Estragole blocks neuronal excitability by direct inhibition of Na+ channels
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , , , , |
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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Brazilian Journal of Medical and Biological Research |
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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 |
_version_ |
1754302942483054592 |