Decrease in Butyrylcholinesterase Accompanied by Intermediate-like Syndrome after Massive Ingestion of a Glyphosate-surfactant

Takeuchi, Ikuto; Yanagawa, Youichi; Nagasawa, Hiroki; Jitsuiki, Kei; Madokoro, Shunsuke; Takahashi, Norihito; Ohsaka, Hiromichi; Ishikawa, Kouhei; Omori, Kazuhiko

doi:10.2169/internalmedicine.2562-18

Cited by 3 publications

(1 citation statement)

References 11 publications

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“…El-Demerdash et al El-Demerdash, et al [58] reported an IC 50 value of 714.3 mM (~120 g/L) to human serum AChE exposed to GLY; a concentration significantly higher than the ones here tested and far above GLY concentrations found in human serum [3]. Concerning BChE, a case study involving a patient that ingested a GLY-based herbicide revealed a decrease in serum levels of BChE [59], while in an assay using a freshwater fish species (Labeo rohita) exposed to Roundup ® , an increase in BChE level was observed and correlated to a potential detoxification activity [60]. Other species, such as toads, have been shown to present inhibition of BChE activity when exposed to GLY-based herbicides [61].…”

Section: Pesticide-induced Cholinesterase Inhibitionmentioning

confidence: 58%

Neurotoxicity Assessment of Four Different Pesticides Using In Vitro Enzymatic Inhibition Assays

Martins-Gomes

Coutinho

Silva

et al. 2022

Toxics

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Pesticides affect different organs and tissues according to their bioavailability, chemical properties and further molecular interactions. In animal models exposed to several classes of pesticides, neurotoxic effects have been described, including the reduction of acetylcholinesterase activity in tissue homogenates. However, in homogenates, the reduction in enzymatic activity may also result from lower enzymatic expression and not only from enzymatic inhibition. Thus, in this work, we aimed to investigate the neurotoxic potential of four distinct pesticides: glyphosate (herbicide), imazalil (fungicide), imidacloprid (neonicotinoid insecticide) and lambda-cyhalothrin (pyrethroid insecticide), by assessing their inhibitory effect on the activity of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase, by using direct in vitro enzymatic inhibition methods. All pesticides dose-dependently inhibited AChE activity, with an inhibition of 11 ± 2% for glyphosate, 48 ± 2% for imidacloprid, 49 ± 3% for imazalil and 50 ± 3% for lambda-cyhalothrin, at 1 mM. Only imazalil inhibited BChE. Imazalil induced dose-dependent inhibition of BChE with identical pattern as that observed for AChE; however, for lower concentrations (up to 500 μM), imazalil showed higher specificity for AChE, and for higher concentrations, the same specificity was found. Imazalil, at 1 mM, inhibited the activity of BChE by 49 ± 1%. None of the pesticides, up to 1 mM, inhibited tyrosinase activity. In conclusion, the herbicide glyphosate shows specificity for AChE but low inhibitory capacity, the insecticides imidacloprid and λ-cyhalothrin present selective AChE inhibition, while the fungicide IMZ is a broad-spectrum cholinesterase inhibitor capable of inhibiting AChE and BChE in an equal manner. Among these pesticides, the insecticides and the fungicide are the ones with higher neurotoxic potential.

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Section: Pesticide-induced Cholinesterase Inhibitionmentioning

confidence: 58%

Neurotoxicity Assessment of Four Different Pesticides Using In Vitro Enzymatic Inhibition Assays

Martins-Gomes

Coutinho

Silva

et al. 2022

Toxics

View full text Add to dashboard Cite

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Evaluation of genotoxic effects in workers and residents of rural areas exposed to pesticides in Brazil

Amazonas,

Poça,

da Silva

et al. 2024

Mutation Research - Genetic Toxicology and Environmental Mutage

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Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase

Kolić,

Pehar,

Kovarik

2024

Archives of Industrial Hygiene and Toxicology

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Glyphosate has remained the leading herbicide on the global market to date, despite the continuous debate between consumers, scientific community, and regulatory agencies over its carcinogenicity, genotoxicity, environmental persistence, and the role in the development of neurodegenerative disorders. Chemically, glyphosate belongs to a large family of organophosphorus pesticides, which exert a neurotoxic effect by inhibiting acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), enzymes of the cholinergic system essential for maintaining neurotransmission. Although research shows that glyphosate is a weak cholinesterase inhibitor in fish and mammals compared to other OP compounds, no conclusive data exist concerning the inhibition of human AChE and BChE. In our study we analysed its inhibitory potency on human AChE and BChE, by establishing its IC50 and reversible inhibition in terms of dissociation inhibition constants. Glyphosate concentration of 40 mmol/L caused near total inhibition of enzyme activity (approx. 10 % activity remaining). Inhibition dissociation constants (K i) of glyphosate-AChE and -BChE complexes were 28.4±2.7 mmol/L and 19.3±1.8 mmol/L, respectively. In conclusion, glyphosate shows a slight binding preference for BChE but exhibits inhibition only in a high concentration range. Our results are in line with studies reporting that its neurotoxic effect is not primarily linked to the cholinergic system.

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Decrease in Butyrylcholinesterase Accompanied by Intermediate-like Syndrome after Massive Ingestion of a Glyphosate-surfactant

Cited by 3 publications

References 11 publications

Neurotoxicity Assessment of Four Different Pesticides Using In Vitro Enzymatic Inhibition Assays

Neurotoxicity Assessment of Four Different Pesticides Using In Vitro Enzymatic Inhibition Assays

Evaluation of genotoxic effects in workers and residents of rural areas exposed to pesticides in Brazil

Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase

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