title: Soluble Epoxide Hydrolase Inhibitory Activity of Selaginellin Derivatives from Selaginella tamariscina.
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.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. oasis5325@lycos.co.kr.|Department of Horticultural Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju-gun, Jeollabuk-do 595-890, Korea. oasis5325@lycos.co.kr.
authors.forename: Jang Hoon
authors.initials: JH
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. chongw113@cnu.ac.kr.
authors.forename: Chong Woon
authors.initials: CW
authors.lastname: Cho
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. bhtaiich@gmail.com.|Institute of Marine Biochemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Caugiay, Hanoi 364-545, Vietnam. bhtaiich@gmail.com.
authors.forename: Bui Huu
authors.initials: BH
authors.lastname: Tai
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. ysy1008@chol.com.
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Yang
authors.affiliation: Department of Horticultural Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju-gun, Jeollabuk-do 595-890, Korea. choigs@korea.kr.
authors.forename: Gug-Seoun
authors.initials: GS
authors.lastname: Choi
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. kangjss@cnu.ac.kr.
authors.forename: Jong Seong
authors.initials: JS
authors.lastname: Kang
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. yhk@cnu.ac.kr.
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D003512:Cyclohexanones / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors*; D006801:Humans; D015394:Molecular Structure; D010936:Plant Extracts / Q000494:pharmacology*; D032503:Selaginellaceae / Q000737:chemistry*
chemical_list: D003512:Cyclohexanones; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D004851:Epoxide Hydrolases
keywords: Selaginella tamariscina; Selaginellaceae; non-competitive inhibition; selaginellin; soluble epoxide hydrolase