• Journal of Korean Society of Environmental Engineers
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• v.30 no.11
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• pp.1087-1094
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• 2008

Diazinon is a phosphorothiate insecticide widely used in the world including Korea. This study investigates the feasibility of photolysis and photocatalysis processes for the degradation of diazinon in water. Both photolysis and photocatalysis reactiosn were effective in degrdading diazinon, however lower TOC removals were achieved. In case of photocatalysis, approximately 40% of nitrogen from diazinon was recovered as NO$_3^-$, and less than 5% of phosphorus as PO$_4{^{3-}}$. However, the sulfur in diazinon molecule was completely recovered to SO$_4{^{2-}}$ from photocatalysis reaction, and the recovery from photolysis was 50%, indicating that P=S bond easily breaks first during photolysis and photocatalysis. The poor recoveries of ionic byproducts and TOC from photolysis and photocatalysis indicate the presence of other organic intermediates during reactions. The formation of organic intermediates were identified during reactions using GC/MS and LC/MS/MS, and the main degradation products were diazoxon, and 2-isopropyl-4-methyl-6-hydroxypyrimidine (IMP), respectively. Finally, the acute 48-hr toxicity test using Daphnia magna were employed to measure the toxicity reduction during photocatalysis of degradation. The results showed that the toxicity increased until 180 min of the photocatalysis reaction (from EC$_{50}$ (%) of 69.6 to 13.2%), however, acute toxicity completely disappeared (>100%) after 360 min. The toxicity results showed that the intermediates from photocatalysis such as diazoxon were more toxic than diazinon itself, however these intermediates can be degraded or mineralized with further reaction.

• Journal of Gastric Cancer
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• v.13 no.3
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• pp.172-178
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• 2013

Purpose: The aims of this study were as follow: 1) to de scribe the expression status of estrogen receptor-${\alpha}$ and -${\beta}$ mRNAs in five gastric carcinoma cell lines; 2) to evaluate in vitro the effects of $17{\beta}$-estradiol and estrogen receptor antagonists on the proliferation of the cell lines. Materials and Methods: Detection of estrogen receptor-${\alpha}$ and estrogen receptor-${\beta}$ mRNA in five human gastric cancer cell lines (AGS, KATO III, MKN28, MKN45 and MKN74) was made by the reverse transcription-polymerase chain reaction system. To evaluate the effect of $17{\beta}$-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell line, the cell lines which expressed both es trogen receptors were chosen and treated with $17{\beta}$-estradiol and estrogen receptor antagonists (methyl-piperidino-pyrazole and pyrazolo [1,5-a] pyrimidine). Cell proliferation was assessed with the methylthiazol tetrazolium test. Results: Estrogen receptor-${\alpha}$ and estrogen receptor-${\beta}$ mRNAs were expressed in three (KATO III, MKN28 and MKN45) and all of the five gastric cancer cell lines, respectively. At higher concentrations, $17{\beta}$-estradiol inhibited cell growth of MKN28, MKN45 and KATO III cell lines. Neither estrogen receptor-${\alpha}$ nor estrogen receptor-${\beta}$ antagonist blocked the anti-proliferative effect of $17{\beta}$-estradiol. Conclusions: Our results indicate that estrogen receptor-${\beta}$ mRNAs are preferentially expressed in gastric cancers and also imply that hormone therapy rather than estrogen receptor blockers may be a useful strategy for the treatment of estrogen receptor-${\beta}$ positive gastric cancer. Its therapeutic significance in gastric cancer are, however, limited until more evidence of the roles of estrogen receptors in the gastric cancer are accumulated.

• BMB Reports
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• v.40 no.6
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• pp.911-920
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• 2007

Tuberculosis, caused by Mycobacterium tuberculosis, continues to be one of the leading infectious diseases to humans. It is urgent to discover novel drug targets for the development of antitubercular agents. The 2-C-methyl-Derythritol-4-phosphate (MEP) pathway for isoprenoid biosynthesis has been considered as an attractive target for the discovery of novel antibiotics for its essentiality in bacteria and absence in mammals. MEP cytidyltransferase (IspD), the third-step enzyme of the pathway, catalyzes MEP and CTP to form 4-diphosphocytidyl-2-C-methylerythritol (CDP-ME) and PPi. In the work, ispD gene from M. tuberculosis H37Rv (MtIspD) was cloned and expressed. With N-terminal fusion of a histidine-tagged sequence, MtIspD could be purified to homogeneity by one-step nickel affinity chromatography. MtIspD exists as a homodimer with an apparent molecular mass of 52 kDa. Enzyme property analysis revealed that MtIspD has high specificity for pyrimidine bases and narrow divalent cation requirements, with maximal activity found in the presence of CTP and $Mg^{2+}$. The turnover number of MtIspD is $3.4 s^{-1}$. The Km for MEP and CTP are 43 and $92{\mu}M$, respectively. Furthermore, MtIspD shows thermal instable above $50^{\circ}C$. Circular dichroism spectra revealed that the alteration of tertiary conformation is closely related with sharp loss of enzyme activity at higher temperature. This study is expected to help better understand the features of IspD and provide useful information for the development of novel antibiotics to treat M. tuberculosis.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1002-1012
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• 2005

5-Substituted 4-oxo-2-thioxo-1,,2,3,4-tetrahydropyrimidine were synthesized by interaction of 4­oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonylhydrazide with some aldehydes to give the corresponding Schiff-bases, which after cyclization gave corresponding thiazolidinones. For some of the thiazolidinones, Mannich bases reaction was carried out. All the derivatives were tested for their possible inhibitory effect on Schistosoma mansoni cercarial elastase (CE). Only, N'-(4-methylbenzyledine)-4-oxo-2-thioxo-1,2 ,3,4-tetrahydropyrimidine-5-sulfonylhydrazide was found to have potent inhibitory effect on the CE activity with $IC_{50} = 264{\mu}M.$ Upon its use as a paint for mice tails before infection with S. mansoni cercariae, the compound formulated in jojoba oil caused a significant reduction ($93\%$; P-value = 0.0002) in the worm burden. IgG & IgM in mice sera were measured by using several S. mansoni antigens by ELISA. Sera from treated infected mice (TIM) 2, 4, and 6 weeks (W) post infection (PI) showed 1.2 folds lower, 1.2 folds higher, 1.7 folds lower IgM reactivity against soluble cercarial antigenic preparation (CAP), respectively, when compared with sera collected from infected untreated mice (IUM). Sera from TIM 2, 4, and 6WPI showed 1.3, 1.6, and 1.7 folds higher IgG reactivity, respectively against CAP than the IgG reactivity from IUM. Sera from TIM 2, 4 and 6WPI showed 1.5, 1.2 folds lower and 1.4 folds higher IgM reactivity, respectively against soluble worm antigenic preparation (SWAP) when compared with sera collected from IUM. Sera from TIM 2, 4, and 6WPI showed 1.4, 1 folds lower and 1 fold higher IgG reactivity, respectivley to SWAP when compared with sera from IUM. Sera from TIM 2, 4, and 6WPI had generaly lower IgM and IgG reactivities against soluble egg antigen (SEA) when compared with sera from IUM.

• Microbiology and Biotechnology Letters
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• v.16 no.6
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• pp.468-475
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• 1988

The cloned B. subtilis cdd gene encoding cytidine/2'deoxycytidine deaminase (EC 3.5.4.5) was expressed in the cdd deficient B. subtilis mutant ED40. The gene was isolted from the cdd complementing plasmid pSO21, and inserted into the EcoR1/Pvu1 sites of pGB215-110 ΔB, which is a temperature sensitivie E. coli-B. subtilis shuttle vector. In the transformed B. subtilis ED4O harboring the resulting plasmid pSO100, cdd was expressed at several hundred fold elevated levels, and the cytidine deaminase activity in E. coli containing pSO100 was twice the level in B. subtilis/pSO0100. The Km value for cytidine of the partially purified enzyme is 1.88$\times$10$^{-4}$M at pH 7.0 and the V$_{max}$ = 11.1 $\mu$mol/min/mg of protein. The enzyme was completely inhibited by 0.1M mercaptoethanol and HgCl$_2$. The inhibition by p-chrolomercurybenzoic acid showed a Ki = 5 uM. These results suggest that sulfhydryl reagents block an active site thiol group, and/or disturb the formation of the tetrameic holoenzyme.

• Korean Journal of Weed Science
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• v.8 no.3
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• pp.237-243
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• 1988

Field study was conducted to evaluate safening effect of fenclorim (4,6-dichloro-2-phenyl pyrimidine) against benthiocarb, butachlor, and pretilachlor injury in rice plants under vinyl-covered subirrigated seedbed. Combinated application of benthiocarb 210, and 315 g ai/10a with fenclorim 10 g ai/10a or higher concentration, butachlor 180, and 270 g ai/10a with fenclorim 20 g ai/10a or higher concentration, and pretilachlor 60, and 90 g ai/10a with fenclorim 30 g ai/10a reduced herbicide injury of rice, and thus increased standing, plant height, tillers, and dry weight of rice plants compared to no combined application of fenclorim.

• Korean Journal of Weed Science
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• v.9 no.3
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• pp.214-220
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• 1989

The experiments were conducted to evaluate safening effect of fenclorim (CGA 123'407, 4,6-dichloro-2-phenyl pyrimidine) against injuries of pretilachlor, butachlor, and benthiocarb in direct-seeded rice under flooded conditions. Pretilachlor and butachlor and benthiocarb reduced crop standing and inhibited growth of rice plants. However, premixture application of pretilachlor, butachlor or benthiocarb with fenclorim at 10-30 g ai/10a greatly reduced rice injury caused by the application of each herbicide alone and thus increased crop standing plant height and dry weight of rice plants compared to herbicide treatments alone.

• Applied Biological Chemistry
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• v.39 no.4
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• pp.297-303
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• 1996

A series of the herbicidal N-(4,6-disubstituted pyrimidin-2-yl)aminocarbonyl-2-(1,1-ethylenedioxy-2-fluoro)ethyIbenzenesulfonamides, 1 and N-(4,6-disubstituted triazin-2-yl)aminocarbonyl-2-(1,1-ethylenodioxy-2-flu ore)ethylbenzenosuIfonamides, 2 were synthesized and their herbicidal activities in-vivo against rice(Oryza sativa L.), barnyard grass (Echinochloa crus-galli), bulrush(Scripus juncoides) and pickerel weed(Monochoria vaginalis presl.) were measured by the pot test under the paddy conditions. The structure activity relationships(SAR) between the herbicidal activity$(pI_{50})$ and a various physicochemical parameters of the hetero group and 4,6-disubstituents on the heterocyclic group were analyzed by the multiple regression technique. The SAR suggest that the 4,6-dimethoxypyrimidine substituent, 1a showed selective$({\Delta}obs.pI_{50}=1.12)$ and the most highest activity against barnyard grass, which depend on the hydrophobicity(log P<0) of heterocyclo group and molecular refractivity$((M_R)_{opt.}=14.58cm^3/mol)$ constant of 4,6-disubstituents on the heterocyclic group.

• Tuberculosis and Respiratory Diseases
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• v.58 no.1
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• pp.83-88
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• 2005

Leflunomide is a new disease modifying anti rheumatic drug (DMARD) for the treatment of active rheumatoid arthritis. Its mechanism of action differs from other DMARDs in that it inhibits the de novo pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase and therefore prevents the proliferation of activated lymphocytes. As it has been prescribed worldwide, there is a great deal of much concerns regarding its potential adverse effects. Because leflunomide has an active metabolite with a long elimination half-life of approximately 2 weeks, serious adverse reactions may occur even after the leflunomide treatment has been stopped. The profile of serious reactions includes liver dysfunction, hematological disorders, severe skin reactions and respiratory dysfunction. Respiratory dysfunctions with leflunomide therapy are very rare and its incidence is lower than that of methotrexate therapy. However, there are reports in Japan showing that 5 patients died of interstitial pneumonitis and another 11 patients developed serious lung complications associated with leflunomide. This suggests the possibility of fatal respiratory toxicity of leflunomide. There are no reports of interstitial pneumonitis associated with leflunomide in Korea. We report a case of a 62-year old woman who developed interstitial pneumonitis, which might have been induced by leflunomide during the treatment of rheumatoid arthritis.

• Korean Journal of Weed Science
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• v.6 no.2
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• pp.134-145
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• 1986

The experiment was crried out to evaluated the herbicidal properties of bensulfuron methyl [methyl 2-[[[[[(4, 6-dimethoxy pyrimidine-2yl) amino] carbonyl] amino] sulfonyl] methyl] benzoate]. No phytotoxicity was observed when bensulfuron methyl was applied at 3 and 6 g a.i./ 10a while the application rate 12 g a.i./10a slightly retared the growth of rice. The phytotoxicity decreased as the application time was delayed. The effect of application rate, leaching grade, transplanting depth, soil type and temperature on crop injury was little. Japonica variety (Dong-Jin) was more sensitive to bensulfuron methyl than indica X japonica variety (Sam-Kang). Bensulfuron methyl controlled effectively perennial weeds such as Sagittaria pygmaea Miq., Potamogeton diatinctus A. Benn., Cyperus serotinus Rottb., Sagittaria trifolia L., Eleocharis kuroguwai Ohwi. including most annual weeds except Echinochloa crus galli P. Beauv. The effect slightly decreased with lowering the temperature increasing the leaching grade. Application time and soil type employed did not affect the weeding effect.