Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers
Autor(a) principal: | |
---|---|
Data de Publicação: | 2012 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1016/j.tox.2011.12.004 http://hdl.handle.net/11449/8134 |
Resumo: | The current Organisation for Economic Co-operation and Development (OECD) guidelines for evaluating organophosphorus-induced delayed neuropathy (OPIDN) require the observation of dosed animals over several days and the sacrifice of 48 hens. Adhering to these protocols in tests with enantiomers is difficult because large quantities of the compound are needed and many animals must be utilized. Thus, developing an in vitro screening protocol to evaluate chiral organophosphorus pesticides (OPs) that can induce delayed neuropathy is important. This work aimed to evaluate, in blood and brain samples from hens, human blood, and human cell culture samples, the potential of the enantiomeric forms of methamidophos to induce acetylcholinesterase (AChE) inhibition and/or delayed neurotoxicity. Calpain activation was also evaluated in the hen brain and SH-SY5Y human neuroblastoma cells. The ratio between the inhibition of neuropathy target esterase (NTE) and AChE activities by the methamidophos enantiomers was evaluated as a possible indicator of the enantiomers' abilities to induce OPIDN. The (-)-methamidophos exhibited an IC50 value approximately 6 times greater than that of the (+)-methamidophos for the lymphocyte NTE (LNTE) of hens, and (+)-methamidophos exhibited an IC50 value approximately 7 times larger than that of the (-)-methamidophos for the hen brain AChE. The IC50 values were 7 times higher for the human erythrocyte AChE and 5 times higher for AChE in the SH-SY5Y human neuroblastoma cells. Considering the esterases inhibition and calpain results, (+)-methamidophos would be expected to have a greater ability to induce OPIDN than the (-)-methamidophos in humans and in hens. (C) 2011 Elsevier B.V. All rights reserved. |
id |
UNSP_6d486753541ff30afd58f1cc58acb16c |
---|---|
oai_identifier_str |
oai:repositorio.unesp.br:11449/8134 |
network_acronym_str |
UNSP |
network_name_str |
Repositório Institucional da UNESP |
repository_id_str |
2946 |
spelling |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomersOrganophosphate pesticidesMethamidophosChiral pesticidesAcetylcholinesteraseNeuropathy target esteraseCalpainThe current Organisation for Economic Co-operation and Development (OECD) guidelines for evaluating organophosphorus-induced delayed neuropathy (OPIDN) require the observation of dosed animals over several days and the sacrifice of 48 hens. Adhering to these protocols in tests with enantiomers is difficult because large quantities of the compound are needed and many animals must be utilized. Thus, developing an in vitro screening protocol to evaluate chiral organophosphorus pesticides (OPs) that can induce delayed neuropathy is important. This work aimed to evaluate, in blood and brain samples from hens, human blood, and human cell culture samples, the potential of the enantiomeric forms of methamidophos to induce acetylcholinesterase (AChE) inhibition and/or delayed neurotoxicity. Calpain activation was also evaluated in the hen brain and SH-SY5Y human neuroblastoma cells. The ratio between the inhibition of neuropathy target esterase (NTE) and AChE activities by the methamidophos enantiomers was evaluated as a possible indicator of the enantiomers' abilities to induce OPIDN. The (-)-methamidophos exhibited an IC50 value approximately 6 times greater than that of the (+)-methamidophos for the lymphocyte NTE (LNTE) of hens, and (+)-methamidophos exhibited an IC50 value approximately 7 times larger than that of the (-)-methamidophos for the hen brain AChE. The IC50 values were 7 times higher for the human erythrocyte AChE and 5 times higher for AChE in the SH-SY5Y human neuroblastoma cells. Considering the esterases inhibition and calpain results, (+)-methamidophos would be expected to have a greater ability to induce OPIDN than the (-)-methamidophos in humans and in hens. (C) 2011 Elsevier B.V. All rights reserved.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Fundação para o Desenvolvimento da UNESP (FUNDUNESP)Virginia-Maryland Regional College of Veterinary MedicineUniv Estadual Paulista UNESP, Sch Pharmaceut Sci, Dept Nat Act Principles & Toxicol, BR-14801902 Araraquara, SP, BrazilUniversidade Federal de São Carlos (UFSCar), Dept Chem, São Carlos, SP, BrazilVirginia Polytech Inst & State Univ, Virginia Maryland Reg Coll Vet Med, Dept Biomed Sci & Pathobiol, Blacksburg, VA 24061 USAUniv Estadual Paulista UNESP, Sch Pharmaceut Sci, Dept Nat Act Principles & Toxicol, BR-14801902 Araraquara, SP, BrazilFAPESP: 09/51048-8FUNDUNESP: 01318/10 DFPElsevier B.V.Universidade Estadual Paulista (Unesp)Universidade Federal de São Carlos (UFSCar)Virginia Polytech Inst & State UnivEmerick, Guilherme Luz [UNESP]DeOliveira, Georgino H. [UNESP]Oliveira, Regina V.Ehrich, Marion2014-05-20T13:25:37Z2014-05-20T13:25:37Z2012-02-26info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article145-150application/pdfhttp://dx.doi.org/10.1016/j.tox.2011.12.004Toxicology. Clare: Elsevier B.V., v. 292, n. 2-3, p. 145-150, 2012.0300-483Xhttp://hdl.handle.net/11449/813410.1016/j.tox.2011.12.004WOS:000300804700010WOS000300804700010.pdfWeb of Sciencereponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengToxicology3.265info:eu-repo/semantics/openAccess2024-06-24T14:51:24Zoai:repositorio.unesp.br:11449/8134Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T14:24:22.858270Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
title |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
spellingShingle |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers Emerick, Guilherme Luz [UNESP] Organophosphate pesticides Methamidophos Chiral pesticides Acetylcholinesterase Neuropathy target esterase Calpain |
title_short |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
title_full |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
title_fullStr |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
title_full_unstemmed |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
title_sort |
Comparative in vitro study of the inhibition of human and hen esterases by methamidophos enantiomers |
author |
Emerick, Guilherme Luz [UNESP] |
author_facet |
Emerick, Guilherme Luz [UNESP] DeOliveira, Georgino H. [UNESP] Oliveira, Regina V. Ehrich, Marion |
author_role |
author |
author2 |
DeOliveira, Georgino H. [UNESP] Oliveira, Regina V. Ehrich, Marion |
author2_role |
author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Universidade Federal de São Carlos (UFSCar) Virginia Polytech Inst & State Univ |
dc.contributor.author.fl_str_mv |
Emerick, Guilherme Luz [UNESP] DeOliveira, Georgino H. [UNESP] Oliveira, Regina V. Ehrich, Marion |
dc.subject.por.fl_str_mv |
Organophosphate pesticides Methamidophos Chiral pesticides Acetylcholinesterase Neuropathy target esterase Calpain |
topic |
Organophosphate pesticides Methamidophos Chiral pesticides Acetylcholinesterase Neuropathy target esterase Calpain |
description |
The current Organisation for Economic Co-operation and Development (OECD) guidelines for evaluating organophosphorus-induced delayed neuropathy (OPIDN) require the observation of dosed animals over several days and the sacrifice of 48 hens. Adhering to these protocols in tests with enantiomers is difficult because large quantities of the compound are needed and many animals must be utilized. Thus, developing an in vitro screening protocol to evaluate chiral organophosphorus pesticides (OPs) that can induce delayed neuropathy is important. This work aimed to evaluate, in blood and brain samples from hens, human blood, and human cell culture samples, the potential of the enantiomeric forms of methamidophos to induce acetylcholinesterase (AChE) inhibition and/or delayed neurotoxicity. Calpain activation was also evaluated in the hen brain and SH-SY5Y human neuroblastoma cells. The ratio between the inhibition of neuropathy target esterase (NTE) and AChE activities by the methamidophos enantiomers was evaluated as a possible indicator of the enantiomers' abilities to induce OPIDN. The (-)-methamidophos exhibited an IC50 value approximately 6 times greater than that of the (+)-methamidophos for the lymphocyte NTE (LNTE) of hens, and (+)-methamidophos exhibited an IC50 value approximately 7 times larger than that of the (-)-methamidophos for the hen brain AChE. The IC50 values were 7 times higher for the human erythrocyte AChE and 5 times higher for AChE in the SH-SY5Y human neuroblastoma cells. Considering the esterases inhibition and calpain results, (+)-methamidophos would be expected to have a greater ability to induce OPIDN than the (-)-methamidophos in humans and in hens. (C) 2011 Elsevier B.V. All rights reserved. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-02-26 2014-05-20T13:25:37Z 2014-05-20T13:25:37Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1016/j.tox.2011.12.004 Toxicology. Clare: Elsevier B.V., v. 292, n. 2-3, p. 145-150, 2012. 0300-483X http://hdl.handle.net/11449/8134 10.1016/j.tox.2011.12.004 WOS:000300804700010 WOS000300804700010.pdf |
url |
http://dx.doi.org/10.1016/j.tox.2011.12.004 http://hdl.handle.net/11449/8134 |
identifier_str_mv |
Toxicology. Clare: Elsevier B.V., v. 292, n. 2-3, p. 145-150, 2012. 0300-483X 10.1016/j.tox.2011.12.004 WOS:000300804700010 WOS000300804700010.pdf |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Toxicology 3.265 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
145-150 application/pdf |
dc.publisher.none.fl_str_mv |
Elsevier B.V. |
publisher.none.fl_str_mv |
Elsevier B.V. |
dc.source.none.fl_str_mv |
Web of Science reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808128356253696000 |