Differential regulation of calcium signalling pathways by components of Piper methysticum ('Awa).
Phytother Res
; 29(4): 582-90, 2015 Apr.
Article
em En
| MEDLINE
| ID: mdl-25640812
ABSTRACT
Kava is a soporific, anxiolytic and relaxant in widespread ritual and recreational use throughout the Pacific. Traditional uses of kava by indigenous Pacific Island peoples reflect a complex pharmacopeia, centered on GABA-ergic effects of the well-characterized kavalactones. However, peripheral effects of kava suggest active components other than the CNS-targeted kavalactones. We have previously shown that immunocytes exhibit calcium mobilization in response to traditionally prepared kava extracts, and that the kavalactones do not induce these calcium responses. Here, we characterize the complex calcium-mobilizing activity of traditionally prepared and partially HPLC-purified kava extracts, noting induction of both calcium entry and store release pathways. Kava components activate intracellular store depletion of thapsigargin-sensitive and -insensitive stores that are coupled to the calcium release activated (CRAC) current, and cause calcium entry through non-store-operated pathways. Together with the pepper-like potency reported by kava users, these studies lead us to hypothesize that kava extracts contain one or more ligands for the transient receptor potential (TRP) family of ion channels. Indeed, TRP-like conductances are observed in kava-treated cells under patch clamp. Thus TRP-mediated cellular effects may be responsible for some of the reported pharmacology of kava.
Palavras-chave
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Extratos Vegetais
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Cálcio
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Sinalização do Cálcio
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Kava
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Canais de Potencial de Receptor Transitório
Limite:
Animals
Idioma:
En
Revista:
Phytother Res
Assunto da revista:
TERAPIAS COMPLEMENTARES
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Estados Unidos