• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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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.

• 한국재료학회:학술대회논문집
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• 한국재료학회 2012년도 춘계학술발표대회
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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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• 제20권2호
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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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• 제23권8호
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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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• 제14권1호
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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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• 제21권8호
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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.

• 한국환경농학회지
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• 제9권1호
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• pp.9-13
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• 1990

수도(水稻)를 재배(栽培)한 실외(室外) 풋트조건(條件)의 담수토양(湛水土壤)에 살충제(殺蟲劑) fenitrothion, 살균제(殺菌劑) IBP, 제초제(除草劑) butachlor 유제(乳劑)를 각각(各各) 100g, 98g, 352.8g ai/10a수준(水準)으로 수면처리(水面處理)하고 답면수(畓面水)(담수액(湛水液)) 및 토양중(土壤中) 3농약(農藥)의 잔류성(殘留性)을 조사하였다. 답면수(畓面水) 중 fenitrothion, IBP, butachlor의 농도(濃度)는 처리(處理) 1시간후에 각각(各各) 3.7, 3.2, 9.1ppm이었다. 그러나 fenitrothion의 농도(濃度)는 처리(處理) 5일(日)후에 0.01ppm이하(以下)였고 IBP와 butachlor의 농도(濃度)는 처리(處理) 20일(日)후에 각각(各各) 0.025와 0.004ppm이었다. Fenitrothion, butachlor, IBP의 답면수(畓面水)중 반감기(半減期)는 각각(各各) 1일(日)이내, 1.7일(日), 3.6일(日)이었다. 답면수(畓面水)로부터 흡착(吸着)된 토양중(土壤中) fenitrothion, IBP, butachlor 농도(濃度)는 토양(土壤) 0-3cm 층위(層位)에서 처리(處理) 후 3일(日)에 각각(各各) 0.05ppm이하(以下), 0.18ppm, 0.39ppm이었다. 그러나 처리(處理) 27일(日)후에 IBP와 butachlor의 검출(檢出) 농도(濃度)가 0-5cm 층위(層位)에서 각각(各各) 0.04, 0.05ppm으로 동일토양(同一土壤)의 실내조건(室內條件)에서보다 월등히 빨리 분해(分解)되었다. 답면수(畓面水) 및 토양중(土壤中) 소실속도(消失速度)는fenitrothion>butachlor>IBP순이었다. 토양층위별(土壤層位別) butachlor의 잔존량(殘存量)은 2cm 이하(以下)에서보다 0-2cm 층위(層位)에서가 현저(顯著)히 많았는데 비(比)하여, IBP의 토양층위별(土壤層位別) 농도(濃度)는 큰 차이(差異)가 없이 5㎝이하(以下)까지 이동(移動)되었다.

• 한국식품위생안전성학회지
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• 제14권4호
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• pp.339-345
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• 1999

Dichlorvos 및 methidathion에 대한 광분해 실험을 수행하여 속도상수와 분해생성물을 측정하였다. 햇빛을 이용한 광분해 실험은 1998년 9월 2일부터 9월 18일 까지 수행하였으며 두가지 농약이 상당기간 동안 안정함을 확인할 수 있었다. 또한 햇빛 아래서는 humic acid의 광관여 효과가 없음을 알 수 있었다. 자외선을 이용한 광분해 실험에서 dichlorvos의 광분해속도상수와 반감기는 각각 0.0208 및 33.3분으로 조사되었고, methidathion의 경우는 각각 0.6189 및 1.0분으로 조사되어 methidathion의 광분해는 4분 이내에 99% 이상의 매우 빠른 분해양상을 보였다. 두가지 농약 모두 3시간 이내에 분해되었고, 따라서 먹는물 정수처리시 농약의 분해가 필요할 때는 자외선을 이용하는 것이 좋을 것으로 생각된다. 또한, dichlorvos 및 methidathion은 자외선을 단독조사 하였을 때 보다 TiO$_2$를 첨가하였을 경우 분해는 다소 빠르게 진행되었다. 광분해에 의한 분해생성물을 확인하고자 GC/MS분석을 한 결과 dichlorvos에서는 분해생성물로 m/z=153의 Ο, Ο-dimethyl phosphate(DMP)를 확인하였다. Methidathion의 경우 분해생성물로 m/z=198 과 m/z=214로 각각 Ο, Ο-dimethyl phosphorothioate(DMTP)와 Ο, Ο-dimethyl phosphorodithioate(DMDTP)를 확인하였다.

• 농약과학회지
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• 제9권1호
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• pp.97-101
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• 2005

피라졸 계통의 유기인계 살충제인 flupyrazofos(O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothioate)의 합성공정에서 생산된 원제 1(95.4%), 원제 2(97.6%) 그리고 정제품(99.2%)에 대한 불순물 조성과 함량을 조사하였으며, 이들 원제 및 정제품을 이용하여 in vitro와 in vivo 상에서 acetylcholinesterase (AChE) 활성 저해 정도를 비교 검정하였다. 실험결과 불순물의 조성은 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 oxon), O,S-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothionate (S-ethyl flupyrazofos)이었으며, 이들 불순물들의 함량이 원제 중에서 전반적으로 높았다. In vitro 상에서 AChE 저해는 불순물들이 많은 원제 1에서 가장 빠르게 저해되었으며, 생쥐 뇌 AChE (in vivo)에 대한 $I_{50}$ 값은 원제 1과 2가 정제품 보다 40% 이상 높았다. 이는 정제품에 비하여 원제 중에 더 많이 함유된 flupyrazofos oxen과 S-methyl flupyrazofos에 의한 영향일 것으로 판단되었다.

• Environmental Analysis Health and Toxicology
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• 제8권1_2호
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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.