Activation of transient receptor potential ankyrin 1 by quercetin and its analogs

Toshiyuki Nakamura, Noriyuki Miyoshi, Takeshi Ishii, Miyu Nishikawa, Shinichi Ikushiro, Tatsuo Watanabe

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The agonistic activity of quercetin and its analogs towards the transient receptor potential ankyrin 1 (TRPA1) has been experimentally investigated. The human TRPA1 was expressed in HEK293T cells using a tetracycline-inducible system. The activation of TRPA1 was evaluated by a fluo-4 fluorescence assay based on calcium sensing. The results of a structure-activity relationship study led to the selection of six flavonoids, all of which activated the TRPA1 channel in a dose-dependent manner. Notably, the activation of TRPA1 by these flavonoid aglycones was completely inhibited by the co-treatment of the HEK293T cells with the TRPA1-specific antagonist, HC-030031. Several flavonoid glycosides and metabolites were also evaluated, but did not activate the TRPA1 except for methylated quercetin. On the other hand, TRPV1 (vanilloid receptor) did not respond to any of the flavonoids evaluated in this study. Therefore, these data suggest that the flavonoids would be promising ligands for the TRPA1.

Original languageEnglish
Pages (from-to)949-954
Number of pages6
JournalBioscience, Biotechnology and Biochemistry
Volume80
Issue number5
DOIs
Publication statusPublished - 2016
Externally publishedYes

Keywords

  • Flavonoid
  • Metabolite
  • Quercetin
  • TRPA1

ASJC Scopus subject areas

  • Biotechnology
  • Biochemistry
  • Molecular Biology
  • Applied Microbiology and Biotechnology
  • Analytical Chemistry
  • Organic Chemistry

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