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KMID : 0620720150210030176
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Natural Product Sciences
2015 Volume.21 No. 3 p.176 ~ p.184
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Soluble Epoxide Hydrolase Inhibitory Activity from Euphorbia supina Rafin
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Bui Thi Thuy Luyen
Nguyen Phuong Thao
Bui Huu Tai
Le Duc Dat
Kim Ji-Eun
Kim Young-Ho
Kwon Se-Uk
Lee Young-Mi
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Abstract
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In our search for natural soluble epoxide hydrolase (sEH) inhibitors from plants, an extract of the dried whole plants of Euphorbia supina Rafin was found to significantly inhibit sEH activity in vitro. Phytochemical investigation of E. supina resulted in isolation of 17 compounds (1 - 17), including triterpenes (1 - 4), phenolic compounds (5 - 8), and flavonoid derivatives (9 - 17). The structures of the isolated compounds were established mainly by extensive analysis of the 1D and 2D NMR, and MS data. All of the isolated compounds were evaluated for their sEH inhibitory activity. Among the isolated phenolic compounds, 8 was identified as a significant inhibitor of sEH, with an IC50 value of 15.4 ± 1.3 μM. Additionally, a kinetic analysis of isolated compounds (2, 5, 8 - 11, 13, and 17) indicated that the inhibitory effects of flavonoid derivatives 10 and 11 were of mixed-type, with inhibitory constants (Ki) ranging from 3.6 ± 0.8 to 21.8 ± 1.0 μM, whereas compounds 2, 5, 8, 9, 13, and 17 were non-competitive inhibitors with inhibition Ki values ranging from 3.3 ± 0.2 to 39.5 ± 0.0 μM.
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KEYWORD
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Euphorbia supina, Euphorbiaceae, Soluble epoxide hydrolase
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