• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1609-1614
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• 2010

Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10 ${\mu}M$). Results were compared to established reactivators pralidoxime, methoxime, HI-6, trimedoxime and obidoxime. More than 30 novel reactivators performed equal or better reactivation ability of POX-inhibited AChE compared to currently used reactivators. The structure-activity relationship for reactivators of paraoxon-inhibited AChE was developed.

• 한국응용곤충학회지
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• 제32권4호
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• pp.373-381
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• 1993

Resistance evolution to organophosphate-based pesticides in apple and pear inhabiting arthropods of western North America extends to many classes of pest and some beneficial species. Resistance management programs to minimize resistance in pests while exploiting it in natural enemies have met with mixed success. Among beneficials, resistances have been exploited mostly among predators of pest mites. Evolution of resistant mites, leafminers, leafhopper, aphids, leafrollers and some internal fruit feeders have led to development of new monitoring methods and means to delay or avoid resistance. But it is resistance to azinphosmethyl in codling moth (Cydia pomonella) that is changing the pest control system and moving it from chemical to biologically-based means. Newly merging IPM system will depend more on use of biological, cultural, behavior and genetic controls. But more selective pesticides also will be needed to augment pheromones, resistant host plants and genetically altered organisms. These more biologically-based tactics will be prone to resistance evolution in pests as well, if used too unilaterally and/or too extensively.

• 생명과학회지
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• 제10권2호
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• pp.164-168
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• 2000

To understand the biological characteristics of Corythucha ciliata occurring in Korea, developmental periods and its susceptibility to several insecticides were examined under growth chamber condition at $25^{\circ}C$. It took 11.1 day from egg to hatch. And duration of each stage up to the 5th nymph after hatching was 4.0, 2.1, 2.0, 2.9, and 4.0 days, respectively. Total duration from egg to adult was 26.1 days, preoviposition period was 12.2 days, and average number of eggs laid by a female was 83.0. Sex ratio of female was 51.6% and lifespan of female adult was 43.2% days. LC50 value of deltamethrin and esfenvalerate were 0.8 and 0.9 ppm, respectively. Insecticidal effects were better in pyrethroids than organophosphates and carbamates.

• Journal of Applied Biological Chemistry
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• 제61권4호
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• pp.411-416
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• 2018

Chlorpyrifos (CPF) is one of the most heavily used organophosphate pesticides and is useful as an insecticide drug. However, CPF also causes toxic effects in nontarget organisms, including humans and animals. Jageum-Jung (JGJ) is a traditional oriental medicine, composed of five specific herbs with antioxidant and hepatoprotective properties, used for detoxification. In the present study, highly concentrated CPF was orally administrated to male Institute of Cancer Research mice to produce acute toxicity, and the protective effects of JGJ administration were investigated through statistical analysis of changes in body and organ weights and serum biochemical parameters. JGJ caused body and organ weights to recover and reduced the levels of serum biochemical parameters indicative of liver damage, such as glutamic oxalate transaminase, glutamic pyruvate transaminase, alkaline phosphatase, lactic dehydrogenase, urea, glucose, total cholesterol, and triglyceride, that had been increased by CPF treatment. Our results demonstrated that JGJ ameliorates the effects of acute chlorpyrifos-induced toxicity. Therefore, JGJ has the potential to be used as a traditional medicine to alleviate insecticide toxicity.

• Applied Biological Chemistry
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• 제44권3호
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• pp.148-152
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• 2001

본 연구에서는 유기인제에 의한 뇌 손상유발에 있어서 흥분성 아미노산계의 역할을 규명하고자 하였다. Djisopropylfluorophosphate(DFP)를 투여하여 뇌 손상을 유발한 흰쥐에 있어서, 뇌 해마부위에서의 aspartate 및 glutamate의 농도를 측정함으로써 경련유발에 따른 신경전달계의 변화와, 이에 따른 신경조직의 변화를 관찰하였다. 치료약물로 항콜린 약물인 atropine과 NMDA 수용체 길항제인 procyclidine을 각각 단독 또는 병합 투여하여 DFP에 의한 뇌신경독성에 대한 방어효과를 관찰하였다. DFP를 투여한 흰쥐는 경련유발과 더불어 해마부위 에서의 현저한 aspartate와 glutamate의 농도 증가를 보였으며, 병리조직학적으로 해마의 신경세포 감소를 보였다. DFP에 의하여 상승되어진 해마부위의 aspartate와 glutamate의 수준은 procyclidine에 의하여 현저히 억제 되었으나, atropine에 의하여는 DFP 투여군과 유의한 차이를 보이지 않았다. Procyclidine과 atropine 병합 투여 시에는 procyclidine 단독 투여시와 동일한 효과를 관찰할 수 있었다. 조직염색소견에서도 DFP에 의하여 현저하게 소실되어진 신경세포는 atropine 단독 투여시보다 procyclidine 단독 투여군 또는 atrpopine과 procyclidine 병합 투여군에서 뚜렷한 신경세포의 손상 및 소실을 방어하는 것을 관찰할 수 있었다. 따라서 DFP에 의하여 유발된 경련은 흥분성 아미노산 신경전달계를 활성화시키고 이에 따라 뇌신경의 손상이 유발되는 것으로 생각된다. 특히 procyclidine은 DEP에 의한 경련유발과 뇌 세포손상을 효과적으로 방어할 수 있었으며, 이는 흥분성 아미노산계 중 NHDA수용체가 DFP에 의한 뇌 손상기전에 관여됨을 시사한다. 이상의 결과로 DFP에 의하여 유발된 경련은 일차적으로 콜린성 신경계를 과도하게 자극하여 이에 따른 흥분성 아미노산의 과도한 분비를 유발하고 특히 NMDA 수용체를 활성화하여 뇌의 손상을 가져온다고 사료된다.

• 농촌의학ㆍ지역보건
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• 제23권2호
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• pp.305-310
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• 1998

배경 : 농약의 사용이 보편화되면서 점차 그 사용량이 증가되고 있다. 저자들은 농한기의 농업인을 대상으로 국내에서 가장 많이 사용되는 맹독성 농약인 methyl bromide와 organophosphate compound의 농업인 체내 잔류 정도를 혈청 bromide 농도와 cholinesterase 활성도도 측정을 통해 조사하고자 하였다. 방법 : 농한기에 경상남도 산청군과 하동군에 거주하는 121명의 농업인을 대상으로 농번기의 농약사용에 관한 설문조사와 농약의 잔류정도를 측정하기 위한 혈액을 채취하였다. 대조군으로는 간 기능이 정상이며 B형 간염 항원이 없는 사람 중에서 연령과 성별에 맞게 무작위로 240명을 선별하였다. 농업인과 대조군에서 혈중 bromide는 혈청을 이용하여 gold chloride방법으로 구하고, cholinesterase는 colorimetric assay로 측정하였다. 대상 농업인중에서 간기능 검사가 이상 소견을 보이거나 B형 간염 항원 양성인 33명과 이에 해당하는 대조군 65명은 비교대상에서 제외하였다. 결과 : 정상인 240명을 대상으로 산정한 혈청 bromide 농도의 참고치는 72.9 ug/mL이하, 혈청 cholinesterase 활성도의 참고치는 1.6-15.9 U/mL 이었다. 정상인 175명의 혈청 bromide 농도는 $29.8{\pm}22.5\;{\mu}g/mL$, 혈청 cholinesterase 활성도는 $8.7{\pm}3.6$ U/mL이었다. 농업인의 혈청 bromide 농도는 $31.7{\pm}18.0\;{\mu}g/mL$로 대조군과 차이를 보이지 않았고, 혈청 cholinesterase도는 $10.9{\pm}4.2$ U/mL로 대조군에 비하여 유의하게 높았다. 농업인을 경작 면적, 농약 사용시 장갑 및 마스크 착용 유무에 따라 분휴류여 비교해 본 결과, 혈청 bromide 농도나 혈청 cholinesterase 활성도 차이가 없었다. 결론 : 농한기 농업이과 정상인을 비교해 보았을 때 methyl bromide 중독시 증가하는 혈청 bromide 농도는 차이가 없었으며, organophosphate compound 중독시 감소되는 cholinesterase는 농한기 농업인에서 대조군보다 높은 값을 보였다. 따라서 혈청 bromide 농도와 cholinesterase 활성도는 농한기 농업인에서 농약의 체내잔류 지표로 유용성이 낮다고 사료된다.

• 대한임상독성학회지
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• 제6권1호
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• pp.9-15
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• 2008

Purpose: Dichlorvos has been in widespread use as an organophosphate (OP) insecticide compound. The purpose of this study was to access the epidemiology and clinical features of dichlorvos in Korea. Methods: This was a 38 multi-center prospective study of dichlorvos poisoning using surveys, a structural reporting system and review of hospital records from August 2005 to July 2006. A total of 54 patients with acute dichlorvos poisoning on a national basis were enrolled. We analyzed the epidemiologic characteristics and clinical manifestations of dichlorvos poisoning. In addition, the clinical features of dichlorvos poisoning were compared with others OP compounds. Results: During the study period, compounds involving pure OP poisoning were dichlorvos (22.7%), methidathion (8.4%), and phosphamidon (6.7%). In acute dichlorvos poisoning, all ingestion routes were oral. Intentional poisoning involved 74.1% of cases. The common initial complaints involved gastrointestinal (64.8%), systemic (61.1%), central or peripheral nervous system (53.7%), and respiratory symptoms (50.0%). The median arrival time to hospital after dichlorvos poisoning was 2.6 hours and mean hospitalization duration was 7.1 days. 2-PAM was administered in 35 patients in mean doses of 6.3 g/day intravenously. Atropine was administered in 30 patients with a mean dose of 62.8 mg/day (maximal 240 mg/day). Overall mortality rate for dichlorvos poisonings were 14.8% (8/54). Immediate causes for death included sudden cardiac arrest or ventricular dysrhythmias (50%), multi-organ failure (25%), acute renal failure (12.5%), and unknown causes (12.5%). Conclusion: When compared to previous reports, dichlorvos poisoning displayed relatively moderate severity. The presence of a lower GCS score, altered mental status, serious dysrhythmias, systemic shock, acute renal failure, and respiratory complications upon presentation were associated with a more serious and fatal poisoning.

• 대한치과보철학회지
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• 제36권1호
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• pp.26-49
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• 1998

The purpose of this study was to confirm the formation of hybrid layer and resin tags in dentin tissue and the possibility of bonding between luting cements used for the prosthesis and the resinous surface coated with resin bonding agents to prevent the dentin hypersensitivity after abutment preparation. Some resin bonding agents, which may have the possibility of bonding with polyacrylic acid as a liquid ingredient of polycarboxylate and glass ionomer cements, were selected. All-Blond desensitizer containing NTG-GMA and BPDM, Scotch-Bond Multipurpose plus containing HEMA, and XR-bond containing organophosphate were selected as a coating agent. Dental cements were zinc phosphate, polycarboxylate, and glass ionomer cement. After the exposed dentin surface of premolars was ethced with 10% phosphoric acid and coated with resin bonding agents, the morphology of treated surfaces and the resin tags and hybrid layers on sectioned surfaces were observed by SEM. Shear bond strength between the resin bonding agents and 3 kinds of cements was measured 24 hours after bonding. On the debonded surfaces of the shear bond strength tested specimens, the cement tags and the bonding sites between the resin materials and cements were examined by SEM. Following conclusions were drawn : 1. Coating of dentin with resin bonding agents had no effect on the shear bond strength of zinc phosphate cement. 2. Both of polycarboxylate and glass ionomer cements showed the increased shear bond strength by the dentinal coating with Scotch-Bond Multipurpose plus containing HEMA. However, in the case of dentinal coating with some agents containing NTG-GMA and BPDM or organophosphate, polycarboxylate cement exhibited the lowered shear bond strength, and glass ionomer cement showed the unchanged shear bond strength. 3. Complete obstructions of dentinal tubules were observed on the dentin coated with All-Bond desensitizer or XR-bond, but distinct shape of the orifices of dentinal tubules was observed consistently on the dentin coated with Scotch-Bond Multipurpose plus. 4. The hybrid layer was thickest on the dentin coated with All-Bond desensitizer, and the length of resin tags was longest on the dentin coated with Scotch-Bond Multipurpose plus. 3. On the debonded specimens which had been bonded with polycarboxylate cement or glass ionomer cement after coating with Scotch-Bond Multipurpose plus, the cement tags and the bonding sites between the resinous surface and the cements could be examined.

• Biomolecules & Therapeutics
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• 제9권1호
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• pp.33-39
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• 2001

Antidotal efficacy of combinational prophylactics composed of physostigmine plus procyclidine, alone or in combination with antidotes such as atropine plus 2-pralidoxime or atropine plus HI-6, was evaluated in rats. Physostigmine (0.1 mg/kg) plus procyclidine (3 mg/kg), pretreated subcutaneously 30 min prior to subcutaneous exposure to organophosphates of militarily importance, exerted protection ratios of 7.2, 6.5, 4.0, 2.9 and 8.0 fold for tabun, saris, soman, cyclosarin and V-agent, respectively. In comparison, low effects (1.7 fold for soman and 1.3 fold for cyclosarin) were achieved with the traditional antidotes atropine (17.4 mg/kg) plus 2-pralidoxime (30 mg/kg) administered intramuscularly immediately after organophosphate, in contrast to high effects (5.5 fold for soman and 160.0 fold for cyclosarin) with atropine (17.4 mg/kg) plus HI-6 (125 mg/kg), although the protection ratio markedly decreased when treatment of antidotes was delayed. Note- worthy, the combinational prophylactics markedly potentiated the effects of antidotes to higher than 5.0 fold in all cases. In addition, the combinational prophylactics fully prevented the seizures and excitotoxic brain injuries induced by a high dose (100 mg/kg, 1.3 LD$_{50}$) of soman. Taken together, it is suggested that the prophylactics composed of physostigmine and procyclidine, in combination with posttreatment antidotes, could be a promising regimen for the prevention of lethality, seizures and brain injuries induced by organophosphates possessing diverse properties.s.

• 대한임상독성학회지
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• 제9권2호
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• pp.56-60
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• 2011

Purpose: The optimal dose of oximes for use in the treatment of organophosphorus pesticide poisoning has not been conclusively established. In this retrospective study, we assessed the effectiveness of the use of high-dose pralidoxime infusion in treating organophosphorus pesticide poisoning. Methods: From January 1998 to December 2009, 71 patients visited the hospital Emergency Department (ED) as a result of organophosphate pesticide intoxication. All of these patients received an initial bolus of 2 g of pralidoxime as the first step of treatment. Patients who then received continuous infusion of pralidoxime at a dose of 500 mg/hr were entered into study group 1 (low dose), and those treated by continuous infusion of pralidoxime at a dose of 1000 mg/hr were entered into study group 2 (high-dose). Plasma cholinesterase activities for each patient were evaluated at ED arrival and re-evaluated 24 hours after pralidoxime infusion. The effectiveness of the two treatment modalities was gauged by comparing the required duration of mechanical ventilation, time spent in the intensive care unit (ICU) and total time spent in the hospital. Results: The mean duration of mechanical ventilation was $9.98{\pm}6.47$ days for group 1 and $4.39{\pm}6.44$ days for group 2. The respective mean duration of time spent in ICU and the total number of days in the hospital were $16.38{\pm}18.84$ days and $21.87{\pm}20.16$ days for group 1, and $7.83{\pm}9.99$ days and $11.71{\pm}13.53$ days for group 2. Highdose pralidoxime treatment was associated with shorter required durations for mechanical ventilation, ICU and hospital stay. In addition, plasma cholinesterase reactivation rates were higher for those patients receiving high-dose pralidoxime treatment. Conclusion: The results suggest that high-dose pralidoxime treatment has greater efficacy for patients suffering from organophosphorus pesticide poisoning.