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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Published in:PloS one 2015-05, Vol.10 (5), p.e0127060-e0127060
Main Authors: Moon, Hana, Kim, Min Jung, Son, Hee Jin, Kweon, Hae-Jin, Kim, Jung Tae, Kim, Yiseul, Shim, Jaewon, Suh, Byung-Chang, Rhyu, Mee-Ra
Format: Article
Language:English
Subjects:
Acetanilides - pharmacology
Agastache
Agastache - chemistry
Agastache rugosa
Allyl isothiocyanate
Anisoles - pharmacology
Benzaldehydes - pharmacology
Brain research
Calcium
Calcium Channels
Calcium compounds
Capsaicin receptors
Carveol
Caryophyllene
Cell culture
Cell Line
Eugenol
Eugenol - analogs & derivatives
Eugenol - pharmacology
Food
Gastric emptying
Health aspects
HEK293 Cells
Humans
Inflammation
Isothiocyanate
Leaves
Methyl eugenol
Monoterpenes - pharmacology
Nerve Tissue Proteins - agonists
Nerve Tissue Proteins - antagonists & inhibitors
Physiological aspects
Phytochemicals
Plant Extracts - pharmacology
Plant Leaves - chemistry
Plant Stems - chemistry
Purines - pharmacology
Rosmarinic acid
Ruthenium
Ruthenium red
Ruthenium Red - pharmacology
Sesquiterpenes - pharmacology
Signaling
Stem cells
Syringate
Transient Receptor Potential Channels - agonists
Transient Receptor Potential Channels - antagonists & inhibitors
Transient receptor potential proteins
TRPA1 Cation Channel
TRPV Cation Channels - agonists
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cited_by cdi_FETCH-LOGICAL-c692t-f464227a9f8c5f4d8e8c11b1f2e21cf9d9acc38715ffc1440f3a1a532a4694483
cites cdi_FETCH-LOGICAL-c692t-f464227a9f8c5f4d8e8c11b1f2e21cf9d9acc38715ffc1440f3a1a532a4694483
container_end_page e0127060
container_issue 5
container_start_page e0127060
container_title PloS one
container_volume 10
creator Moon, Hana
Kim, Min Jung
Son, Hee Jin
Kweon, Hae-Jin
Kim, Jung Tae
Kim, Yiseul
Shim, Jaewon
Suh, Byung-Chang
Rhyu, Mee-Ra
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 (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.
doi_str_mv 10.1371/journal.pone.0127060
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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. 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Kim, Min Jung ; Son, Hee Jin ; Kweon, Hae-Jin ; Kim, Jung Tae ; Kim, Yiseul ; Shim, Jaewon ; Suh, Byung-Chang ; Rhyu, Mee-Ra</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c692t-f464227a9f8c5f4d8e8c11b1f2e21cf9d9acc38715ffc1440f3a1a532a4694483</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Acetanilides - pharmacology</topic><topic>Agastache</topic><topic>Agastache - chemistry</topic><topic>Agastache rugosa</topic><topic>Allyl isothiocyanate</topic><topic>Anisoles - pharmacology</topic><topic>Benzaldehydes - pharmacology</topic><topic>Brain research</topic><topic>Calcium</topic><topic>Calcium Channels</topic><topic>Calcium compounds</topic><topic>Capsaicin receptors</topic><topic>Carveol</topic><topic>Caryophyllene</topic><topic>Cell culture</topic><topic>Cell Line</topic><topic>Eugenol</topic><topic>Eugenol - analogs &amp; derivatives</topic><topic>Eugenol - pharmacology</topic><topic>Food</topic><topic>Gastric emptying</topic><topic>Health aspects</topic><topic>HEK293 Cells</topic><topic>Humans</topic><topic>Inflammation</topic><topic>Isothiocyanate</topic><topic>Leaves</topic><topic>Methyl eugenol</topic><topic>Monoterpenes - pharmacology</topic><topic>Nerve Tissue Proteins - agonists</topic><topic>Nerve Tissue Proteins - antagonists &amp; 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Allied Health Database (Alumni Edition)</collection><collection>Meteorological &amp; Geoastrophysical Abstracts - Academic</collection><collection>ProQuest Engineering Collection</collection><collection>ProQuest Biological Science Collection</collection><collection>Agriculture Science Database</collection><collection>Health &amp; Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>ProQuest Biological Science Journals</collection><collection>Engineering Database</collection><collection>Nursing &amp; Allied Health Premium</collection><collection>ProQuest advanced technologies &amp; aerospace journals</collection><collection>ProQuest Advanced Technologies &amp; Aerospace Collection</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Environmental Science Database</collection><collection>Materials science collection</collection><collection>Publicly Available Content Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>Engineering collection</collection><collection>Environmental Science Collection</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><collection>DOAJ Directory of Open Access Journals</collection><jtitle>PloS one</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Moon, Hana</au><au>Kim, Min Jung</au><au>Son, Hee Jin</au><au>Kweon, Hae-Jin</au><au>Kim, Jung Tae</au><au>Kim, Yiseul</au><au>Shim, Jaewon</au><au>Suh, Byung-Chang</au><au>Rhyu, Mee-Ra</au><au>Simon, Sidney Arthur</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa</atitle><jtitle>PloS one</jtitle><addtitle>PLoS One</addtitle><date>2015-05-15</date><risdate>2015</risdate><volume>10</volume><issue>5</issue><spage>e0127060</spage><epage>e0127060</epage><pages>e0127060-e0127060</pages><issn>1932-6203</issn><eissn>1932-6203</eissn><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.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>25978436</pmid><doi>10.1371/journal.pone.0127060</doi><oa>free_for_read</oa></addata></record>
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identifier ISSN: 1932-6203
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issn 1932-6203
1932-6203
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subjects Acetanilides - pharmacology
Agastache
Agastache - chemistry
Agastache rugosa
Allyl isothiocyanate
Anisoles - pharmacology
Benzaldehydes - pharmacology
Brain research
Calcium
Calcium Channels
Calcium compounds
Capsaicin receptors
Carveol
Caryophyllene
Cell culture
Cell Line
Eugenol
Eugenol - analogs & derivatives
Eugenol - pharmacology
Food
Gastric emptying
Health aspects
HEK293 Cells
Humans
Inflammation
Isothiocyanate
Leaves
Methyl eugenol
Monoterpenes - pharmacology
Nerve Tissue Proteins - agonists
Nerve Tissue Proteins - antagonists & inhibitors
Physiological aspects
Phytochemicals
Plant Extracts - pharmacology
Plant Leaves - chemistry
Plant Stems - chemistry
Purines - pharmacology
Rosmarinic acid
Ruthenium
Ruthenium red
Ruthenium Red - pharmacology
Sesquiterpenes - pharmacology
Signaling
Stem cells
Syringate
Transient Receptor Potential Channels - agonists
Transient Receptor Potential Channels - antagonists & inhibitors
Transient receptor potential proteins
TRPA1 Cation Channel
TRPV Cation Channels - agonists
title Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa
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