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目的研究有机磷类杀虫剂对G蛋白结合受体激酶2介导的毒蕈碱乙酰胆碱m2受体磷酸化的影响和可能存在的其他作用途径。方法将纯化的毒蕈碱乙酰胆碱m2受体,G蛋白结合受体激酶-2,[γ-p32]ATP与对氧磷(PO)、氧毒死蜱(CPO)共同保温,聚丙烯酰胺凝胶电泳分离蛋白,放射性自显影检测m2受体磷酸化结果。结果氧毒死蜱完全抑制m2受体的磷酸化,其半数抑制浓度为(IC50)70μmol/L;毒死蜱也抑制m2受体的磷酸化,而对氧磷与对硫磷不抑制m2受体的磷酸化。结论不同的有机磷杀虫剂对m2受体的磷酸化有完全不同的作用;毒死蜱阻断m2受体的磷酸化,提示有机磷杀虫剂的毒性作用存在其他途径。
Objective To study the effect of organophosphate insecticides on G protein-coupled receptor kinase 2-mediated phosphorylation of muscarinic acetylcholine receptor (m2) and other possible pathways. Methods Purified muscarinic acetylcholine m2 receptor, G protein-binding receptor kinase-2 and [γ-p32] ATP were co-incubated with paraoxon and chlorpyrifos (CPO) and separated by polyacrylamide gel electrophoresis Protein, autoradiography test m2 receptor phosphorylation results. Results Chlorpyrifos completely inhibited the phosphorylation of m2 receptor, with a half-maximal inhibitory concentration (IC50) of 70 μmol / L; chlorpyrifos also inhibited the phosphorylation of m2 receptor, while paraoxon and parathion did not inhibit the phosphorylation of m2 receptor . Conclusion Different organophosphate pesticides have completely different effects on the phosphorylation of m2 receptor. Chlorpyrifos blocks the phosphorylation of m2 receptor, suggesting that there are other ways for the toxicity of organophosphate insecticides.