Cargando…

α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice

α-Spinasterol is a plant-derived compound which was reported to act as a selective antagonist for the transient receptor potential vanilloid 1 (TRPV1) receptor. Several studies revealed that the TRPV1 receptors might modulate seizure activity in animal models of seizures and epilepsy. The aim of the...

Descripción completa

Detalles Bibliográficos
Autores principales: Socała, Katarzyna, Nieoczym, Dorota, Pieróg, Mateusz, Wlaź, Piotr
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer Vienna 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4540766/
https://www.ncbi.nlm.nih.gov/pubmed/25764210
http://dx.doi.org/10.1007/s00702-015-1391-7
_version_ 1782386283816943616
author Socała, Katarzyna
Nieoczym, Dorota
Pieróg, Mateusz
Wlaź, Piotr
author_facet Socała, Katarzyna
Nieoczym, Dorota
Pieróg, Mateusz
Wlaź, Piotr
author_sort Socała, Katarzyna
collection PubMed
description α-Spinasterol is a plant-derived compound which was reported to act as a selective antagonist for the transient receptor potential vanilloid 1 (TRPV1) receptor. Several studies revealed that the TRPV1 receptors might modulate seizure activity in animal models of seizures and epilepsy. The aim of the present study was to investigate the effect of α-spinasterol on the seizure threshold in three acute models of seizures, i.e., in the intravenous (i.v.) pentylenetetrazole (PTZ) seizure test, in the maximal electroshock seizure threshold (MEST) test and in the model of psychomotor seizures induced by 6 Hz stimulation in mice. Our results revealed significant anticonvulsant effect of α-spinasterol in all the used seizure tests. In the i.v. PTZ test, statistically significant elevation was noted in case of the threshold for myoclonic twitches (doses of 0.1–1 mg/kg) and generalized clonus seizures (doses of 0.5 and 1 mg/kg) but not for tonic seizures. The studied TRPV1 antagonist also increased the threshold for tonic hindlimb extension in the MEST (doses of 0.5 and 1 mg/kg) and 6 Hz psychomotor seizure (doses of 0.1 and 0.5 mg/kg) tests in mice. Furthermore, α-spinasterol did not produce any significant impairment of motor coordination (assessed in the chimney test) and muscular strength (investigated in the grip-strength test) and it did not provoke significant changes in body temperature in mice. Based on the results of our study and the fact that α-spinasterol is characterized by good blood–brain permeability, we postulate further investigation of this compound to precisely evaluate mechanism of its anticonvulsant action and opportunity of its usage in clinical practice.
format Online
Article
Text
id pubmed-4540766
institution National Center for Biotechnology Information
language English
publishDate 2015
publisher Springer Vienna
record_format MEDLINE/PubMed
spelling pubmed-45407662015-08-21 α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice Socała, Katarzyna Nieoczym, Dorota Pieróg, Mateusz Wlaź, Piotr J Neural Transm (Vienna) Translational Neurosciences - Original Article α-Spinasterol is a plant-derived compound which was reported to act as a selective antagonist for the transient receptor potential vanilloid 1 (TRPV1) receptor. Several studies revealed that the TRPV1 receptors might modulate seizure activity in animal models of seizures and epilepsy. The aim of the present study was to investigate the effect of α-spinasterol on the seizure threshold in three acute models of seizures, i.e., in the intravenous (i.v.) pentylenetetrazole (PTZ) seizure test, in the maximal electroshock seizure threshold (MEST) test and in the model of psychomotor seizures induced by 6 Hz stimulation in mice. Our results revealed significant anticonvulsant effect of α-spinasterol in all the used seizure tests. In the i.v. PTZ test, statistically significant elevation was noted in case of the threshold for myoclonic twitches (doses of 0.1–1 mg/kg) and generalized clonus seizures (doses of 0.5 and 1 mg/kg) but not for tonic seizures. The studied TRPV1 antagonist also increased the threshold for tonic hindlimb extension in the MEST (doses of 0.5 and 1 mg/kg) and 6 Hz psychomotor seizure (doses of 0.1 and 0.5 mg/kg) tests in mice. Furthermore, α-spinasterol did not produce any significant impairment of motor coordination (assessed in the chimney test) and muscular strength (investigated in the grip-strength test) and it did not provoke significant changes in body temperature in mice. Based on the results of our study and the fact that α-spinasterol is characterized by good blood–brain permeability, we postulate further investigation of this compound to precisely evaluate mechanism of its anticonvulsant action and opportunity of its usage in clinical practice. Springer Vienna 2015-03-13 2015 /pmc/articles/PMC4540766/ /pubmed/25764210 http://dx.doi.org/10.1007/s00702-015-1391-7 Text en © The Author(s) 2015 https://creativecommons.org/licenses/by/4.0/ Open AccessThis article is distributed under the terms of the Creative Commons Attribution License which permits any use, distribution, and reproduction in any medium, provided the original author(s) and the source are credited.
spellingShingle Translational Neurosciences - Original Article
Socała, Katarzyna
Nieoczym, Dorota
Pieróg, Mateusz
Wlaź, Piotr
α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title_full α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title_fullStr α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title_full_unstemmed α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title_short α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
title_sort α-spinasterol, a trpv1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice
topic Translational Neurosciences - Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4540766/
https://www.ncbi.nlm.nih.gov/pubmed/25764210
http://dx.doi.org/10.1007/s00702-015-1391-7
work_keys_str_mv AT socałakatarzyna aspinasterolatrpv1receptorantagonistelevatestheseizurethresholdinthreeacuteseizuretestsinmice
AT nieoczymdorota aspinasterolatrpv1receptorantagonistelevatestheseizurethresholdinthreeacuteseizuretestsinmice
AT pierogmateusz aspinasterolatrpv1receptorantagonistelevatestheseizurethresholdinthreeacuteseizuretestsinmice
AT wlazpiotr aspinasterolatrpv1receptorantagonistelevatestheseizurethresholdinthreeacuteseizuretestsinmice