| Abstract |
The capacity of estrogen and stilbene derivatives to modulate the activity of superoxide dismutases in relation with their estrogenic properties has been studied. The properties of trans-resveratrol (3,5,4 -trihydroxystilbene) and its analogues, 4-hydroxystilbene, 4,4 -dihydroxystilbene, 3,5-dihydroxystilbene, 3,5,4 -trimethoxystilbene and 4,4 -dihydroxy-3,5,3 ,5 -tetramethylstilbene were compared to 17beta-estradiol and its analogues (2-methoxyestradiol, estrone, 2-hydroxyestradiol and 2-methoxyestrone). Measurement of estrogen receptor-beta (ER-beta) binding capacity was carried out by a receptor competitor assay associated with fluorescence polarisation detection. The superoxide dismutase (SOD) modulation activity was followed with a spectrophotometric assay using the sequence xanthine/xanthine oxidase-2,3-bis[2-methoxy-4-nitro-sulfo-phenyl-1-2H-tetrazolium-5-carb oxanilide (X/XO-XTT). The structure-activity relationship was different for the two series tested. In the estrogenic series, a compound which does not inhibit SOD, is recognized by the ER-p. In contrast for the stilbenic series both properties are parallel each other. (C) 2003 Elsevier B.V. All rights reserved. |
