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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa

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 wit...

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Autores principales: Moon, Hana, Kim, Min Jung, Son, Hee Jin, Kweon, Hae-Jin, Kim, Jung Tae, Kim, Yiseul, Shim, Jaewon, Suh, Byung-Chang, Rhyu, Mee-Ra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4433173/
https://www.ncbi.nlm.nih.gov/pubmed/25978436
http://dx.doi.org/10.1371/journal.pone.0127060
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author Moon, Hana
Kim, Min Jung
Son, Hee Jin
Kweon, Hae-Jin
Kim, Jung Tae
Kim, Yiseul
Shim, Jaewon
Suh, Byung-Chang
Rhyu, Mee-Ra
author_facet Moon, Hana
Kim, Min Jung
Son, Hee Jin
Kweon, Hae-Jin
Kim, Jung Tae
Kim, Yiseul
Shim, Jaewon
Suh, Byung-Chang
Rhyu, Mee-Ra
author_sort Moon, Hana
collection PubMed
description 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 (EC(50)=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.
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spelling pubmed-44331732015-05-27 Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa Moon, Hana Kim, Min Jung Son, Hee Jin Kweon, Hae-Jin Kim, Jung Tae Kim, Yiseul Shim, Jaewon Suh, Byung-Chang Rhyu, Mee-Ra PLoS One Research Article 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 (EC(50)=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. Public Library of Science 2015-05-15 /pmc/articles/PMC4433173/ /pubmed/25978436 http://dx.doi.org/10.1371/journal.pone.0127060 Text en © 2015 Moon et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Moon, Hana
Kim, Min Jung
Son, Hee Jin
Kweon, Hae-Jin
Kim, Jung Tae
Kim, Yiseul
Shim, Jaewon
Suh, Byung-Chang
Rhyu, Mee-Ra
Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title_full Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title_fullStr Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title_full_unstemmed Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title_short Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
title_sort five htrpa1 agonists found in indigenous korean mint, agastache rugosa
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4433173/
https://www.ncbi.nlm.nih.gov/pubmed/25978436
http://dx.doi.org/10.1371/journal.pone.0127060
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