Inhibition of acetylcholinesterase activity by impurities in technical grades and purified flupyrazofos

Flupyrazofos 원제 및 정제품의 불순물 조성과 Acetylcholinesterase에 대한 저해 비교

  • You, Kyoung-Youl (Research Institute SUNGBO Chemicals Co., Ltd.) ;
  • Cho, Boo-Yeon (Research Institute SUNGBO Chemicals Co., Ltd.) ;
  • Park, Dong-Sik (Division of Biological Environment, College of Agricultural and Life Sciences, Kangwon National University) ;
  • Hur, Jang-Hyun (Division of Biological Environment, College of Agricultural and Life Sciences, Kangwon National University)
  • 유경렬 ((주)성보화학 중앙연구소) ;
  • 조부연 ((주)성보화학 중앙연구소) ;
  • 박동식 (강원대학교 농업생명과학대학 생물환경학부) ;
  • 허장현 (강원대학교 농업생명과학대학 생물환경학부)
  • Published : 2005.03.31

Abstract

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.

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