Soluble epoxide hydrolase inhibitory activity of selaginellin derivatives from selaginella tamariscina

Jang Hoon Kim; Chong Woon Cho; Bui Huu Tai; Seo Young Yang; Gug Seoun Choi; Jong Seong Kang; Young Ho Kim; Derek J. McPhee

doi:10.3390/molecules201219774

Soluble epoxide hydrolase inhibitory activity of selaginellin derivatives from selaginella tamariscina

Jang Hoon Kim, Chong Woon Cho, Bui Huu Tai, Seo Young Yang, Gug Seoun Choi, Jong Seong Kang, Young Ho Kim, Derek J. McPhee

Department of Biology Education

Research output: Contribution to journal › Article › peer-review

23 Scopus citations

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.

Original language	English
Pages (from-to)	21405-21414
Number of pages	10
Journal	Molecules
Volume	20
Issue number	12
DOIs	https://doi.org/10.3390/molecules201219774
State	Published - 2 Dec 2015

Keywords

Non-competitive inhibition
Selaginella tamariscina
Selaginellaceae
Selaginellin
Soluble epoxide hydrolase

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/molecules201219774

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@article{d930014c7d304c7ba1fe9acc5756ee8c,

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.",

keywords = "Non-competitive inhibition, Selaginella tamariscina, Selaginellaceae, Selaginellin, Soluble epoxide hydrolase",

author = "Kim, {Jang Hoon} and Cho, {Chong Woon} and Tai, {Bui Huu} and Yang, {Seo Young} and Choi, {Gug Seoun} and Kang, {Jong Seong} and Kim, {Young Ho} and McPhee, {Derek J.}",

note = "Publisher Copyright: {\textcopyright} 2015 by the authors.",

year = "2015",

month = dec,

day = "2",

doi = "10.3390/molecules201219774",

language = "English",

volume = "20",

pages = "21405--21414",

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T1 - Soluble epoxide hydrolase inhibitory activity of selaginellin derivatives from selaginella tamariscina

AU - Kim, Jang Hoon

AU - Cho, Chong Woon

AU - Tai, Bui Huu

AU - Yang, Seo Young

AU - Choi, Gug Seoun

AU - Kang, Jong Seong

AU - Kim, Young Ho

AU - McPhee, Derek J.

PY - 2015/12/2

Y1 - 2015/12/2

N2 - 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.

AB - 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.

KW - Non-competitive inhibition

KW - Selaginella tamariscina

KW - Selaginellaceae

KW - Selaginellin

KW - Soluble epoxide hydrolase

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U2 - 10.3390/molecules201219774

DO - 10.3390/molecules201219774

M3 - Article

C2 - 26633335

AN - SCOPUS:84954341924

SN - 1420-3049

VL - 20

SP - 21405

EP - 21414

JO - Molecules

JF - Molecules

IS - 12

ER -

Soluble epoxide hydrolase inhibitory activity of selaginellin derivatives from selaginella tamariscina

Abstract

Keywords

UN SDGs

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