• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.129-129
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• 1995

ASPS against TGF-${\beta}$ is developing as scar formation inhibitor. The scar was caused by undesired collagen deposition due to overexpression of TGF-${\beta}$ in wounded tissue. The in vitro percutaneous absorption of ASPS(25mer)was investigated by using Furanz Diffusion Cell. The flux of ASPS cannot be found through normal skin due to high molecular weight (MW 10,000) and polyanionic charge. However, the skin permeation of ASPS through tape-stripped damaged skin was markedly increased. The skin fluxs of ASPS were decreased in the following order; hairless mouse> rat >human cadaver skin.

• Proceedings of the Materials Research Society of Korea Conference
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• 2012.05a
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• pp.55.1-55.1
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• 2012

In the first part of this talk, I will introduce an effort to use gold nanoparticles and UO22+ (uranyl) specific DNAzyme for development of highly sensitive and selective colorimetric uranyl sensors. In addition, I will discuss how DNA aptamers can be delivered by nanoparticles to cancer cell nucleus and released by ultrafast femtosecond pulsed laser for targeted cancer therapy. Finally, I will show how proteins such as streptavidin and myoglobin, or nanoparticles can be precisely aligned on DNA with nanometer resolution via backbone-modified phosphorothioate DNA and bifunctional linkers. These interesting functional and structural properties of DNA can provide new opportunities to develop dynamic DNA structures for potential use as intracellular sensors and drug delivery agents.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.115-121
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• 1997

Ile-269 in horse liver alcohol dehydrogenase isoenzyme S(HLADH-S) was mutated to serine by phosphorothioate-based site-directed mutagenesis in order to study the role of the residue in coenzyme binding. The specific activity of the mutant(1269S) enzyme to ethanol was increased 49-fold. All turnover numbers of 1269S enzyme toward 9 primary alcohols were increased. The mutant enzyme showed 3.6, 4.6, 11.6-fold higher catalytic efficiency for $5{\beta}$-androstane-3, 17-dione, $5{\beta}$-cholanic acid-3-one and retinal than wild-type, respectively. The reaction mechanism of 1269S enzyme was ordered bi bi as wild-type's. These results indicate that the hydrophobic interaction of Ile-269 residue with coenzyme plays an important role in dissociation of coenzyme from enzyme-coenzyme complex, which has been known as the rate limiting step of ADH reaction.

• Bulletin of the Korean Chemical Society
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• v.23 no.8
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• pp.1116-1119
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• 2002

Monoclonal antibodies have been generated against a generic hapten, ο,ο-diethyl ο-(5-carboxy-2-fluorophenyl) phosphorothioate, for the determination of organophosphorus (OP) pesticides in a class-specific manner. In an indirect competitive enzyme-linked immunosorbent assay (ELISA) format, employing a heterologous coating antigen, these monoclonal antibodies showed desirable properties for use in the class-specific determination, i.e., broad specificity and high sensitivity. The IC50 values of four commonly used ο,ο-diethyl OP pesticides were fairly uniform ranging from 0.1 to 0.3 ㎛/mL. The IC50 values of three ο,ο-dimethyl derivatives were between 0.3 and 1.4 ㎛/mL. These values, together with the limits of detection (LOD), were better, in terms of the specificity and sensitivity, compared with the values obtained previously with polyclonal antibodies.

• Bulletin of the Korean Chemical Society
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• v.14 no.1
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• pp.52-55
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• 1993

A procedure is described for the synthesis of the title compound via phosphotriester intermediates. The preparation of $R_p\;and\;S_p$ diastereomeric dinucleotide of d[Ap(S)A] was performed by the condensation of protected deoxyadenosine, 2,5-dichlorophenylphosphorodichloridothioate and 1-hydroxybenzotriazole in THF. Their designation of configuration at phosphorus as $R_p\;and\;S_p$ follows from analysis of $^{31}P$-NMR spectroscopy and reversed-phase HPLC and the stereospecificity in the hydrolysis catalyzed by nuclease Pl.

• Bulletin of the Korean Chemical Society
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• v.21 no.8
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• pp.785-792
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• 2000

Mass spectral fragmentations of six chlorinated organophosphorus pesticides were investigated using electron impact mass spectrometry. Understanding the fragmentation pathways, based on the fragment ions of mass spectra, should be useful in the structural elucidation and chemical identification of these compounds. The pro-posed fragmentation pathways were verified by collision-induced dissociation B/E-linked scan spectra. ln most cases,the structures of characteristic fragment ions could be expected by the observation of the peak clusters due to 35Cl and 37Cl isotopes. According to substituted groups on phosphorus atom, phosphate and phospho-rothioate exhibited significantIy differentfragmentation patterns. Especially, phosphate and phosphorothioate with diethyl ester produced more diverse fragment ions than that with dimethyl ester.

• Korean Journal of Environmental Agriculture
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• v.9 no.1
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• pp.9-13
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• 1990

The dissipation of insecticide fenitrothion(O,O-dimethyl O-4-nitro-m-tolyl phosphorothioate), fungicide IBP(S-benzyl O, O-diisopropyl phosphorothioate), and herbicide butachlor(N-butozymethyl-2-chloro-2', 6'-diethylacetanilide) in flooded soil planted with rice plants was investigated in outdoor pot conditions. The half lives of IBP, butachlor and fenitrothion in the flooding water treated with IBP at 98g, butachlor at 352.8g, and fenitrothion at 100g ai/10a, were 3.6, 1.7 and within 1 day, respectively. The concentration of fenitrothion at 5 days after application was found to be less than 0.0lppm. In the case of IBP and butachlor after 20 days, the concentration was 0.025 and 0.004ppm, respectively. The concentration of fenitrothion, IBP, butachlor in a soil depth of 0-3cm was 0.07, 1.45 and 3.37ppm on the 3rd day after application, and below 0.05, 0.18, 0.39ppm after 7 days, respectively. However, 27 days after application concentration of IBP and butachlor at 0-5cm soil depth resulted in 0.04 and 0.05ppm, respectively. The disappearance of pesticides was remarkably rapid, compared to those in the some soil under the laboratory conditions. Differences in the concentration of IBP in different soil profiles were few, but amounts of butachlor were remarkably higher at 0-2cm soil depth than below 2cm soil depth.

• Journal of Food Hygiene and Safety
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• v.14 no.4
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• pp.339-345
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• 1999

The present study was performed to investigate photodegradation rate constants and degradation products of dichlorvos and methidathion by the USEPA method. The two pesticides were very stable in sunlight for 16 days from September 2 to 18, 1998 and humic acid had no sensitizing effect on the photolysis of each pesticide in sunlight. The photolysis rate was fast-est for methidathion, followed by dichlorvos in the presence of UV irradiation. Photodegradation rate constant and half-life of dichlorvos were 0.0208 and 33.3 min, respectively. Photodegradation rate constant and half-life of methidathion were 0.6789 and 1.0min, respectively. The two pesticides were degraded completely in the presence of UV irradiation and UV irradiation with TiO$_2$in about 3 hours. Therefore, it is suggested that UV treatment will be effective for the degradation of pesticides in the process of drinking water purification. In case of dichlorvos and methidathion, UV irradiation with TiO$_2$was more effective for degradation than W irradiation. In order to identify photolysis products, the extracts of degradation products were analyzed by GC/ MS. The mass spectrum of photolysis products of dichlorvos was at m/z 153, those of the photolysis of methidathion were at m/z 198 and 214, respectively. Photolysis products of dichlorvos was Ο, Ο-dimethyl phosphate(DMP), those of methidathion were Ο, Ο-dimethyl phosphorothioate(DMTP) and Ο, Ο-dimethyl phosphorodithioate (DMDTP).

• The Korean Journal of Pesticide Science
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• v.9 no.1
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• pp.97-101
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• 2005

Flupyrazofos (O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothioate) is an organophosphorus insecticide with a pyrazole moiety which is newly developed and commercialized by SUNGBO chemical company and Korean Research Institute of Chemical Technology for effectively control against diamond back moth. This study was conducted to determine the composition and quantity of impurities in technical 1 (94.5%), technical 2 (97.6%) and purified (99.2%) flupyrazofos using GLC/MSD. Bimolecular inhibition rate constant($k_i$) with acethylcholinesterase (in vitro) and $I_{50}$ with mouse brain acetylcholinesterase (in vivo) were measured for comparing inhibitory patterns of two technicals and purified flupyrazofos. Impurities of flupyrazofos were identified as O,O,O-triethylthio-phosphoric acid (TEA), 1-phenyl-3-trifluoromethyl-5-ethoxy pyrazole(PTMEP), O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphoric acid ester(flupyrazofos oxen), O,S-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothionate (S-ethyl flupyrazofos). In in vitro, technical 1 showed the fastest inhibition on AChE activity among them. And technical 1 and 2 showed 40% higher in vivo inhibition against mouse brian AChE than purified flupyrazofos did. These results could be caused by the impurities such as flupyrazofos oxen and S-methyl flupyrazofos contained in technical grades of flupyrazofos.

• Environmental Analysis Health and Toxicology
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• v.8 no.1_2
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• pp.19-29
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• 1993

The toxicity and histopathologic changes of diazinon (O, O-diethy-O-(2-isopropyl-6-methyl-4-pyrimidinyl)phosphorothioate) was investigated in rat. Rat was treated with diazinon (100 mg/kg/day) by oral administration for 12 days. The experimental results were summarized as follows. Biochemical parameters such as ALT, AST, LDH and glucose in serum were significantly increased and hematological parameters such as Hb, Hct and PLT in blood were slightly increased in treated groups. Also the activities of serum cholinesterase were very significantly decreased in treated groups. In the histopathological changes, the normal lobular architectural pattern of the liver was well preserved in all treated groups. However, vacuolation or fatty change were represent in hepatocytes. Sections of liver from rats treated with diazinon for 3 and 6 days contained slight lipid infiltration in the form of small droplets randomly distributed that were graded minimal (＋) or moderate (＋＋) compared with the respective control condition. After 9 days, there were numerous small and large vacuoles in the terminal hepatic venule and perilobular areas of many serial sections of these rats indicative of fatty infiltration which were graded moderate (＋＋) and severe (＋＋＋). After 12 days, fatty infiltration progressed periportal tract areas and graded severe (＋＋＋) and very severe (＋＋＋＋) in experimental groups. Note absence of cellular necrosis or inflammation.