Title of article :
Discovery of soluble epoxide hydrolase inhibitors from natural products
Author/Authors :
Lee، نويسنده , , Gwan Ho and Oh، نويسنده , , Soo Jin and Lee، نويسنده , , Sang Yoon and Lee، نويسنده , , Ji-Yoon and Ma، نويسنده , , Jin Yeul and Kim، نويسنده , , Young Ho and Kim، نويسنده , , Sang Kyum، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2014
Pages :
6
From page :
225
To page :
230
Abstract :
With the goal of developing soluble epoxide hydrolase (sEH) inhibitors with novel chemical structures, the sEH inhibitory activities of 30 natural compounds were evaluated using both a fluorescent substrate, 3-phenyl-cyano(6-methoxy-2-naphthalenyl)methyl ester- 2-oxiraneacetic acid, and a physiological substrate, 14,15-epoxyeicosatrienoic acid. To evaluate the selectivity of sEH inhibition, the inhibition of microsomal epoxide hydrolase (mEH), which plays a critical role in detoxification of toxic epoxides, was determined using human liver microsomes. Honokiol and β-amyrin acetate, isolated from Magnolia officinalis and Acer mandshuricum, respectively, displayed strong inhibition of sEH activity, with respective IC50 values of 0.57 μM and 3.4 μM determined using the fluorescent substrate, and 1.7 μM and 6.1 μM determined using 14,15-epoxyeicosatrienoic acid. mEH activity was decreased to 49% or 61% of control activity by 25 μM honokiol or β-amyrin acetate, respectively. These results suggest that β-amyrin acetate and honokiol exhibit sEH inhibitory activity, although their sEH selectivity should be improved.
Keywords :
Soluble epoxide hydrolase , Selectivity , Honokiol , ?-Amyrin acetate
Journal title :
Food and Chemical Toxicology
Serial Year :
2014
Journal title :
Food and Chemical Toxicology
Record number :
2126760
Link To Document :
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