Polygodial, a drimane sesquiterpenoid dialdehyde purified from Drimys winteri, inhibits voltage-gated sodium channels

Primer Autor
Paz, Cristian
Co-autores
Ortiz, Leandro
Deuis, Jennifer R.
Vetter, Irina
Título
Polygodial, a drimane sesquiterpenoid dialdehyde purified from Drimys winteri, inhibits voltage-gated sodium channels
Editorial
TAYLOR & FRANCIS LTD
Revista
NATURAL PRODUCT RESEARCH
Lenguaje
en
Resumen
Drimys winteri J.R.Forst. & G.Forst, a South American evergreen shrub that is used by the Mapuche people for treatment of several painful conditions, contains polygodial, a lipophilic drimane-type sesquiterpene dialdehyde with known activity at transient receptor potential channel family members including TRPA1 and TRPV1. We sought to assess the activity of polygodial at Na(V)1.7 and Na(V)1.8, two key isoforms of the voltage-gated sodium channel family involved in nociception. Polygodial was isolated from D. winteri by thin-layer chromatography and analysed structurally by 1 D and 2 D nuclear magnetic resonance (NMR) spectroscopy. Activity at heterologously expressed Na(V)1.7 and Na(V)1.8 was assessed using automated whole-cell patch-clamp electrophysiology. Here, we show that polygodial inhibits members of the voltage-gated sodium channel family, specifically Na(V)1.7 and Na(V)1.8, without changing the voltage-dependence of activation or inactivation. Activity of polygodial at voltage-gated sodium channels may contribute to the previously reported antinociceptive properties.
Tipo de Recurso
artículo original
Description
This research was funded by ANID of Chile government with the grant number Fondecyt 11181076 to CP. J.R.D. and I.V. were supported by research fellowships from the Australian National Health and Medical Research Council (APP1162503 and APP1139961).
Esta investigación fue financiada por la ANID del gobierno de Chile con el subsidio número Fondecyt 11181076 a CP. J.R.D. y I.V. fueron apoyados por becas de investigación del Consejo Nacional de Investigación Médica y de Salud de Australia (APP1162503 y APP1139961).
doi
10.1080/14786419.2022.2025592
Formato Recurso
PDF
Palabras Claves
Polygodial
analgesia
Na(V)1
8
7
patch-clamp
ACTIVATION
Ubicación del archivo
http://dx.doi.org/10.1080/14786419.2022.2025592
Categoría OCDE
Química Aplicada
Química
Medicinal
Materias
Poligodial
analgesia
Na(V)1
8
7
parche-clamp
ACTIVACIÓN
Disciplinas de la OCDE
Farmacología y Farmacia
Química Orgánica
Neurociencias
Título de la cita (Recomendado-único)
Polygodial, a drimane sesquiterpenoid dialdehyde purified from Drimys winteri, inhibits voltage-gated sodium channels
Página de inicio (Recomendado-único)
6318
Página final (Recomendado-único)
6323
Identificador del recurso (Mandatado-único)
artículo original
Versión del recurso (Recomendado-único)
version publicada
Condición de la licencia (Recomendado-repetible)
0
Derechos de acceso
metadata
Access Rights
metadata
Referencia del Financiador (Mandatado si es aplicable-repetible)
ANID-FONDECYT 11181076
NHMRC APP1162503
NHMRC APP1139961
ANID FONDECYT 11181076
Id de Web of Science
WOS:000742286700001
Colecciones
Colección Publicaciones Científicas
Colección ANID
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