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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
- Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
- Moon, H[Moon, Hana]; Kim, MJ[Kim, Min Jung]; Son, HJ[Son, Hee Jin]; Kweon, HJ[Kweon, Hae-Jin]; Kim, JT[Kim, Jung Tae]; Kim, Y[Kim, Yiseul]; Shim, J[Shim, Jaewon]; Suh, B. C.[Suh, Byung Chang]; Rhyu, MR[Rhyu, Mee-Ra]
- DGIST Authors
- Kweon, HJ[Kweon, Hae-Jin]; Suh, B. C.[Suh, Byung Chang]
- Issue Date
- PLoS ONE, 10(5)
- Article Type
- Acacetin; Agastache; Agastache Rugosa; Anisaldehyde; Anti-Inflammatory Activity; Apigetrin; Calcium Transport; Carveol; Caryophyllene; Cell Culture; Concentration Response; Controlled Study; Drug Screening; Drug Structure; Estragole; Gastrointestinal Agent; Lamiaceae; Mentha; Methyleugenol; Pachypodol; Phytochemistry; Plant Leaf; Plant Stem; Protein Expression; Rosmarinic Acid; Trans Para Methoxycinnamaldehyde; Transient Receptor Potential Ankyrin1 Agonist; Transient Receptor Potential Channel A1; Unclassified Drug; Vanilloid Receptor1; Vanilloid Receptor1 Antagonist
- Transient receptor potential ankyrin1 (TRPA1) and transient receptor potential vanilloid 1 (TRPV1) are members of the TRP superfamily of structurally related, nonselective cation channels and mediators of several signaling pathways. Previously, we identified methyl syringate as an hTRPA1 agonist with efficacy against gastric emptying. The aim of this study was to find hTRPA1 and/or hTRPV1 activators in Agastache rugosa (Fisch. et Meyer) O. Kuntze (A.rugosa), commonly known as Korean mint to improve hTRPA1-related phenomena. An extract of the stem and leaves of A.rugosa (Labiatae) selectively activated hTRPA1 and hTRPV1. We next investigated the effects of commercially available compounds found in A.rugosa (acacetin, 4-allylanisole, p-anisaldehyde, apigenin 7-glucoside, L-carveol, β- caryophyllene, trans-p-methoxycinnamaldehyde, methyl eugenol, pachypodol, and rosmarinic acid) on cultured hTRPA1- and hTRPV1-expressing cells. Of the ten compounds, L-carveol, trans-p-methoxycinnamaldehyde, methyl eugenol, 4-allylanisole, and p-anisaldehyde selectively activated hTRPA1, with EC50 values of 189.1±26.8, 29.8±14.9, 160.2 ±21.9, 1535±315.7, and 546.5±73.0 μM, respectively. The activities of these compounds were effectively inhibited by the hTRPA1 antagonists, ruthenium red and HC-030031. Although the five active compounds showed weaker calcium responses than allyl isothiocyanate (EC50=7.2±1.4 μM), our results suggest that these compounds from the stem and leaves of A.rugosa are specific and selective agonists of hTRPA1. © 2015 Moon et al.
- Public Library of Science
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