期刊
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
卷 158, 期 -, 页码 1362-1368出版社
ELSEVIER
DOI: 10.1016/j.ijbiomac.2020.04.227
关键词
Soluble epoxide hydrolase; Kinetics; Molecular stimulation
资金
- National Natural Science Foundation of China [81703769]
- National Key Research and Development Program of China [2018YFC1705900]
- National Science and Technology Major Project of the Ministry of Science and Technology of the People's Republic of China [2018ZX09735005]
- Liaoning Provincial Key Research and Development Program [2019JH2/10300022]
- Liaoning Revitalization Talents Program
- Dalian Young Star of Science and Technology
The inhibition of soluble epoxide hydrolase (sEH) is regarded as a promising therapeutic approach to treat in-flammation and its related disorders. In present work, we investigated inhibitory effects of forty-nine kinds of tra-ditional Chinese medicines against sEH. Inula helenium showed significant inhibitory effect against sEH, and the extract of I. helenium was isolated to obtain eight compounds, including 4H-tomentosin (1), xanthalongin (2), linoleic acid (3), 8-hydroxy-9-isobutyryloxy-10(2)-methylbutyrylthymol (4), dehydrocostus lactone (5), alantolactone (6), costunolide (7), and isoalantolactone (8). Among them, 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) showed significantly inhibitory activities on sEH with half maximal inhibitory concen-tration (IC50) from 5.88 +/- 0.97 mu M to 11.63 +/- 0.58 mu M. The inhibition kinetics suggested that 4H-tomentosin (1) and xanthalongin (2) were mixed-competitive type inhibitors with inhibition constants (K-i) of 7.02 and 6.57 mu M, respectively, and linoleic acid (3) was a competitive type inhibitor with a K-i values of 3.52 mu M. The po-tential interactions of 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) with sEH were analyzed by mo-lecular docking, which indicated that these bioactive compounds had interactions with key amino acid residues Tyr343, Ile363, Tyr383, and His524. (C) 2020 Elsevier B.V. All rights reserved.
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