Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase
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...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Sciendo
2024-03-01
|
| Series: | Arhiv za Higijenu Rada i Toksikologiju |
| Subjects: | |
| Online Access: | https://doi.org/10.2478/aiht-2024-75-3822 |
| _version_ | 1827298464423215104 |
|---|---|
| author | Kolić Dora Pehar Vesna Kovarik Zrinka |
| author_facet | Kolić Dora Pehar Vesna Kovarik Zrinka |
| author_sort | Kolić Dora |
| collection | DOAJ |
| description | 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 (Ki) 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. |
| first_indexed | 2024-04-24T15:15:18Z |
| format | Article |
| id | doaj.art-c45ccb9eb4584778b08f143bfc7218a7 |
| institution | Directory Open Access Journal |
| issn | 1848-6312 |
| language | English |
| last_indexed | 2024-04-24T15:15:18Z |
| publishDate | 2024-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Arhiv za Higijenu Rada i Toksikologiju |
| spelling | doaj.art-c45ccb9eb4584778b08f143bfc7218a72024-04-02T09:28:46ZengSciendoArhiv za Higijenu Rada i Toksikologiju1848-63122024-03-01751768010.2478/aiht-2024-75-3822Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesteraseKolić Dora0Pehar Vesna1Kovarik Zrinka2Institute for Medical Research and Occupational Health, Division of Toxicology, Zagreb, CroatiaDr Franjo Tuđman Croatian Defence Academy, Zagreb, CroatiaInstitute for Medical Research and Occupational Health, Division of Toxicology, Zagreb, CroatiaGlyphosate 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 (Ki) 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.https://doi.org/10.2478/aiht-2024-75-3822achebchecholinesteraseinhibitionherbicideneurotoxicityorganophosphorus compoundspesticideachebcheherbicidinhibicijakolinesterazakonstanta disocijacijeneurotoksičnostorganofosforni spojevi |
| spellingShingle | Kolić Dora Pehar Vesna Kovarik Zrinka Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase Arhiv za Higijenu Rada i Toksikologiju ache bche cholinesterase inhibition herbicide neurotoxicity organophosphorus compounds pesticide ache bche herbicid inhibicija kolinesteraza konstanta disocijacije neurotoksičnost organofosforni spojevi |
| title | Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| title_full | Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| title_fullStr | Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| title_full_unstemmed | Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| title_short | Environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| title_sort | environmental exposure to glyphosate does not inhibit human acetylcholinesterase and butyrylcholinesterase |
| topic | ache bche cholinesterase inhibition herbicide neurotoxicity organophosphorus compounds pesticide ache bche herbicid inhibicija kolinesteraza konstanta disocijacije neurotoksičnost organofosforni spojevi |
| url | https://doi.org/10.2478/aiht-2024-75-3822 |
| work_keys_str_mv | AT kolicdora environmentalexposuretoglyphosatedoesnotinhibithumanacetylcholinesteraseandbutyrylcholinesterase AT peharvesna environmentalexposuretoglyphosatedoesnotinhibithumanacetylcholinesteraseandbutyrylcholinesterase AT kovarikzrinka environmentalexposuretoglyphosatedoesnotinhibithumanacetylcholinesteraseandbutyrylcholinesterase |