Details

Autor(en) / Beteiligte

• Vinh, Le Ba
• Kim, Jang Hoon
• Lee, Ji Sun
• Nguyet, Nguyen Thi Minh
• Yang, Seo Young
• Ma, Jin Yeul
• Kim, Young Ho

Titel

Soluble epoxide hydrolase inhibitory activity of phenolic glycosides from Polygala tenuifolia and in silico approach

Ist Teil von

• Medicinal chemistry research, 2018-03, Vol.27 (3), p.726-734

Ort / Verlag

New York: Springer US

Erscheinungsjahr

2018

Quelle

SpringerLink

Beschreibungen/Notizen

• The goal of this study was to identify soluble epoxide hydrolase (sEH) inhibitors from plants. Our efforts led to the isolation of nine phenolic glycosides 1 – 9 from the roots of Polygala tenuifolia Willd. The structures of compounds were determined by spectroscopic methods, including mass spectroscopy and one-dimensional and two-dimensional nuclear magnetic resonance, and compared with published data. All the isolated compounds were evaluated for their inhibitory activity against sEH. The IC 50 values for inhibition ranged 6.4 ± 0.4 to 27.2 ± 0.3 µM. Inhibitors 2 – 9 were confirmed the interaction with receptor as competitive type. Molecular docking demonstrated that inhibitors 2 – 9 could bind sufficiently to the right pocket. Additionally, potential inhibitors ( 5 , 6 , and 8 ) were confirmed to show the flexible movement with the protein in these sites of receptor.