gene might therefore be directly involved in the etiology of CLL. Here, the Ala394Thr polymorphism (rs2305160:G>A) in the NPAS2 gene was genotyped and melatonin concentrations were measured in a total of seventy-four individuals, including thirty-seven CLL cases and an equal number of age- and sex-matched healthy controls in order to examine the effect of NPAS2 polymorphism and melatonin concentrations on CLL risk in a Pakistani population. Materials and Methods: Genotyping of rs2305160:G>A polymorphism at NPAS2 locus was carried out by amplification refractory mutation system-polymerase chain reaction (ARMS-PCR). Melatonin concentrations were determined by enzyme linked immunosorbent assay (ELISA). Statistical analysis was performed using Statistical Package for Social Sciences software. Results: Our results demonstrated no association of the variant Thr genotypes (Ala/Thr and Thr/Thr) with risk of CLL. Similarly, no association of rs2305160 with CLL was observed in either females or males after stratification of study population on a gender basis. Moreover, when the subjects with CLL were further stratified into shift-workers and non-shift-workers, no association of rs2305160 with CLL was seen in either case. However, significantly low serum melatonin levels were observed in CLL patients as compared to healthy subjects (p<0.05). Also, lower melatonin levels were seen in shift-workers as compared to non-shift-workers (p<0.05). There was no significant difference (p>0.05) in the melatonin levels across NPAS2 genotypes in all subjects, subjects with CLL who were either shift workers or non-shift-workers. General Linear Model (GLM) univariate analysis revealed no significant association (p>0.05) of the rs2305160 polymorphism of the NPAS2 gene with melatonin levels in any of the groups. Conclusions: While low melatonin levels and shift-work can be considered as one of the risk factors for CLL, the NPAS2 rs2305160 polymorphism does not appear to have any association with risk of CLL in our Pakistani population.