Effect of estradiol metabolites on prostacyclin synthesis in human endothelial cell cultures.
Estradiol can stimulate prostacyclin production in the vessel wall, thereby eliciting vasodilatation. In the present work the effect of the estradiol metabolites estrone, 2-methoxyestrone, 2-methoxyestradiol, and 16alpha-hydroxyestrone were investigated to find out if they are also able to stimulate prostacyclin synthesis. All metabolites triggered an increase of prostacyclin synthesis in human endothelial cells starting at a concentration of 10(-9) M. The parent substance, 17beta-estradiol, accomplished this effect only starting at a concentration of 10(-8) M. These results indicate that estradiol metabolites may take part in the estradiol-induced vasodilatation in vivo.
Seeger
H
H
Department of Obstetrics and Gynecology, University Tuebingen, Germany.
Mueck
A O
AO
Lippert
T H
TH
D000077584:2-Methoxyestradiol; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000378:metabolism*; D011464:Epoprostenol / Q000096:biosynthesis*; D004958:Estradiol / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D004970:Estrone / Q000494:pharmacology; D006801:Humans; D006894:Hydroxyestrones / Q000494:pharmacology
D006894:Hydroxyestrones; C026702:16-hydroxyestrone; D004970:Estrone; D004958:Estradiol; D000077584:2-Methoxyestradiol; D011464:Epoprostenol; C003655:2-methoxyestrone