Soluble Epoxide Hydrolase Inhibitory Activity of Selaginellin Derivatives from Selaginella tamariscinaReport as inadecuate




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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



These authors contributed equally to this work.





*

Authors to whom correspondence should be addressed.



Academic Editor: Derek J. McPhee

Abstract Selaginellin derivatives 1–3 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 1–3 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 1–3 and sEH were solved by docking simulations. According to quantitative analysis, 1–3 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





Author: Jang Hoon Kim 1,2,†, Chong Woon Cho 1,†, Bui Huu Tai 1,3, Seo Young Yang 1, Gug-seoun Choi 2, Jong Seong Kang 1,* and Young Ho Kim 1,*

Source: http://mdpi.com/



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