Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i>
Soluble epoxide hydrolase (sEH) is a target enzyme for the treatment of inflammation and cardiovascular disease. A <i>Glycyrrhiza uralensis</i> extract exhibited ~50% inhibition of sEH at 100 μg/mL, and column chromatography yielded compounds <b>1</b>–<b>11</b>. I...
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MDPI AG
2023-03-01
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author | Jang Hoon Kim Yun-Chan Huh Mok Hur Woo Tae Park Youn-Ho Moon Tae Il Kim Yong Il Kim Seon Mi Kim Jeonghoon Lee Ik Soo Lee |
author_facet | Jang Hoon Kim Yun-Chan Huh Mok Hur Woo Tae Park Youn-Ho Moon Tae Il Kim Yong Il Kim Seon Mi Kim Jeonghoon Lee Ik Soo Lee |
author_sort | Jang Hoon Kim |
collection | DOAJ |
description | Soluble epoxide hydrolase (sEH) is a target enzyme for the treatment of inflammation and cardiovascular disease. A <i>Glycyrrhiza uralensis</i> extract exhibited ~50% inhibition of sEH at 100 μg/mL, and column chromatography yielded compounds <b>1</b>–<b>11</b>. Inhibitors <b>1</b>, <b>4</b>–<b>6</b>, <b>9</b>, and <b>11</b> were non-competitive; inhibitors <b>3, 7</b>, <b>8</b>, and <b>10</b> were competitive. The IC<sub>50</sub> value of inhibitor <b>10</b> was below 2 μM. Molecular simulation was used to identify the sEH binding site. Glycycoumarin (<b>10</b>) requires further evaluation in cells and animals. |
first_indexed | 2024-03-11T05:34:57Z |
format | Article |
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institution | Directory Open Access Journal |
issn | 1661-6596 1422-0067 |
language | English |
last_indexed | 2024-03-11T05:34:57Z |
publishDate | 2023-03-01 |
publisher | MDPI AG |
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series | International Journal of Molecular Sciences |
spelling | doaj.art-79daaf98695c4ede9a1c4236f70ec72c2023-11-17T16:51:45ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-03-01247648510.3390/ijms24076485Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i>Jang Hoon Kim0Yun-Chan Huh1Mok Hur2Woo Tae Park3Youn-Ho Moon4Tae Il Kim5Yong Il Kim6Seon Mi Kim7Jeonghoon Lee8Ik Soo Lee9Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaDepartment of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Republic of KoreaKm Covergence Research Division, Korea Institute of Oriental Medicien, Daejeon 34134, Republic of KoreaSoluble epoxide hydrolase (sEH) is a target enzyme for the treatment of inflammation and cardiovascular disease. A <i>Glycyrrhiza uralensis</i> extract exhibited ~50% inhibition of sEH at 100 μg/mL, and column chromatography yielded compounds <b>1</b>–<b>11</b>. Inhibitors <b>1</b>, <b>4</b>–<b>6</b>, <b>9</b>, and <b>11</b> were non-competitive; inhibitors <b>3, 7</b>, <b>8</b>, and <b>10</b> were competitive. The IC<sub>50</sub> value of inhibitor <b>10</b> was below 2 μM. Molecular simulation was used to identify the sEH binding site. Glycycoumarin (<b>10</b>) requires further evaluation in cells and animals.https://www.mdpi.com/1422-0067/24/7/6485<i>Glycyrrhiza uralensis</i>soluble epoxide hydrolasecompetitive inhibitornoncompetitive inhibitor |
spellingShingle | Jang Hoon Kim Yun-Chan Huh Mok Hur Woo Tae Park Youn-Ho Moon Tae Il Kim Yong Il Kim Seon Mi Kim Jeonghoon Lee Ik Soo Lee Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> International Journal of Molecular Sciences <i>Glycyrrhiza uralensis</i> soluble epoxide hydrolase competitive inhibitor noncompetitive inhibitor |
title | Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> |
title_full | Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> |
title_fullStr | Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> |
title_full_unstemmed | Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> |
title_short | Inhibition of Soluble Epoxide Hydrolase Activity by Components of <i>Glycyrrhiza uralensis</i> |
title_sort | inhibition of soluble epoxide hydrolase activity by components of i glycyrrhiza uralensis i |
topic | <i>Glycyrrhiza uralensis</i> soluble epoxide hydrolase competitive inhibitor noncompetitive inhibitor |
url | https://www.mdpi.com/1422-0067/24/7/6485 |
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