Soluble Epoxide Hydrolase Inhibitory Activity of Selaginellin Derivatives from Selaginella tamariscina

Molecules

Jang Hoon Kim²  Chong Woon Cho²  Bui Huu Tai²  Seo Young Yang²  Gug-seoun Choi¹  Jong Seong Kang²  Young Ho Kim² 

[1] Department of Horticultural Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju-gun, Jeollabuk-do 595-890, Korea;College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea;

关键词: Selaginella tamariscina;    Selaginellaceae;    selaginellin;    soluble epoxide hydrolase;    non-competitive inhibition;   

DOI  :  10.3390/molecules201219774

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.