ArticleEnvironmental science & technology2016
Metabolism and Bioactivation of Fluorochloridone, a Novel Selective Herbicide, in Vivo and in Vitro.
Article in Environmental science & technology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 24 citations in OpenAlex.
- Genotoxic Herbicide Exposures in Golden Retrievers With and Without Multicentric Lymphoma.Veterinary and comparative oncology · 2025Article
- Unveiling the nexus between environmental exposures and testicular damages: revelations from autophagy and oxidative stress imbalance.Cell death discovery · 2025Review
- Characterization of Cytosolic GlutathioneDrug metabolism and disposition: the biological fate of chemicals · 2021Article
- Effects of Flurochloridone Application on Rhizosphere Soil Fungal Community and Composition in Potato Growing Areas of the Qinghai-Tibet Plateau.Journal of fungi (Basel, Switzerland) · 2021Article
- Chloro-s-triazines-toxicokinetic, Toxicodynamic, Human Exposure, and Regulatory Considerations.Current drug metabolism · 2021Review
- Toxicity of the herbicide flurochloridone to the aquatic plants Ceratophyllum demersum and Lemna minor.Environmental science and pollution research international · 2020Article
- Low dose of flurochloridone affected reproductive system of male rats but not fertility and early embryonic development.Reproductive biology and endocrinology : RB&E · 2019Article
- Antibiotics may increase triazine herbicide exposure risk via disturbing gut microbiota.Microbiome · 2018Article
- Identification and Quantification of Novel Major Metabolites of the Steroidal Aromatase Inhibitor, Exemestane.Drug metabolism and disposition: the biological fate of chemicals · 2018Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
Fluorochloridone (FLC) is a herbicide used worldwide that is thought to be safe. However, due to its potential genotoxicity, cytotoxicity, and even systematic toxicity, there are increasing concerns about human exposure to this compound. Thus, the metabolism and bioactivation of FLC was investigated. After oral administration to mice, 27 metabolites were identified by ultrahigh performance liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry and with further structural identification by nuclear magnetic resonance spectroscopy. Hydroxylation and oxidative dechlorination were the major phase I pathways, while glutathione (GSH) and N-acetylcysteine conjugations were two major phase II pathways, indicating the formation of a reactive intermediate. In vitro microsomal and cytosolic studies revealed that a GSH conjugate (M13) was the predominant metabolite of FLC formed through a nucleophilic SN2 substitution of 3-Cl by GSH; this pathway is NADPH independent and accelerated by glutathione S-transferase (GST). Further, a kinetic study showed that M13 formation in both human liver microsomes and cytosols obeyed typical Michaelis-Menten kinetics. The maximum clearance (Vmax/Km) of GSH conjugation in human liver microsomes was approximately 5.5-fold higher than human liver cytosol, thus implying that microsomal GST was mainly responsible for M13 formation. These findings are important for understanding the potential hazard of human exposure to FLC.
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Registered trials
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