Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides
- Autores
- Asis Rodriguez, Marcos Alberto; Felsztyna, Iván; Garcia, Daniel Asmed; Sánchez, Mariela Eugenia; Miguel, Virginia
- Año de publicación
- 2022
- Idioma
- inglés
- Tipo de recurso
- documento de conferencia
- Estado
- versión publicada
- Descripción
- Fluralaner and Fipronil are gabaergic insecticides belonging to the non-competitive antagonists NCA-I and NCA-II families, respectively. While fipronil binds to the pore of the insect homopentameric GABAA receptor (RDL), fluralaner targets a site located in the transmembrane region, at the receptor subunits interface. There is a major interest in the development of highly selective insecticides that are not toxic to vertebrates. In this context, it is interesting the fact that, unlike mammal membranes, which are mainly composed of phosphatidylcholine (PC) lipids, sphingolipids and sterols; insects cannot synthesize sterols. Therefore, they modulate membrane fluidity through the modification of the PC/phosphatidylethanolamine (PE) lipids ratio. This variation in the composition of the membrane of vertebrates and insects could be relevant when we analyze the nonspecific effects of lipophilic compounds on the structure and dynamics of the membrane and ultimately of RDL. Due to the lipophilicity of these compounds, and the location of the receptor binding site for fluralaner, it is probable that these insecticides could reach their binding site through the lipid bilayer. We performed Free diffusion MD simulations of POPC bilayers with increasing concentrations of Cholesterol (CHOL) or POPE, in the absence and in presence of fluralaner or fipronil. Fluralaner and fipronil acted differentially in membranes with the same composition. The analysis of these trajectories showed that fluralaner has a marked effect on the physical properties of binary bilayers containing POPE, and a negligible effect on bilayers containing CHOL. The opposite is true in the case of fipronil. On the other hand, both, fluralaner and fipronil, reduced the CHOL flip-flop rates, except for the POPC-CHOL 1:1 system in which fipronil enhanced it considerably. Our results suggest that fipronil and fluralaner may impact differentially on the physical properties of both types of membranes.
Fil: Asis Rodriguez, Marcos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
Fil: Felsztyna, Iván. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
Fil: Sánchez, Mariela Eugenia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
Fil: Miguel, Virginia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
L Reunion Anual de la Sociedad Argentina de Biofisica
Rosario
Argentina
Sociedad Argentina de Biofísica
Universidad Nacional de Rosario - Materia
-
fipronil
fluralaner
insect membranes
mimetic - Nivel de accesibilidad
- acceso abierto
- Condiciones de uso
- https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
- Repositorio
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/234446
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Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticidesAsis Rodriguez, Marcos AlbertoFelsztyna, IvánGarcia, Daniel AsmedSánchez, Mariela EugeniaMiguel, Virginiafipronilfluralanerinsect membranesmimetichttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Fluralaner and Fipronil are gabaergic insecticides belonging to the non-competitive antagonists NCA-I and NCA-II families, respectively. While fipronil binds to the pore of the insect homopentameric GABAA receptor (RDL), fluralaner targets a site located in the transmembrane region, at the receptor subunits interface. There is a major interest in the development of highly selective insecticides that are not toxic to vertebrates. In this context, it is interesting the fact that, unlike mammal membranes, which are mainly composed of phosphatidylcholine (PC) lipids, sphingolipids and sterols; insects cannot synthesize sterols. Therefore, they modulate membrane fluidity through the modification of the PC/phosphatidylethanolamine (PE) lipids ratio. This variation in the composition of the membrane of vertebrates and insects could be relevant when we analyze the nonspecific effects of lipophilic compounds on the structure and dynamics of the membrane and ultimately of RDL. Due to the lipophilicity of these compounds, and the location of the receptor binding site for fluralaner, it is probable that these insecticides could reach their binding site through the lipid bilayer. We performed Free diffusion MD simulations of POPC bilayers with increasing concentrations of Cholesterol (CHOL) or POPE, in the absence and in presence of fluralaner or fipronil. Fluralaner and fipronil acted differentially in membranes with the same composition. The analysis of these trajectories showed that fluralaner has a marked effect on the physical properties of binary bilayers containing POPE, and a negligible effect on bilayers containing CHOL. The opposite is true in the case of fipronil. On the other hand, both, fluralaner and fipronil, reduced the CHOL flip-flop rates, except for the POPC-CHOL 1:1 system in which fipronil enhanced it considerably. Our results suggest that fipronil and fluralaner may impact differentially on the physical properties of both types of membranes.Fil: Asis Rodriguez, Marcos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaFil: Felsztyna, Iván. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaFil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaFil: Sánchez, Mariela Eugenia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaFil: Miguel, Virginia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaL Reunion Anual de la Sociedad Argentina de BiofisicaRosarioArgentinaSociedad Argentina de BiofísicaUniversidad Nacional de RosarioSociedad Argentina de BiofísicaAmbroggio, Ernesto EstebanCelej, Maria SoledadAcierno, Juan Pablo2022info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/conferenceObjectCongresoBookhttp://purl.org/coar/resource_type/c_5794info:ar-repo/semantics/documentoDeConferenciaapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/234446Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides; L Reunion Anual de la Sociedad Argentina de Biofisica; Rosario; Argentina; 2022; 108-108978-987-48938-0-2CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://biofisica.org.ar/reuniones-cientificas/reunionsab-previas/Internacionalinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T09:43:40Zoai:ri.conicet.gov.ar:11336/234446instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 09:43:40.78CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse |
dc.title.none.fl_str_mv |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
title |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
spellingShingle |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides Asis Rodriguez, Marcos Alberto fipronil fluralaner insect membranes mimetic |
title_short |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
title_full |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
title_fullStr |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
title_full_unstemmed |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
title_sort |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides |
dc.creator.none.fl_str_mv |
Asis Rodriguez, Marcos Alberto Felsztyna, Iván Garcia, Daniel Asmed Sánchez, Mariela Eugenia Miguel, Virginia |
author |
Asis Rodriguez, Marcos Alberto |
author_facet |
Asis Rodriguez, Marcos Alberto Felsztyna, Iván Garcia, Daniel Asmed Sánchez, Mariela Eugenia Miguel, Virginia |
author_role |
author |
author2 |
Felsztyna, Iván Garcia, Daniel Asmed Sánchez, Mariela Eugenia Miguel, Virginia |
author2_role |
author author author author |
dc.contributor.none.fl_str_mv |
Ambroggio, Ernesto Esteban Celej, Maria Soledad Acierno, Juan Pablo |
dc.subject.none.fl_str_mv |
fipronil fluralaner insect membranes mimetic |
topic |
fipronil fluralaner insect membranes mimetic |
purl_subject.fl_str_mv |
https://purl.org/becyt/ford/1.6 https://purl.org/becyt/ford/1 |
dc.description.none.fl_txt_mv |
Fluralaner and Fipronil are gabaergic insecticides belonging to the non-competitive antagonists NCA-I and NCA-II families, respectively. While fipronil binds to the pore of the insect homopentameric GABAA receptor (RDL), fluralaner targets a site located in the transmembrane region, at the receptor subunits interface. There is a major interest in the development of highly selective insecticides that are not toxic to vertebrates. In this context, it is interesting the fact that, unlike mammal membranes, which are mainly composed of phosphatidylcholine (PC) lipids, sphingolipids and sterols; insects cannot synthesize sterols. Therefore, they modulate membrane fluidity through the modification of the PC/phosphatidylethanolamine (PE) lipids ratio. This variation in the composition of the membrane of vertebrates and insects could be relevant when we analyze the nonspecific effects of lipophilic compounds on the structure and dynamics of the membrane and ultimately of RDL. Due to the lipophilicity of these compounds, and the location of the receptor binding site for fluralaner, it is probable that these insecticides could reach their binding site through the lipid bilayer. We performed Free diffusion MD simulations of POPC bilayers with increasing concentrations of Cholesterol (CHOL) or POPE, in the absence and in presence of fluralaner or fipronil. Fluralaner and fipronil acted differentially in membranes with the same composition. The analysis of these trajectories showed that fluralaner has a marked effect on the physical properties of binary bilayers containing POPE, and a negligible effect on bilayers containing CHOL. The opposite is true in the case of fipronil. On the other hand, both, fluralaner and fipronil, reduced the CHOL flip-flop rates, except for the POPC-CHOL 1:1 system in which fipronil enhanced it considerably. Our results suggest that fipronil and fluralaner may impact differentially on the physical properties of both types of membranes. Fil: Asis Rodriguez, Marcos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina Fil: Felsztyna, Iván. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina Fil: Sánchez, Mariela Eugenia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina Fil: Miguel, Virginia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina L Reunion Anual de la Sociedad Argentina de Biofisica Rosario Argentina Sociedad Argentina de Biofísica Universidad Nacional de Rosario |
description |
Fluralaner and Fipronil are gabaergic insecticides belonging to the non-competitive antagonists NCA-I and NCA-II families, respectively. While fipronil binds to the pore of the insect homopentameric GABAA receptor (RDL), fluralaner targets a site located in the transmembrane region, at the receptor subunits interface. There is a major interest in the development of highly selective insecticides that are not toxic to vertebrates. In this context, it is interesting the fact that, unlike mammal membranes, which are mainly composed of phosphatidylcholine (PC) lipids, sphingolipids and sterols; insects cannot synthesize sterols. Therefore, they modulate membrane fluidity through the modification of the PC/phosphatidylethanolamine (PE) lipids ratio. This variation in the composition of the membrane of vertebrates and insects could be relevant when we analyze the nonspecific effects of lipophilic compounds on the structure and dynamics of the membrane and ultimately of RDL. Due to the lipophilicity of these compounds, and the location of the receptor binding site for fluralaner, it is probable that these insecticides could reach their binding site through the lipid bilayer. We performed Free diffusion MD simulations of POPC bilayers with increasing concentrations of Cholesterol (CHOL) or POPE, in the absence and in presence of fluralaner or fipronil. Fluralaner and fipronil acted differentially in membranes with the same composition. The analysis of these trajectories showed that fluralaner has a marked effect on the physical properties of binary bilayers containing POPE, and a negligible effect on bilayers containing CHOL. The opposite is true in the case of fipronil. On the other hand, both, fluralaner and fipronil, reduced the CHOL flip-flop rates, except for the POPC-CHOL 1:1 system in which fipronil enhanced it considerably. Our results suggest that fipronil and fluralaner may impact differentially on the physical properties of both types of membranes. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022 |
dc.type.none.fl_str_mv |
info:eu-repo/semantics/publishedVersion info:eu-repo/semantics/conferenceObject Congreso Book http://purl.org/coar/resource_type/c_5794 info:ar-repo/semantics/documentoDeConferencia |
status_str |
publishedVersion |
format |
conferenceObject |
dc.identifier.none.fl_str_mv |
http://hdl.handle.net/11336/234446 Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides; L Reunion Anual de la Sociedad Argentina de Biofisica; Rosario; Argentina; 2022; 108-108 978-987-48938-0-2 CONICET Digital CONICET |
url |
http://hdl.handle.net/11336/234446 |
identifier_str_mv |
Effects of the composition of insects and mammals membranes on the non-specific action of GABAergic insecticides; L Reunion Anual de la Sociedad Argentina de Biofisica; Rosario; Argentina; 2022; 108-108 978-987-48938-0-2 CONICET Digital CONICET |
dc.language.none.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
info:eu-repo/semantics/altIdentifier/url/https://biofisica.org.ar/reuniones-cientificas/reunionsab-previas/ |
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info:eu-repo/semantics/openAccess https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
eu_rights_str_mv |
openAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
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application/pdf application/pdf application/pdf application/pdf application/pdf |
dc.coverage.none.fl_str_mv |
Internacional |
dc.publisher.none.fl_str_mv |
Sociedad Argentina de Biofísica |
publisher.none.fl_str_mv |
Sociedad Argentina de Biofísica |
dc.source.none.fl_str_mv |
reponame:CONICET Digital (CONICET) instname:Consejo Nacional de Investigaciones Científicas y Técnicas |
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Consejo Nacional de Investigaciones Científicas y Técnicas |
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CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.mail.fl_str_mv |
dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar |
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