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Open AccessArticle

Soluble Epoxide Hydrolase Inhibitory Activity of Selaginellin Derivatives from Selaginella tamariscina

1
College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea
2
Department of Horticultural Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju-gun, Jeollabuk-do 595-890, Korea
3
Institute of Marine Biochemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Caugiay, Hanoi 364-545, Vietnam
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Derek J. McPhee
Molecules 2015, 20(12), 21405-21414; https://doi.org/10.3390/molecules201219774
Received: 23 October 2015 / Revised: 23 November 2015 / Accepted: 26 November 2015 / Published: 2 December 2015
(This article belongs to the Section Bioorganic Chemistry)
Selaginellin derivatives 13 isolated from Selaginella tamariscina were evaluated for their inhibition of soluble epoxide hydrolase (sEH) to demonstrate their potential for the treatment of cardiovascular disease. All selaginellin derivatives (13) inhibited sEH enzymatic activity and PHOME hydrolysis, in a dose-dependent manner, with IC50 values of 3.1 ± 0.1, 8.2 ± 2.2, and 4.2 ± 0.2 μM, respectively. We further determined that the derivatives function as non-competitive inhibitors. Moreover, the predicted that binding sites and interaction between 13 and sEH were solved by docking simulations. According to quantitative analysis, 13 were confirmed to have high content in the roots of S. tamariscina; among them, selaginellin 3 exhibited the highest content of 189.3 ± 0.0 μg/g. View Full-Text
Keywords: Selaginella tamariscina; Selaginellaceae; selaginellin; soluble epoxide hydrolase; non-competitive inhibition Selaginella tamariscina; Selaginellaceae; selaginellin; soluble epoxide hydrolase; non-competitive inhibition
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Kim, J.H.; Cho, C.W.; Tai, B.H.; Yang, S.Y.; Choi, G.-S.; Kang, J.S.; Kim, Y.H. Soluble Epoxide Hydrolase Inhibitory Activity of Selaginellin Derivatives from Selaginella tamariscina. Molecules 2015, 20, 21405-21414.

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