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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa

Title
Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
Authors
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
2015-05-15
Citation
PLoS ONE, 10(5)
Type
Article
Article Type
Article
Keywords
AcacetinAgastacheAgastache RugosaAnisaldehydeAnti-Inflammatory ActivityApigetrinCalcium TransportCarveolCaryophylleneCell CultureConcentration ResponseControlled StudyDrug ScreeningDrug StructureEstragoleGastrointestinal AgentLamiaceaeMenthaMethyleugenolPachypodolPhytochemistryPlant LeafPlant StemProtein ExpressionRosmarinic AcidTrans Para MethoxycinnamaldehydeTransient Receptor Potential Ankyrin1 AgonistTransient Receptor Potential Channel A1Unclassified DrugVanilloid Receptor1Vanilloid Receptor1 Antagonist
ISSN
1932-6203
Abstract
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.
URI
http://hdl.handle.net/20.500.11750/1572
DOI
10.1371/journal.pone.0127060
Publisher
Public Library of Science
Related Researcher
Files:
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Collection:
Brain and Cognitive SciencesETC1. Journal Articles


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