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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa.

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, ?-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 ?M, 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 ?M), our results suggest that these compounds from the stem and leaves of A.rugosa are specific and selective agonists of hTRPA1.

SUBMITTER: Moon H

PROVIDER: S-EPMC4433173 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature

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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa.

Moon Hana H Kim Min Jung MJ Son Hee Jin HJ Kweon Hae-Jin HJ Kim Jung Tae JT Kim Yiseul Y Shim Jaewon J Suh Byung-Chang BC Rhyu Mee-Ra MR

PloS one 20150515 5

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 impr ...[more]

PMID: 25978436

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Project description:The objective of this study was to determine the optimal dose of silver nitrate (AgNO3) for plant growth and to increase the main bioactive compounds in A. rugosa cultivated in a hydroponic system. The application of soaked diniconazole (120 μmol mol-1) to all plants at 7 days after transplanting (DAT) for dwarfing plant height, optimizing cultivation space in the plant factory. Subsequently, plants were soaked with 50, 100, 200, and 400 μmol mol-1 AgNO3 for 10 min at 25 DAT and harvested at 39 DAT. The results indicated that 200 and 400 μmol mol-1 treatments tended to severely decrease plant growth parameters compared to treatments with lower concentrations. The net photosynthetic rate was significantly reduced by the 200 and 400 μmol mol-1 treatments compared to treatments with other concentrations. The 400 μmol mol-1 treatment led to the lowest concentrations of chlorophyll a, chlorophyll a/b, total carotenoid, chlorophyll b, and the total chlorophyll. However, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity was considerably increased in 50, 100, 200, and 400 μmol mol-1 compared to that of the control plants. A higher rosmarinic acid (RA) concentration in the whole plant was noticed with the 400 μmol mol-1 treatment compared with that of the untreated plants. The 100 μmol mol-1 treatment exhibited the highest concentration and content of tilianin in the whole plant. Concentration of acacetin 1 significantly increased in the whole plant with 100 and 200 μmol mol-1 treatments compared with that of the untreated plants. Concentrations of acacetin 2 and 3 in the whole plant were the highest with 100 and 200 μmol mol-1 treatments, respectively. The results demonstrated that 100 μmol mol-1 treatments can be used to increase bioactive compounds without severely limiting the plant growth and reducing chlorophyll concentrations of A. rugosa. Implementing this optimal dose can enable growers and researchers to cultivate A. rugosa more efficiently, enhancing bioactive compound content and overall plant performance, thus harnessing the potential health benefits of this valuable plant species.

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Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa.

Publications

Five hTRPA1 Agonists Found in Indigenous Korean Mint, Agastache rugosa.

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