Estragole blocks neuronal excitability by direct inhibition of Na+ channels

Detalhes bibliográficos
Autor(a) principal: Silva-Alves,K.S.
Data de Publicação: 2013
Outros Autores: Ferreira-da-Silva,F.W., Peixoto-Neves,D., Viana-Cardoso,K.V., Moreira-Júnior,L., Oquendo,M.B., Oliveira-Abreu,K., Albuquerque,A.A.C., Coelho-de-Souza,A.N., Leal-Cardoso,J.H.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Medical and Biological Research
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013001201056
Resumo: Estragole is a volatile terpenoid, which occurs naturally as a constituent of the essential oils of many plants. It has several pharmacological and biological activities. The objective of the present study was to investigate the mechanism of action of estragole on neuronal excitability. Intact and dissociated dorsal root ganglion neurons of rats were used to record action potential and Na+ currents with intracellular and patch-clamp techniques, respectively. Estragole blocked the generation of action potentials in cells with or without inflexions on their descendant (repolarization) phase (Ninf and N0 neurons, respectively) in a concentration-dependent manner. The resting potentials and input resistances of Ninf and N0 cells were not altered by estragole (2, 4, and 6 mM). Estragole also inhibited total Na+ current and tetrodotoxin-resistant Na+ current in a concentration-dependent manner (IC50 of 3.2 and 3.6 mM, respectively). Kinetic analysis of Na+ current in the presence of 4 mM estragole showed a statistically significant reduction of fast and slow inactivation time constants, indicating an acceleration of the inactivation process. These data demonstrate that estragole blocks neuronal excitability by direct inhibition of Na+ channel conductance activation. This action of estragole is likely to be relevant to the understanding of the mechanisms of several pharmacological effects of this substance.
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spelling Estragole blocks neuronal excitability by direct inhibition of Na+ channelsEstragoleLocal anestheticEssential oilDorsal root gangliaPhenylpropanoidNa+ currentEstragole is a volatile terpenoid, which occurs naturally as a constituent of the essential oils of many plants. It has several pharmacological and biological activities. The objective of the present study was to investigate the mechanism of action of estragole on neuronal excitability. Intact and dissociated dorsal root ganglion neurons of rats were used to record action potential and Na+ currents with intracellular and patch-clamp techniques, respectively. Estragole blocked the generation of action potentials in cells with or without inflexions on their descendant (repolarization) phase (Ninf and N0 neurons, respectively) in a concentration-dependent manner. The resting potentials and input resistances of Ninf and N0 cells were not altered by estragole (2, 4, and 6 mM). Estragole also inhibited total Na+ current and tetrodotoxin-resistant Na+ current in a concentration-dependent manner (IC50 of 3.2 and 3.6 mM, respectively). Kinetic analysis of Na+ current in the presence of 4 mM estragole showed a statistically significant reduction of fast and slow inactivation time constants, indicating an acceleration of the inactivation process. These data demonstrate that estragole blocks neuronal excitability by direct inhibition of Na+ channel conductance activation. This action of estragole is likely to be relevant to the understanding of the mechanisms of several pharmacological effects of this substance.Associação Brasileira de Divulgação Científica2013-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013001201056Brazilian Journal of Medical and Biological Research v.46 n.12 2013reponame:Brazilian Journal of Medical and Biological Researchinstname:Associação Brasileira de Divulgação Científica (ABDC)instacron:ABDC10.1590/1414-431X20133191info:eu-repo/semantics/openAccessSilva-Alves,K.S.Ferreira-da-Silva,F.W.Peixoto-Neves,D.Viana-Cardoso,K.V.Moreira-Júnior,L.Oquendo,M.B.Oliveira-Abreu,K.Albuquerque,A.A.C.Coelho-de-Souza,A.N.Leal-Cardoso,J.H.eng2015-10-08T00:00:00Zoai:scielo:S0100-879X2013001201056Revistahttps://www.bjournal.org/https://old.scielo.br/oai/scielo-oai.phpbjournal@terra.com.br||bjournal@terra.com.br1414-431X0100-879Xopendoar:2015-10-08T00:00Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC)false
dc.title.none.fl_str_mv Estragole blocks neuronal excitability by direct inhibition of Na+ channels
title Estragole blocks neuronal excitability by direct inhibition of Na+ channels
spellingShingle Estragole blocks neuronal excitability by direct inhibition of Na+ channels
Silva-Alves,K.S.
Estragole
Local anesthetic
Essential oil
Dorsal root ganglia
Phenylpropanoid
Na+ current
title_short Estragole blocks neuronal excitability by direct inhibition of Na+ channels
title_full Estragole blocks neuronal excitability by direct inhibition of Na+ channels
title_fullStr Estragole blocks neuronal excitability by direct inhibition of Na+ channels
title_full_unstemmed Estragole blocks neuronal excitability by direct inhibition of Na+ channels
title_sort Estragole blocks neuronal excitability by direct inhibition of Na+ channels
author Silva-Alves,K.S.
author_facet Silva-Alves,K.S.
Ferreira-da-Silva,F.W.
Peixoto-Neves,D.
Viana-Cardoso,K.V.
Moreira-Júnior,L.
Oquendo,M.B.
Oliveira-Abreu,K.
Albuquerque,A.A.C.
Coelho-de-Souza,A.N.
Leal-Cardoso,J.H.
author_role author
author2 Ferreira-da-Silva,F.W.
Peixoto-Neves,D.
Viana-Cardoso,K.V.
Moreira-Júnior,L.
Oquendo,M.B.
Oliveira-Abreu,K.
Albuquerque,A.A.C.
Coelho-de-Souza,A.N.
Leal-Cardoso,J.H.
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Silva-Alves,K.S.
Ferreira-da-Silva,F.W.
Peixoto-Neves,D.
Viana-Cardoso,K.V.
Moreira-Júnior,L.
Oquendo,M.B.
Oliveira-Abreu,K.
Albuquerque,A.A.C.
Coelho-de-Souza,A.N.
Leal-Cardoso,J.H.
dc.subject.por.fl_str_mv Estragole
Local anesthetic
Essential oil
Dorsal root ganglia
Phenylpropanoid
Na+ current
topic Estragole
Local anesthetic
Essential oil
Dorsal root ganglia
Phenylpropanoid
Na+ current
description Estragole is a volatile terpenoid, which occurs naturally as a constituent of the essential oils of many plants. It has several pharmacological and biological activities. The objective of the present study was to investigate the mechanism of action of estragole on neuronal excitability. Intact and dissociated dorsal root ganglion neurons of rats were used to record action potential and Na+ currents with intracellular and patch-clamp techniques, respectively. Estragole blocked the generation of action potentials in cells with or without inflexions on their descendant (repolarization) phase (Ninf and N0 neurons, respectively) in a concentration-dependent manner. The resting potentials and input resistances of Ninf and N0 cells were not altered by estragole (2, 4, and 6 mM). Estragole also inhibited total Na+ current and tetrodotoxin-resistant Na+ current in a concentration-dependent manner (IC50 of 3.2 and 3.6 mM, respectively). Kinetic analysis of Na+ current in the presence of 4 mM estragole showed a statistically significant reduction of fast and slow inactivation time constants, indicating an acceleration of the inactivation process. These data demonstrate that estragole blocks neuronal excitability by direct inhibition of Na+ channel conductance activation. This action of estragole is likely to be relevant to the understanding of the mechanisms of several pharmacological effects of this substance.
publishDate 2013
dc.date.none.fl_str_mv 2013-12-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013001201056
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013001201056
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/1414-431X20133191
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Associação Brasileira de Divulgação Científica
publisher.none.fl_str_mv Associação Brasileira de Divulgação Científica
dc.source.none.fl_str_mv Brazilian Journal of Medical and Biological Research v.46 n.12 2013
reponame:Brazilian Journal of Medical and Biological Research
instname:Associação Brasileira de Divulgação Científica (ABDC)
instacron:ABDC
instname_str Associação Brasileira de Divulgação Científica (ABDC)
instacron_str ABDC
institution ABDC
reponame_str Brazilian Journal of Medical and Biological Research
collection Brazilian Journal of Medical and Biological Research
repository.name.fl_str_mv Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC)
repository.mail.fl_str_mv bjournal@terra.com.br||bjournal@terra.com.br
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