1. The Inhibition Activity of Natural Methoxyflavonoid from Inula britannica on Soluble Epoxide Hydrolase and NO Production in RAW264.7 Cells.
- Author
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Kim JH, Han KS, Lee ES, Kim YG, Kim YI, Cho BO, and Lee IS
- Subjects
- Animals, Mice, RAW 264.7 Cells, Enzyme Inhibitors pharmacology, Enzyme Inhibitors chemistry, Molecular Docking Simulation, Kinetics, Anti-Inflammatory Agents pharmacology, Anti-Inflammatory Agents chemistry, Flowers chemistry, Epoxide Hydrolases antagonists & inhibitors, Epoxide Hydrolases metabolism, Nitric Oxide metabolism, Flavonoids pharmacology, Flavonoids chemistry, Flavonoids isolation & purification, Inula chemistry
- Abstract
Soluble epoxide hydrolase (sEH) is an enzyme targeted for the treatment of inflammation and cardiovascular diseases. Activated inflammatory cells produce nitric oxide (NO), which induces oxidative stress and exacerbates inflammation. We identify an inhibitor able to suppress sEH and thus NO production. Five flavonoids 1 - 5 isolated from Inula britannica flowers were evaluated for their abilities to inhibit sEH with IC
50 values of 12.1 ± 0.1 to 62.8 ± 1.8 µM and for their effects on enzyme kinetics. A simulation study using computational chemistry was conducted as well. Furthermore, five inhibitors ( 1 - 5 ) were confirmed to suppress NO levels at 10 µM. The results showed that flavonoids 1 - 5 exhibited inhibitory activity in all tests, with compound 3 exhibiting the most significant efficacy. Thus, in the development of anti-inflammatory inhibitors, compound 3 is a promising natural candidate.- Published
- 2024
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