Ethiprole is widely used as a second-generation phenyl pyrazole insecticide.Previous studies indicated that ethiprole exhibited thyroid toxicity while two main metabolites(ethiprole sulfone(M1)and ethiprole sulfide(M2...Ethiprole is widely used as a second-generation phenyl pyrazole insecticide.Previous studies indicated that ethiprole exhibited thyroid toxicity while two main metabolites(ethiprole sulfone(M1)and ethiprole sulfide(M2))of ethiprole showed higher acute toxicity than ethiprole.Therefore,assessing the thyroid toxicity of its metabolites is crucial for safety assessment.In this study,the thyroid toxicity and underlying mechanisms of ethiprole and its metabolites were explored using in silico,in vitro,and in vivo assays,with the aim of conducting a comparative study on thyroid toxicity.Molecular docking analysis showed that ethiprole,M1 and M2 could bind with thyroid receptor isoforms and exhibited higher binding affinity compared to 3,3,5-triiodothyronine(T3).GH3 cell proliferation assays revealed that ethiprole,M1 and M2 all served as thyroid hormone antagonists to hinder the T3-induced cell proliferation.Using the zebrafish model,we further investigated that exposure to ethiprole,M1,and M2 disrupted thyroid hormone levels and the transcriptional expressions of hypothalamus-pituitary-thyroid(HPT)axis-related genes.Ethiprole induced thyroid disrupting effects by binding with the thyroid receptor beta,M1 mainly through binding with the corticotropin releasing factor receptor-1,and M2 exposure firstly inhibited the thyroid peroxidase enzyme activity.M2 showed the highest developmental toxicity and thyroid disrupting effects,which significantly reducing hatching rates,increasing deformity rates,exhibiting the lowest lethal concentration 50 value and showing the most serious transcription inhibitory effects on the HPT axis.This study suggested the risk assessment of metabolites should be considered in assessing potential environmental risk of ethiprole.展开更多
In this study, the hydrolysis of the insecticide ethiprole in buffered solutions at pH 4.0, 7.0 and 9.0, respectively, and the degradation and adsorption-desorption behaviors of ethiprole in ifve agricultural soil sam...In this study, the hydrolysis of the insecticide ethiprole in buffered solutions at pH 4.0, 7.0 and 9.0, respectively, and the degradation and adsorption-desorption behaviors of ethiprole in ifve agricultural soil samples from China were investigated. The half-lives under anaerobic conditions were faster than that in the aerobic experiment. Ethiprole was relatively stable under both acidic and neutral conditions while it was readily hydrolyzed under alkaling condition. The sorption of ethiprole on ifve soils was well described by the linear and Freundlich equation and mainly governed by soil organic matter. The exothermic process of ethiprole adsorption can also be well explained by physical adsorption. A weak adsorption capacity was observed in all soils, which could readily lead to leaching problems.展开更多
Increasing numbers of chiral insecticides have been released into aquatic environments,leading to adverse effects on the environment.Furthermore,these insecticides have potentially undesirable side effects on the envi...Increasing numbers of chiral insecticides have been released into aquatic environments,leading to adverse effects on the environment.Furthermore,these insecticides have potentially undesirable side effects on the environment,humans and other non-target species,potentially disrupting entire ecosystems.This study investigated the effects of ethiprole enantiomers against microorganisms in sediment,duckweed,and human cells.The results showed that S-ethiprole degraded preferentially in sediment,demonstrating enantioselective behavior.In sediment,catalase and superoxide dismutase activities were significantly inhibited,and the frond number of duckweed preferably decreased with exposure to S-ethiprole at high concentration treatments(33:25=R-ethiprole:S-ethiprole).Additionally,the content of chlorophyll b decreased nearly 2 times in R-ethiprole(0.42 mg/g)treatment group in comparison to S-ethiprole(0.20 mg/g)treatment.Cytotoxicity test revealed that S-ethiprole was 2 and 3 times more toxic than rac-and R-ethiprole.The expressions of CAT,SOD and caspase-3 were upregulated in human cells treated with ethiprole enantiomers,indicating oxidative stress as a key factor in toxicity.Overall,S-ethiprole exhibited greater adverse effects than rac-and R-enantiomers in human cells.These findings demonstrate the importance of considering chirality in the risk assessment of harmful chemicals in the aquatic environment.展开更多
基金supported by the National Natural Science Foundation of China(Nos.42207320 and 22076214).
文摘Ethiprole is widely used as a second-generation phenyl pyrazole insecticide.Previous studies indicated that ethiprole exhibited thyroid toxicity while two main metabolites(ethiprole sulfone(M1)and ethiprole sulfide(M2))of ethiprole showed higher acute toxicity than ethiprole.Therefore,assessing the thyroid toxicity of its metabolites is crucial for safety assessment.In this study,the thyroid toxicity and underlying mechanisms of ethiprole and its metabolites were explored using in silico,in vitro,and in vivo assays,with the aim of conducting a comparative study on thyroid toxicity.Molecular docking analysis showed that ethiprole,M1 and M2 could bind with thyroid receptor isoforms and exhibited higher binding affinity compared to 3,3,5-triiodothyronine(T3).GH3 cell proliferation assays revealed that ethiprole,M1 and M2 all served as thyroid hormone antagonists to hinder the T3-induced cell proliferation.Using the zebrafish model,we further investigated that exposure to ethiprole,M1,and M2 disrupted thyroid hormone levels and the transcriptional expressions of hypothalamus-pituitary-thyroid(HPT)axis-related genes.Ethiprole induced thyroid disrupting effects by binding with the thyroid receptor beta,M1 mainly through binding with the corticotropin releasing factor receptor-1,and M2 exposure firstly inhibited the thyroid peroxidase enzyme activity.M2 showed the highest developmental toxicity and thyroid disrupting effects,which significantly reducing hatching rates,increasing deformity rates,exhibiting the lowest lethal concentration 50 value and showing the most serious transcription inhibitory effects on the HPT axis.This study suggested the risk assessment of metabolites should be considered in assessing potential environmental risk of ethiprole.
基金supported by the National Natural Science Foundation of China (31272070)
文摘In this study, the hydrolysis of the insecticide ethiprole in buffered solutions at pH 4.0, 7.0 and 9.0, respectively, and the degradation and adsorption-desorption behaviors of ethiprole in ifve agricultural soil samples from China were investigated. The half-lives under anaerobic conditions were faster than that in the aerobic experiment. Ethiprole was relatively stable under both acidic and neutral conditions while it was readily hydrolyzed under alkaling condition. The sorption of ethiprole on ifve soils was well described by the linear and Freundlich equation and mainly governed by soil organic matter. The exothermic process of ethiprole adsorption can also be well explained by physical adsorption. A weak adsorption capacity was observed in all soils, which could readily lead to leaching problems.
基金he National Natural Science Foundation of China(42377391)the Excellent Youth Science Foundation of BAAFs(YXQN202201)+2 种基金the Fundamental Research Funds for the Central Universities(2023CDJXY-034)the Guangdong Provincial Key Laboratory ofWater Quality Improvement and Ecology Restoration for Watersheds(2021-03)the Beijing Natural Science Foundation(8222046)for their support of this research via grants.
文摘Increasing numbers of chiral insecticides have been released into aquatic environments,leading to adverse effects on the environment.Furthermore,these insecticides have potentially undesirable side effects on the environment,humans and other non-target species,potentially disrupting entire ecosystems.This study investigated the effects of ethiprole enantiomers against microorganisms in sediment,duckweed,and human cells.The results showed that S-ethiprole degraded preferentially in sediment,demonstrating enantioselective behavior.In sediment,catalase and superoxide dismutase activities were significantly inhibited,and the frond number of duckweed preferably decreased with exposure to S-ethiprole at high concentration treatments(33:25=R-ethiprole:S-ethiprole).Additionally,the content of chlorophyll b decreased nearly 2 times in R-ethiprole(0.42 mg/g)treatment group in comparison to S-ethiprole(0.20 mg/g)treatment.Cytotoxicity test revealed that S-ethiprole was 2 and 3 times more toxic than rac-and R-ethiprole.The expressions of CAT,SOD and caspase-3 were upregulated in human cells treated with ethiprole enantiomers,indicating oxidative stress as a key factor in toxicity.Overall,S-ethiprole exhibited greater adverse effects than rac-and R-enantiomers in human cells.These findings demonstrate the importance of considering chirality in the risk assessment of harmful chemicals in the aquatic environment.
