A Study on Neuro-Irreversible Factor of Dechlorinated Products for Chlorpyrifos and its Oxon Compounds

DOI Web Site Web Site 18 References

Bibliographic Information

Other Title
  • クロルピリホス脱塩素化オキソン体の不可逆的神経毒性指標に関する研究
  • クロルピリホス ダツエンソカ オキソンタイ ノ フカギャクテキ シンケイ ドクセイ シヒョウ ニ カンスル ケンキュウ

Search this article

Abstract

We focused on dechlorinated compounds of chlorpyrifos (CPF) that is well-known as one of the organophosphorus insecticides. We synthesized some of them and observed their acetylcholinesterase 50% inhibitory concentration, IC50, by using the Ellman's method. It was found that the relative activity defined as Log10 (IC50Gal / IC50) in term of IC50Gal of galantamine was estimated as follows; CPFoxon ; 3.16, 3,5Cl-CPFoxon; 1.84, 6Cl-CPFoxon; 1.04, NonCl-CPFoxon; 1.93, and CPF; −0.39. In addition, we carried out docking simulation, and it was found that the relative activity depends on the length between the ligand-binding site of acetylcholinesterase and the P-atom in ligand molecule. Next, in order to evaluate the irreversible inhibition-abilities of the synthesized compounds, we introduced neurotoxicity factor, NIF, defined as Log10(IC50Gal / IC504h) using IC504h observed after 4 h of reaction. The NIF values were estimated as follows; CPFoxon; 4.6, 3,5Cl-CPFoxon; 3.2, 6Cl-CPFoxon; 2.0, NonCl-CPFoxon; 2.5, and CPF; 1.2. It was found that the dechlorinated CPFoxons exhibited not only marked relative activity, but also irreversible inhibition-abilities judging from the NIF. Therefore, we concluded that NIF can be regarded as a useful index to reveal the irreversible inhibition-abilities induced by the CPFoxons and its dechlorinated relatives, because the irreversibility should be considered to clarify the detailed neurotoxic risk.

Journal

  • Indoor Environment

    Indoor Environment 26 (1), 3-14, 2023

    Society of Indoor Environment, Japan

References(18)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top