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prothioconazole
ENVIRONMENTAL POLLUTION · 2020 · IF 6.793

Effects of exposure to prothioconazole and its metabolite prothioconazole-desthio on oxidative stress and metabolic profiles of liver and kidney tissues in male mice

Zhiyuan Meng,Sinuo Tian,Wei Sun,Li Liu,Sen Yan,Shiran Huang,Wentao Zhu,Zhiqiang Zhou

Prothioconazole (PTC), a popular agricultural fungicide , and its main metabolite prothioconazole-desthio (PTCd) are receiving great attention due to their toxicological effects in the non-target organisms. This study investigated their dosage-dependent (1 and 5 mg/kg BW/day) toxicological effects on oxidative stress and metabolic profiles of liver and kidney tissues using male mice. PTC and PTCd significantly inhibited the growth phenotype including body weights gain, liver and kidney indices. Furthermore, these effects were deeply investigated using the biomarkers of oxidative stress, and metabolomics. Notably, these effects were dose and tissue-dependent. Specifically, the more serious impacts involving oxidative stress and metabolic disorders were observed in the high concentration treatment groups. Also, the liver tissue was more severely affected than the kidney tissue. Lastly, the change in oxidative stress biomarkers and metabolomics profile revealed that PTCd induced more severe toxic effects than the parent compound PTC. In brief, these results indicate that exposure to PTC and PTCd could cause potential health risks in mammals.

研究领域: 毒理学 · 环境科学 · 代谢组学
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CHEMOSPHERE · 2020 · IF 5.778

Exposure to prothioconazole induces developmental toxicity and cardiovascular effects on zebrafish embryo

Yongqi Sun,Yi Cao,Lili Tong,Fangyi Tao,Xiaonan Wang,Huiming Wu,Mengcen Wang

Prothioconazole is a fungicide that has been widely used in general agriculture and livestock husbandry. This study evaluated the acute toxicity of prothioconazole to zebrafish embryos by assessing their hatching rate and malformation when exposed to different concentrations of prothioconazole. The 96 h-LC 50 value of zebrafish embryos was 1.70 mg/L. Upon exposure to 0.85 mg/L, the mortality rate of the embryos significantly increased while their hatching rate decreased significantly. At prothioconazole concentrations higher than 0.43 mg/L, developmental morphologic abnormalities such as heart and yolk-sac edema, spine curvature, tail deformity, shortened body length and decreased eye area were observed. The heart rate of embryos decreased in a dose-dependent fashion during the exposure time. Prothioconazole exposure also resulted in increased rates of cardiac malformation detected by significant increase in the distance between the sinus venosus and bulbus arteriosus and the pericardium area. Moreover, the expression levels of genes related to cardiac development ( amhc, vmhc, fli1, hand2, gata4, nkx2.5, tbx5 and atp2a2a ) were significantly altered after exposure to prothioconazole. Indeed, this study revealed the adverse effects on the developmental and cardiovascular system of zebrafish embryo caused by prothioconazole. It further elucidated the risk of prothioconazole exposure to vertebrate cardiovascular toxicity. As such, it provides a theoretical foundation for pesticide risk management measures.

研究领域: 毒理学 · 环境科学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2023 · IF 6.1

Residue Behavior of Chiral Fungicide Prothioconazole and Its Major Chiral Metabolite in Flour Product Processing

Qingkui Fang,Kang Zheng,Rong Zeng,Zhaoxian Zhang,Yanhong Shi,Quan Gao,Jinjing Xiao,Min Liao,Jinsheng Duan,Haiqun Cao

This study systematically investigates the stereoselective metabolism and residue behavior of chiral pesticide prothioconazole enantiomers during the steaming, baking, and frying of steamed buns, bread, and deep-fried dough sticks. The results show that steaming, baking, and frying can significantly promote the degradation of the prothioconazole enantiomers. In low- and high-concentration treatments, the degradation rates of prothioconazole enantiomers were over 96.0% and 45.4%, respectively, and the residual concentration of prothioconazole-desthio enantiomers was less than 32.7 μg/kg (excluding fried processing). During the processing of steamed buns, bread, and deep-fried dough sticks, the enantiomer fraction (EF) value of the prothioconazole enantiomer was close to 0.5, and the stereoselectivity was not significant. During the processing of steamed buns (low concentration), bread (low and high concentrations), and deep-fried dough sticks (low concentration), the stereoselectivity of prothioconazole-desthio was significant, and preferential enantiomer degradation occurred. Following the analysis of 120 flour product samples, the residual risk.

CAS / MDL: 7647-14-5 7487-88-9
研究领域: 食品科学 · 环境毒理学 · 农药化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Additives and Contaminants Part A-Chemistry Analysis Control Exposure & Risk Assessment · 2023 · IF 2.9

Residue levels and dietary risk evaluation of prothioconazole-desthio and kresoxim-methyl in cucumbers after field application in twelve regions in China

Chao Dong,Jiye Hu

A commercial formulation called prothioconazole·kresoxim-methyl 50% water dispersible granule (WG), used to control the powdery mildew, is under registration for use on cucumbers. Therefore it is urgent to validate the reliability of the recommended good agricultural practices (GAP) conditions (187.5 g a.i. ha−1, three sprays with a 7-d interval, and a pre-harvest interval of 3 d) by conducting field trials in 12 regions in China, as required by national regulations, with a subsequent risk assessment. The residues of prothioconazole-desthio and kresoxim-methyl in field samples were determined using QuEChERS coupled with high-performance liquid chromatography – tandem mass spectrometry (HPLC-MS/MS). On the suggested pre-harvest interval (PHI, 3 d), the residual concentrations of prothioconazole-desthio (no maximum residue limit set in China) and kresoxim-methyl (maximum residue limit = 0.5 mg/kg) in cucumbers were 0.01–0.020 and 0.01–0.050 mg/kg, respectively. The acute risk quotients of prothioconazole-desthio in cucumbers were no higher than 0.079% for Chinese consumers. The chronic dietary risk quotient of kresoxim-methyl and of prothioconazole-desthio for different groups of consumers in China ranged from 2.3% to 5.3% and from 1.6% to 4.6%, respectively. Thus, prothioconazole·kresoxim-methyl 50% WG sprayed on cucumbers under the recommended GAP information can pose a negligible risk for Chinese consumers.

CAS / MDL: 75-05-8 64-18-6
研究领域: 植物保护 · 食品安全
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Environmental Science-Nano · 2022 ·Vol. 9 ·期 7 ·2548-2558 · IF 9.473

Synthesis, antifungal evaluation, and safety assessment of mesoporous silica nanoparticles loaded with prothioconazole against crop pathogens

Jianguo Feng,Li Sun,Wang Chen,Nuo Wei,Chaoqun Hou,Zhiyang Chen,Fei Meng,Hongen Cao

Mesoporous silica nanoparticles (MSNs) can be used as carriers to prepare pesticide controlled release formulations with high pesticide loadings and reduce the negative environmental impact of pesticides. In this study, MSNs were prepared as carriers to load prothioconazole using the sol–gel method and one-pot method. The results show that the prepared MSNs had a high loading content of prothioconazole (38.8%, w/w). The release rate of MSNs loaded with prothioconazole (Prot@MSNs) was related to environmental pH and temperature. The release rate of prothioconazole was higher under weak acid and weak base conditions than under neutral conditions. The release rate increased with the increase of temperature. Compared with the prothioconazole oil dispersion, Prot@MSNs showed better antifungal activity against rice blast (Magnaporthe oryzae) and wheat scab (Fusarium graminearum) with a longer duration. Furthermore, Prot@MSNs showed lower toxicity to zebrafish, earthworms and BEAS-2B cells, and also alleviated the inhibitory effect of prothioconazole on rice and wheat. Therefore, Prot@MSNs has great potential for agricultural applications as an effective, environment-friendly and sustained-release pesticide formulation.

研究领域: 植物保护 · 农药科学 · 纳米材料 · 毒理学
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FOOD CHEMISTRY · 2021 · IF 7.514

Popping candy-assisted dispersive liquid–liquid microextraction for enantioselective determination of prothioconazole and its chiral metabolite in water, beer, Baijiu, and vinegar samples by HPLC

Xu Jing,Xin Huang,Huihui Wang,Haoyue Xue,Beiqi Wu,Xiaowen Wang,Liyan Jia

To simultaneously determine the enantiomers of prothioconazole and its chiral metabolite prothioconazole-desthio in water, beer, Baijiu, and vinegar samples by HPLC, a simple, fast, environmentally-friendly popping candy-assisted dispersive liquid–liquid microextraction technique was developed. A green medium-chain fatty acid (decanoic acid) and popping candy could be used as the extractant and solid dispersant respectively to avoid the use of toxic organic solvents. Decanoic acid was collected after extraction by solidification at room temperature. The linear range of this technique was from 27.1 to 1000 µg L −1 . The limits of detection and quantification were within the ranges of 8.1–11.2 μg L -1 and 27.1–37.3 μg L -1 , respectively. The extraction recovery was 80.8% to 102.5% with the relative standard deviation ranged from 1.1 to 7.1%. This technique has been successfully applied to enantioselectively determine the residues of prothioconazole and prothioconazole-desthio in water, beer, Baijiu, and vinegar samples.

研究领域: 分析化学 · 环境科学 · 食品科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

A Typical Fungicide and Its Main Metabolite Promote Liver Damage in Mice through Impacting Gut Microbiota and Intestinal Barrier Function

Zhiyuan Meng,Shiran Huang,Wei Sun,Sen Yan,Xiaojun Chen,Jinling Diao,Zhiqiang Zhou,Wentao Zhu

The environmental risks of prothioconazole (PTC), a popular agricultural fungicide, and its main metabolite, prothioconazole-desthio (PTCd), have attracted more and more attention recently. In this study, the adverse effects of PTC and PTCd on liver function in mice and their underlying mechanisms have been systematically studied from the perspective of gut microbiota. Combining the results of physiological, biochemical, and histopathological analysis showed that PTC and PTCd exposure could cause lipid accumulation and inflammation in the liver of mice. In addition, exposure to PTC and PTCd could also significantly affect the transcriptome of liver tissue, leading to disorders of lipid metabolism of the liver. Particularly, the abundances of bacteria in liver tissues were significantly increased with PTC and PTCd exposure. Further results show that PTC and PTCd could affect the expression of genes related to inflammation and the barrier function in colon tissue, leading to intestinal dysfunction in mice. Last but not least, the results based on 16S rRNA gene sequencing and 1H NMR metabolomics analysis showed that exposure to PTC and PTCd could cause gut microbiota imbalances and cecal content metabolic profile disorders. In short, this study found that PTC and PTCd exposure could cause liver damage in mice by changing the gut microbiota, disrupting the intestinal barrier function and promoting bacterial translocation. These results clarified the key role of gut microbiota in liver damage induced by PTC and PTCd in mice and proposed a new insight into the mechanisms of liver toxicity induced by pesticides through the dialogue of the gut–liver axis.

CAS / MDL: 7789-20-0
研究领域: 毒理学 · 环境科学 · 微生物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2023 ·Vol. 28 ·期 12 ·4774 · IF 4.6

Enantioselective Toxic Effects of Prothioconazole toward Scenedesmus obliquus

Qingqing Xiang,Ying Zhou,Chengxia Tan

Prothioconazole (PTC) is a broad-spectrum triazole fungicide with one asymmetric center and consists of two enantiomers,R-(−)-PTC andS-(+)-PTC. To address the concern of its environmental safety, the enantioselective toxic effects of PTC onScendesmus obliquus(S. obliquus) were investigated. PTC racemates (Rac-PTC) and enantiomers exhibited dose-dependent acute toxicity effects againstS. obliquusat a concentration from 1 to 10 mg·L−1. The 72 h-EC50 value ofRac-,R-(−)-, andS-(+)-PTC is 8.15, 16.53, and 7.85 mg·L−1, respectively. The growth ratios and photosynthetic pigment contents of theR-(−)-PTC treatment groups were higher than theRac- andS-(+)-PTC treatment groups. Both catalase (CAT) activities and esterase activities were inhibited in theRac- andS-(+)-PTC treatment groups at high concentrations of 5 and 10 mg·L−1, and the levels of malondialdehyde (MDA) were elevated, which exceeded the levels in algal cells for theR-(−)-PTC treatment groups. PTC could disrupt the cell morphology ofS. obliquusand induce cell membrane damage, following the order ofS-(+)-PTC ≈Rac-PTC >R-(−)-PTC. The enantioselective toxic effects of PTC onS. obliquusprovide essential information for its ecological risk assessment.Keywords:prothioconazole;toxicity effects;Scenedesmus obliquus;enantioselectivity

CAS / MDL: 67-68-5
研究领域: 环境科学 · 毒理学 · 生态学
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PEST MANAGEMENT SCIENCE · 2025 · IF 3.8

Pesticide–fertilizer interactions: nutrient effects on wheat detoxification of prothioconazole

Linlin Shi,Lei Yang,Zixuan Yan,Chang Xu,Wenhui Li,Tingting Wang,Quan Gao,Min Liao,Haiqun Cao,Qingkui Fang

Background Prothioconazole (PTC), a triazole fungicide, and its metabolite prothioconazole-desthio (dPTC) present potential phytotoxic risks in crops. However, the mechanisms governing their uptake and detoxification in wheat remain unknown. This study aimed to determine how macronutrients and endogenous signaling compounds regulate PTC absorption and metabolism in wheat seedlings. Results High potassium availability markedly enhanced PTC uptake, resulting in a > 600% increase in PTC uptake over 12 h compared to the low potassium. Exogenous application of indole-3-acetic acid and brassinolide led to significant increases in PTC accumulation by 121.7% and 94.4%, respectively. Transcriptomic analysis revealed that PTC activated detoxification pathways, with prominent up-regulation of adenosine triphosphate (ATP)-binding cassette transporters and mitogen-activated protein kinase (MAPK) signaling components. Under nitrogen-deficient conditions, 1493 genes were specifically down-regulated, including those related to ribosome biogenesis, phenylalanine metabolism, and membrane transport, indicating a reduced detoxification capacity and enhanced dPTC retention. Conclusion Nitrogen availability plays a pivotal role in modulating the molecular response of wheat to PTC exposure. Nitrogen deficiency markedly down-regulated key genes involved in detoxification processes, thereby aggravating PTC-induced phytotoxicity. These results underscore the critical interplay between nutrient status and pesticide metabolism, providing mechanistic evidence to inform integrated pesticide–fertilizer management strategies aimed at minimizing chemical residues in food crops and enhancing agroecosystem sustainability. © 2025 Society of Chemical Industry.

CAS / MDL: 64-18-6
研究领域: 植物生理学 · 农药代谢 · 作物营养 · 分子生物学 · 环境毒理学 · 农业可持续性
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Applied Nanoscience · 2022 ·Vol. 12 ·期 9 ·2683-2693 · IF 3.869

Fabrication and applications of a microencapsulated prothioconazole based on β-cyclodextrin

Chi Yu,Ye Zhenghe,Su Xianyan,Li Zhao,Ren Xuexiang

In this work, a compound was fabricated using β-cyclodextrin (β-CD) and propithiumazole (PTC). FTIR and TG were used to analyze the intermolecular force and thermal stability of the compound and results indicated. The intermolecular forces were van der Waals forces. According to previous research, the seed coat agent and suspension concentrate (SC) were prepared using this compound and auxiliary. The inhibitory effect on Fusarium graminearum was studied with a bioassay. The data suggested inhibition rate of microencapsulated PTC are about 7.8% and 5% higher than PTC at 72 h and 192 h, respectively. In addition, results of pot experiments suggested dry weight of crops were increased after using seed coat agent contained microencapsulated prothioconazole which indicates that the seed coat agent may be beneficial to protein synthesis. Compared to commercial PTC, field experiments were conducted to investigate the preventive effects of SC against fusarium head blight (FHB). The results of toxicity test and field experiment showed that this compound can improve the utilization efficiency about 5% of PTC and reduce pesticide injury to wheat seeds.

CAS / MDL: 7585-39-9 11138-66-2
研究领域: 植物保护 · 农药科学
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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Integrated cell–mouse metabolomics reveals toxicity mechanisms and biomarkers of prothioconazole exposure

Linlin Shi,Wenhui Li,Xiandan Zhu,Heng Zhang,Lei Yang,Siyu Chen,Jinjing Xiao,Xiude Hua,Haiqun Cao,Qingkui Fang

BACKGROUND Prothioconazole (PTC) is one of the most widely used triazole fungicides worldwide, while its major metabolite, prothioconazole-desthio (dPTC), exhibits enhanced toxicological potential. However, the metabolic perturbations induced by chronic PTC exposure and sensitive biomarkers for exposure monitoring remain poorly understood. This study aimed to elucidate the metabolic toxicity mechanisms of PTC and identify reliable biomarkers using integrated in vitro and in vivo metabolomics. RESULTS Cytotoxicity assays demonstrated significant differences in the toxicity of eight representative pesticides toward L-02 hepatocytes, with half-maximal inhibitory concentration (IC 50 ) values of 102.8 and 167.3 μmol L −1 for PTC and dPTC, respectively. Untargeted metabolomics revealed that PTC exposure significantly disturbed lipid metabolism, nicotinate metabolism, amino acid metabolism, and mitochondrial energy homeostasis. Corticosterone, equol, and uric acid exhibited excellent discriminatory performance (area under the curve (AUC) > 0.95) and were identified as potential cellular biomarkers of exposure. In C57BL/6J mice, chronic PTC exposure for 28 days induced systemic metabolic disturbances involving the tricarboxylic acid cycle, lysine degradation, and host–microbiota co-metabolism. Targeted metabolomics further validated significant increases in succinic acid, heptanedioic acid, and 2-oxohexanedioic acid, together with a marked decrease in indole-3-propionic acid, consistent with the untargeted metabolomics results. These metabolites demonstrated high sensitivity and specificity for discriminating PTC exposure. CONCLUSIONS This study demonstrates that chronic PTC exposure disrupts mitochondrial energy metabolism and multiple metabolic pathways, leading to systemic metabolic dysfunction. The identified metabolic biomarkers provide promising tools for pesticide biomonitoring and mechanistic toxicity assessment, improving exposure surveillance and health risk evaluation of triazole fungicides. © 2026 Society of Chemical Industry.

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JOURNAL OF HAZARDOUS MATERIALS · 2022 · IF 14.224

Environmental fate and metabolism of the systemic triazolinthione fungicide prothioconazole in different aerobic soils

Xingyan Pang,Jiaoyang Li,Pengfei Xu,Wenjun Yang,Lei Huang,Sufen Zhang,Zhiyang Yu,Qingfu Ye

As a best-selling triazolinthione fungicide , prothioconazole (PTZ) has been widely used worldwide and has aroused concern about its environmental effect. This study used phenyl-UL- 14 C-labeled PTZ and an improved fate model to investigate the fate and metabolism of this fungicide in aerobic soil. During 120 d of incubation, PTZ rapidly transformed into metabolites and bound residues, with a half-life (DT 50 ) of less than 1 d. After 120 d, approximately 45–55% of PTZ formed bound residues, and the extractable metabolite residues were gradually degraded over time. Approximately 19%, 44% and 27% of phenyl-UL- 14 C-PTZ was mineralized in red soil, fluvo-aquic soil and cinnamon soil, respectively, but only approximately 3% was mineralized in black soil. Five metabolites were identified and confirmed, and a possible metabolic pathway for phenyl-UL- 14 C-PTZ in soil was proposed. Based on the correlation analysis between soil properties and model rate constants, soil properties exerted important effects on PTZ transformation. These results will provide basic data for environmental risk assessments and removal of the PTZ pollutant and suggest that the soil type should be considered in the selection and application of pesticides.

研究领域: 环境科学 · 农药学
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