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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, HanaKim, Min JungSon, Hee JinKweon, Hae JinKim, Jung TaeKim, YiseulShim, JaewonSuh, Byung ChangRhyu, Mee-Ra
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Suh, Byung Chang
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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
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
Related Researcher
  • 서병창 Suh, Byung-Chang 뇌과학과
  • Research Interests Molecular mechanisms of epilepsy and sensory pain transmission; Signaling mechanism of ion channel regulation and membrane excitability; 분자전기생리; 간질 및 통증의 분자적 기전 연구
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Department of Brain Sciences Laboratory of Brain Signal and Synapse Research 1. Journal Articles


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