Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors

Autores
Hernando, Guillermina Silvana; Chrestia, Juan Facundo; Bouzat, Cecilia Beatriz
Año de publicación
2024
Idioma
inglés
Tipo de recurso
documento de conferencia
Estado
versión publicada
Descripción
Natural extracts and essential oils, often containing a diverse array of bioactive compounds, are appealing sources for identifying new potential drug candidates in drug discovery. Bioactive compounds have been used in traditional medicine for centuries to treat a variety of diseases. In recent times, there has been a resurgence of interest in these bioactive compounds due to their medicinal properties. Research has shown that many of these compounds act on neurotransmitter receptors, particularly Cys-loop receptors such as the nicotinic acetylcholine receptor (nAChR). nAChRs are a family of acetylcholine-gated ion channels found in the central and peripheral nervous systems, playing key roles in processes likemuscle contraction,memory, and attention. The primary goal of this project was to investigate the molecular effects of two naturally occurring phenylpropanoids found in Cinnamomum verum oil, transcinnamaldehyde (TCA) and eugenol (EGN), on two types of mammalian nAChRs, both of which are involved in various pathological conditions. Since TCA and EGN are multitarget compounds, it is essential to understand the molecular mechanisms underlying their potential therapeutic and adverse effects. Through single-channel recordings, we observed that TCA exerts a negative modulatory effect on both α7 and muscular nAChRs. In α7 receptors, TCA significantly reduces activity by decreasing the frequency of activation episodes without affecting the amplitude or open duration. In contrast, for muscular nAChRs, both TCA and EGNinduce a concentration-dependent reduction in open channel duration within themicromolar range. This reduction is accompanied by a shift towards shorter durations in the main closed component. The modulation of nAChRs by these compounds is pharmacologically significant and should be considered when evaluating the therapeutic potential of TCA and EGN. Our findings provide valuable insights into how natural compounds affect Cys-loop receptors, which are underexplored but critical targets for various therapeutic strategies.
Fil: Hernando, Guillermina Silvana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Chrestia, Juan Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Bouzat, Cecilia Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
LVI Reunión Anual Asociación Argentina de Farmacología Experimental
Bahía Blanca
Argentina
Asociación Argentina de Farmacología Experimental
Universidad Nacional del Sur
Materia
LIGAND-GATED ION CHANNEL
PATCH-CLAMP
ESSENTIAL OIL
C. ELEGANS
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/278295
Acceder
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network_name_str CONICET Digital (CONICET)
spelling Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine ReceptorsHernando, Guillermina SilvanaChrestia, Juan FacundoBouzat, Cecilia BeatrizLIGAND-GATED ION CHANNELPATCH-CLAMPESSENTIAL OILC. ELEGANShttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Natural extracts and essential oils, often containing a diverse array of bioactive compounds, are appealing sources for identifying new potential drug candidates in drug discovery. Bioactive compounds have been used in traditional medicine for centuries to treat a variety of diseases. In recent times, there has been a resurgence of interest in these bioactive compounds due to their medicinal properties. Research has shown that many of these compounds act on neurotransmitter receptors, particularly Cys-loop receptors such as the nicotinic acetylcholine receptor (nAChR). nAChRs are a family of acetylcholine-gated ion channels found in the central and peripheral nervous systems, playing key roles in processes likemuscle contraction,memory, and attention. The primary goal of this project was to investigate the molecular effects of two naturally occurring phenylpropanoids found in Cinnamomum verum oil, transcinnamaldehyde (TCA) and eugenol (EGN), on two types of mammalian nAChRs, both of which are involved in various pathological conditions. Since TCA and EGN are multitarget compounds, it is essential to understand the molecular mechanisms underlying their potential therapeutic and adverse effects. Through single-channel recordings, we observed that TCA exerts a negative modulatory effect on both α7 and muscular nAChRs. In α7 receptors, TCA significantly reduces activity by decreasing the frequency of activation episodes without affecting the amplitude or open duration. In contrast, for muscular nAChRs, both TCA and EGNinduce a concentration-dependent reduction in open channel duration within themicromolar range. This reduction is accompanied by a shift towards shorter durations in the main closed component. The modulation of nAChRs by these compounds is pharmacologically significant and should be considered when evaluating the therapeutic potential of TCA and EGN. Our findings provide valuable insights into how natural compounds affect Cys-loop receptors, which are underexplored but critical targets for various therapeutic strategies.Fil: Hernando, Guillermina Silvana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; ArgentinaFil: Chrestia, Juan Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; ArgentinaFil: Bouzat, Cecilia Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; ArgentinaLVI Reunión Anual Asociación Argentina de Farmacología ExperimentalBahía BlancaArgentinaAsociación Argentina de Farmacología ExperimentalUniversidad Nacional del SurAsociación Argentina de Farmacología Experimental2024info: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/11336/278295Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors; LVI Reunión Anual Asociación Argentina de Farmacología Experimental; Bahía Blanca; Argentina; 2024; 50-50978-631-90806-0-5CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://aafeargentina.org/congresos-aafe/Nacionalinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-12-23T13:18:59Zoai:ri.conicet.gov.ar:11336/278295instacron: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:34982025-12-23 13:18:59.67CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
title Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
spellingShingle Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
Hernando, Guillermina Silvana
LIGAND-GATED ION CHANNEL
PATCH-CLAMP
ESSENTIAL OIL
C. ELEGANS
title_short Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
title_full Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
title_fullStr Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
title_full_unstemmed Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
title_sort Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors
dc.creator.none.fl_str_mv Hernando, Guillermina Silvana
Chrestia, Juan Facundo
Bouzat, Cecilia Beatriz
author Hernando, Guillermina Silvana
author_facet Hernando, Guillermina Silvana
Chrestia, Juan Facundo
Bouzat, Cecilia Beatriz
author_role author
author2 Chrestia, Juan Facundo
Bouzat, Cecilia Beatriz
author2_role author
author
dc.subject.none.fl_str_mv LIGAND-GATED ION CHANNEL
PATCH-CLAMP
ESSENTIAL OIL
C. ELEGANS
topic LIGAND-GATED ION CHANNEL
PATCH-CLAMP
ESSENTIAL OIL
C. ELEGANS
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Natural extracts and essential oils, often containing a diverse array of bioactive compounds, are appealing sources for identifying new potential drug candidates in drug discovery. Bioactive compounds have been used in traditional medicine for centuries to treat a variety of diseases. In recent times, there has been a resurgence of interest in these bioactive compounds due to their medicinal properties. Research has shown that many of these compounds act on neurotransmitter receptors, particularly Cys-loop receptors such as the nicotinic acetylcholine receptor (nAChR). nAChRs are a family of acetylcholine-gated ion channels found in the central and peripheral nervous systems, playing key roles in processes likemuscle contraction,memory, and attention. The primary goal of this project was to investigate the molecular effects of two naturally occurring phenylpropanoids found in Cinnamomum verum oil, transcinnamaldehyde (TCA) and eugenol (EGN), on two types of mammalian nAChRs, both of which are involved in various pathological conditions. Since TCA and EGN are multitarget compounds, it is essential to understand the molecular mechanisms underlying their potential therapeutic and adverse effects. Through single-channel recordings, we observed that TCA exerts a negative modulatory effect on both α7 and muscular nAChRs. In α7 receptors, TCA significantly reduces activity by decreasing the frequency of activation episodes without affecting the amplitude or open duration. In contrast, for muscular nAChRs, both TCA and EGNinduce a concentration-dependent reduction in open channel duration within themicromolar range. This reduction is accompanied by a shift towards shorter durations in the main closed component. The modulation of nAChRs by these compounds is pharmacologically significant and should be considered when evaluating the therapeutic potential of TCA and EGN. Our findings provide valuable insights into how natural compounds affect Cys-loop receptors, which are underexplored but critical targets for various therapeutic strategies.
Fil: Hernando, Guillermina Silvana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Chrestia, Juan Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Bouzat, Cecilia Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur. Instituto de Investigaciones Bioquímicas de Bahía Blanca; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
LVI Reunión Anual Asociación Argentina de Farmacología Experimental
Bahía Blanca
Argentina
Asociación Argentina de Farmacología Experimental
Universidad Nacional del Sur
description Natural extracts and essential oils, often containing a diverse array of bioactive compounds, are appealing sources for identifying new potential drug candidates in drug discovery. Bioactive compounds have been used in traditional medicine for centuries to treat a variety of diseases. In recent times, there has been a resurgence of interest in these bioactive compounds due to their medicinal properties. Research has shown that many of these compounds act on neurotransmitter receptors, particularly Cys-loop receptors such as the nicotinic acetylcholine receptor (nAChR). nAChRs are a family of acetylcholine-gated ion channels found in the central and peripheral nervous systems, playing key roles in processes likemuscle contraction,memory, and attention. The primary goal of this project was to investigate the molecular effects of two naturally occurring phenylpropanoids found in Cinnamomum verum oil, transcinnamaldehyde (TCA) and eugenol (EGN), on two types of mammalian nAChRs, both of which are involved in various pathological conditions. Since TCA and EGN are multitarget compounds, it is essential to understand the molecular mechanisms underlying their potential therapeutic and adverse effects. Through single-channel recordings, we observed that TCA exerts a negative modulatory effect on both α7 and muscular nAChRs. In α7 receptors, TCA significantly reduces activity by decreasing the frequency of activation episodes without affecting the amplitude or open duration. In contrast, for muscular nAChRs, both TCA and EGNinduce a concentration-dependent reduction in open channel duration within themicromolar range. This reduction is accompanied by a shift towards shorter durations in the main closed component. The modulation of nAChRs by these compounds is pharmacologically significant and should be considered when evaluating the therapeutic potential of TCA and EGN. Our findings provide valuable insights into how natural compounds affect Cys-loop receptors, which are underexplored but critical targets for various therapeutic strategies.
publishDate 2024
dc.date.none.fl_str_mv 2024
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info:eu-repo/semantics/conferenceObject
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status_str publishedVersion
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dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/278295
Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors; LVI Reunión Anual Asociación Argentina de Farmacología Experimental; Bahía Blanca; Argentina; 2024; 50-50
978-631-90806-0-5
CONICET Digital
CONICET
url http://hdl.handle.net/11336/278295
identifier_str_mv Molecular Insights Into Natural Compounds: Electrophysiological Effects Of Trans-Cinnamaldehyde And Eugenol On Nicotinic Acetylcholine Receptors; LVI Reunión Anual Asociación Argentina de Farmacología Experimental; Bahía Blanca; Argentina; 2024; 50-50
978-631-90806-0-5
CONICET Digital
CONICET
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dc.publisher.none.fl_str_mv Asociación Argentina de Farmacología Experimental
publisher.none.fl_str_mv Asociación Argentina de Farmacología Experimental
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