• 한국환경농학회지
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• 제12권2호
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• pp.176-183
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• 1993

신규 살충제인 KH-502의 안전성을 조사하기 위하여 다양한 조건하에서 광(光) 분해(分解) 실험을 수행하였다. 이 실험에서 KH-502를 acetone 또는 acetonitrile 용액에 첨가한 뒤 태양광선 또는 자외선 $(300{\sim}350nm)$을 조사(照射)하였고, acetone 또는 acetonitrile 용액에는 수분함량, 산소함량이 달랐으며, 부식산,rosebengal 또는 tryptophan이 첨가 되었다. KH-502의 안전성 및 분해경향에 대한 결과를 요약하면 다음과 같다. 1. KH-502의 광분해(光分解)는 자외선을 조사(照射)한 경우와 그렇치 않은 경우에 매우 유의성있는 차이를 보여 주었다. KH-502는 acetone 용매에서 광관여효과에 의해 광분해(光分解)되었으나, acetonitrile 용매 하(下)에서는 광분해되지 않았다. 2. KH-502의 광분해 경향은 열 분해 경향과 판이하게 달랐으며, 광분해산물은 KH-502 oxo형, S-ethyl KH-502, PTMHP 및 몇가지 미지물질 등이었다. 3. acetone 또는 acetonitrile에 첨가된 부식산, rosebengal, tryptophan은 KH-502의 광분해에 광관여효과를 나타내지 않았다. acetone 용매의 용존산소는 acetone과 함께 경쟁적으로 광관여효과를 나타내어 KH-502의 분해를 촉진시켰다. 4. acetone 용매를 부식산 또는 논물로 처리했을때, KH-502의 광분해는 감소하였다.

• 한국환경농학회지
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• 제16권1호
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• pp.72-79
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• 1997

신규 활성물질인 Flupyrazofos(KH-502)의 토양에서의 흡착성, 용탈성 및 잔류성을 실내조건과 포장조건하에서 연구하여 본 공시약제의 안전사용을 위한 기초자료를 제공하고 토양-수질환경에 미칠 영향을 예측 평가하기 위한 목적으로 수행한 연구결과는 다음과 같다. 1. Flupyrazofos의 흡착량과 시간과의 사이에는 유의성있는 power function 관계가 있어서, 흡착이 빨리 일어나서 반응 30분 후에 45%가 흡착되고, $6{\sim}12$시간 이후에는 의사(疑似)평형에 도달했다. 2. Flupyrazofos의 흡착은 First-order kinetic model에 유의성있게 따랐고, 가해준 Flupyrazofos의 50%가 흡착되는 시간은 사양토의 경우 5.8시간이었다. 3. Flupyrazofos의 농도에 따른 흡착양상은 Freundlich 등온식으로 설명될 수 있었고, 등온식은 S-형(型)으로 분류될 수 있었다. 4. 토양 column을 통해 용탈된 Flupyrazofos의 농도는 가해준 농도에 비해 매우 낮았다. 용탈된 Flupyrazofos의 농도는 사양토가 식양토보다 약간 높았다. 사양토(砂壤土)에서 용탈된 최대 $C/C_0$ 값이 0.073, 식양토(埴壤土)에서는 0.017에 불과했다. 5. 표토에서 Flupyrazofos의 잔류량은 낮은편이며 시간이 경과할 수록 현저히 감소했다. 반감기는 사양토의 경우 20일, 식양토는 18일이었다. 심토로 이동${\cdot}$잔류된 농도는 매우 낮았다. 6. Flupyrazofos의 흡착시험, 용탈시험, 포장시험 결과와 약제의 물리화학적 특성을 근거로 판단할 때 공시농약은 토양에서 잘 흡착되고 이동${\cdot}$잔류성이 낮기 때문에, 상용농도를 시용할 경우 주변 환경에 미칠 수 있는 위해성은 낮은 것으로 판단된다.

• 한국환경농학회지
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• 제11권3호
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• pp.225-234
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• 1992

Thermal decomposition was conducted to investigate the influence of the various factors on stability of a new insecticide, [O, O-Diethyl O-(1-phenyl-3-trifluoromethyl-5-pyrazoyl) thiophosphoric acid ester : KH-502], in view of those informations applicable for industrial exploitation. In the thermal decomposition experiment, KH-502 was, after mixing with Fe, Cu and adjustment of moisture and pH conditions, subjected to three temperatures, 25, 50, and $100^{\circ}C$. Results for stability, and degradation pattern of KH-502 from the above experiment can be summarized as follows: 1. Main products of the thermal decomposition when this was conducted in the closed system were identified as following five compounds:O, O, O-Triethylthiophosphoric acid(TEPA), 1-Phenyl-3-trifluoromethyl-5-ethoxypyrazole(PTMEP), 1-Phenyl-2-ethyl-3-trifluoromethyl-5-hydroxypyrazole(PETMHP), O, O-Diethyl O-(1-phenyl-3-trifluoromethyl-5-pyrazoyl)phosphoric acid ester(KH-502 oxo form), O, S-Diethyl O-(1-phenyl-3-trifluoromethyl-5-pyrazoyl)phospho rothiolate(S-ethyl KH-502). However, compounds such as oxo form and S-ethyl KH-502 were not identified when the thermal decomposition was proceeded in the open system. 2. KH-502 was stable at 25 and 50$^{\circ}C$, but it was decomposed at 100$^{\circ}C$ following the first-order kinetics at the early stages of decomposition. 3. Rate constants for the thermal decomposition of KH-502 at 100$^{\circ}C$ were in the orders of Cu powder addition 0.344>Cu plate addition 0.21>moisture addition 0.05>closed system=open system=iron addition=pH 5.5 adjustment 0.04>pH 8.5 adjustment 0.027 day$^{-1}$, representing KH-502 was decomposed fast at Cu powder treatment and slow at pH 8.5 adjustment. 4. Half-life for the thermal decomposition of KH-502 at 100$^{\circ}C$ was in the orders of Cu powder addition 2.02

• Toxicological Research
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• 제14권2호
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• pp.227-235
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• 1998

KH-502 (Flupyrazofos), a new organophosphorus insecticide synthesized by Korea Re-search Institute of Chemical Technology, was found to be effective against diamond-back moth(Plutella xylostella). This study was carried out to determine the acute toxicity of KH-502 in Sprague-Dawley rats and ICR mice. The test article was orally or dermally administered to the animals. Death, tremors, salivation, lacrimation, abnormal gait and corneal opacity were observed. Decrease in body weight gain was observed in all treatment groups. At necropsy, dark red coloration of lung, enlargement of adrenal glands and atrophy of spleen were observed. The oral $LD_{50}$ value was 372 mg/kg in male rats, 605 mg/kg in female rats, 186 mg/kg in male mice, and 115 mg/kg in female mice. And the dermal $LD_{50}$ was 4086 mg/kg in male and 3881 mg/kg in female rats.

• Toxicological Research
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• 제13권4호
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• pp.317-322
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• 1997

Acute delayed neurotoxicity of KH-502 [O.O-Diethyl O-(1-phenyyl-3-trifluoromethyl-5-pyrazoyl) thiophosphoric acid ester], an insecticide synthesized newly in Korea, was studied in White Leghorn hens. The doses were determined on the basis of preliminary $LD_{50}$ study. High, middle and low doses were determined to be 1123 mg/kg, 762 mg/kg and 518 mg/kg, respectively. The animals were pretreated with atropine (30 mg/kg) prior to administration of KH-502. The chemical was administrated at the first and 21st day of the study. As positive controls, animals were admlnistrated with triorthocresylphosphate (TOCP 1000 mg/kg and 500 mg/kg). Animals administrated with TOCP or KH-502 were sacrificed by perfusion-fixation at 21st and 42nd day of the study, respectively. The central and peripheral nerve tissues were routinely treated for microscopic observation. As results, eight, three, one, and one chickens died within 2 day after adminiatration with signs of cholinergic acute toxicity in high, middle low and TOCP dose-group (500 mg/kg), respectively. No abnormal clinical signs were observed in the survived chickens administrated with KH-502 in the duration of the study. The chickens in positive control groups showed ataxia and incoordination at the 14th day after administration of TOCP. From necropsy, macroscopic changes were not observed in all groups including positive control groups. Histopathologically, oxonal swelling with myelin loss, focal gliosis, distention around axonal space were observed in the spinal cords of the chickens administrated with TOCP 1000 mg/kg. The lesions were distinct in the dorsal and lateral funiculi of cervical spinal cord, in the lateral and ventral funiculi of thoracic spinal cord and in ventral funiculi of lumbosacral spinal cord. Axonal swelling and mlcrogliosis were infrequently observed in the chickens of other groups including negative control one. However, they were nonspecifically distributed in the spinal cords. In this study, we concluded that the new chemical, KH-502 did not have acute delayed neurotoxicity in White Leghorn hens.

• 농약과학회지
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• 제8권3호
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• pp.162-167
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• 2004

십자화과 식물을 가해하는 세계적으로 중요한 해충의 하나인 배추좀나방(diamondback moth, Plutella xylostella)을 방제를 하기위하여 개발된 새로운 형태의 thiophosphoryl pyrazole계 살충제 KH502 유도체들의 구조와 살충활성을 CoMFA 방법으로 조사한 결과 효소의 결합부위에서 가장 중요한 역할을 하는 작용기는 trifluoro-methyl group과 thiophosphoryl group으로 밝혀졌다. 이와 같은 3D-QSAR 분석결과는 새로운 배추좀나방 방제용 살충제를 설계하는데 유용한 정보로 이용할 수 있을 것이다.

• 농약정보
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• 제19권2호통권143호
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• pp.26-29
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• 1998

• Applied Biological Chemistry
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• 제40권1호
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• pp.76-79
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• 1997

국내에서 최초로 합성, 개발된 유기인계 살충제인 flupyrazofos(KH-502)의 물리화학적 특성으로 수용성, 가수분해, 증기압, 분배계수를 EPA와 OECD 방법에 준하여 측정하였다. 수용성은 $25^{\circ}C$에서 0.80 ppm으로 낮았고 가수분해 반감기는 $25^{\circ}C$에서 266.5시간(pH 4.0), 180.0시간(pH 7.0), 120.9시간(pH 9.0)으로 알칼리 조건에서 불안정하였으며 $40^{\circ}C$에서는 $25^{\circ}C$보다 $2{\sim}4$배 정도 가수분해가 빠르게 진행되었다. 상은($25^{\circ}C$)에서의 증기압은 $2.81{\times}10^{-5}$ torr로 측정되었고, 다른 두 온도(35, $45^{\circ}C$)에서 증기압을 측정하여 log P=0.673-(1565.4/T)라는 관계식을 구하였다. Flupyrazofos의 상온($25^{\circ}C$)에서의 증기압은 diazinon과 유사한 수준이었고, DDVP보다는 약 1,000배 정도 낮은 수치로 휘발에 의하여 환경에 영향을 미칠 가능성은 낮을 것으로 판단되었다. Flupyrazofos의 옥탄올/물 분배계수치를 보면(log Kow=5.24) 먹이연쇄를 통한 생물농축이 예상되나 비교적 가수분해가 빠르기 때문에 비록 수계에 노출된다고 하여도 그 가능성은 매우 낮을 것으로 사료된다.

• Archives of Pharmacal Research
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• 제21권5호
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• pp.496-502
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• 1998

The present study was carried out to determine the possible use of cTn-I in the cardiac myofibrillar architecture, as a potential target for in vivo radioimmunodetection of cardiac damage in a brain death pig model. Radioiodiantion of the anti-cTn-I 5F4 McAb was carried out by lactoperoxidase method. the percentage iodine incorporation achieved was 70-75%. The radioiodinated McAbs were purified on Sephadex G-25 column and characterised by Paper chromatography, Phast Gel electrophoresis and electroimmunoblotting. Radioiodinated anticTn-I 5F4 McAbs were employed alongside Pyrophosphate($Tc_{99m}$-PPi$) and $Thallium^{201}$ chloride($TI^{201}$) in 24 landrace pigs (brain-dead=18 & sham-operated=6). The percentage cardiac uptake of the radiolabelled antibody injected dose was significantly higher in the brain dead animals(0.196%) as compared to that of sham-operated animals (0.11%). Specific in vivo localization of radiolabelled McAbs in the infarcted cardiac tissue was confirmed by computer-aided reconstruction of 3-D images of the isolated heart. The preliminary results of the study revealed preferential uptake of radiolabelled antibody at the site of myocyte damage resulting from artificially induced brain death.

• Journal of Microbiology and Biotechnology
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• 제25권4호
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• pp.496-502
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• 2015

Polyketide secondary metabolites share common precursor pools, acyl-CoA. Thus, the effects of engineering strategies for heterologous and native secondary metabolite production are often determined by the measurement of pikromycin in Streptomyces venezuelae. It is hard to compare the effectiveness of engineering targets among published data owing to the different pikromycin production media used from one study to the other. To determine the most important nutritional factor and establish optimal culture conditions, medium optimization of pikromycin from Streptomyces venezuelae ATCC 15439 was studied with a statistical method, Plackett-Burman design. Nine variables (glucose, sucrose, peptone, (NH₄)₂SO₄, K₂HPO₄, KH₂PO₄, NaCl, MgSO₄·7H₂O, and CaCO₃) were analyzed for their effects on a response, pikromycin. Glucose, K₂HPO₄, and CaCO₃ were determined to be the most significant factors. The path of the steepest ascent and response surface methodology about the three selected components were performed to study interactions among the three factors, and the fine-tune concentrations for maximized product yields. The significant variables and optimal concentrations were 139 g/1 sucrose, 5.29 g/l K₂HPO₄, and 0.081 g/l CaCO₃, with the maximal pikromycin yield of 35.5 mg/l. Increases of the antibiotics production by 1.45-fold, 1.3-fold, and 1.98-fold, compared with unoptimized medium and two other pikromycin production media SCM and SGGP, respectively, were achieved.