2-methoxyestrone and 16-hydroxyestrone

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.

Topics: 2-Methoxyestradiol; Cells, Cultured; Endothelium, Vascular; Epoprostenol; Estradiol; Estrone; Humans; Hydroxyestrones

The main estradiol metabolites 2-hydroxyestrone, 2-methoxyestrone and 16alpha-hydroxyestrone were investigated in vitro for the susceptibility of low density lipoprotein to oxidation and the effects compared with those of estradiol and vitamin E. 2-hydroxyestrone and 2-methoxyestrone had a greater inhibitory effect than estradiol and vitamin E whereas 16alpha-hydroxyestrone approximates the inhibition of estradiol. These results indicate that 2-hydroxyestrone and 2-methoxyestrone possess non-genomic actions which may play a role in the lipid metabolism.

Topics: Estradiol; Estrogens, Catechol; Humans; Hydroxyestrones; Kinetics; Lipoproteins, LDL; Oxidation-Reduction; Vitamin E

Humans with SLE were studied with regard to their ability to metabolize estradiol and testosterone. Significant abnormalities in the patterns of metabolism of both classes of sex steroids were found. Estradiol hydroxylation at C-16 was more extensive in both males and females with SLE -- leading to more estrogenic metabolites; and testosterone oxidation was elevated in patients with SLE resulting in a decrease in total androgens. Some normal first degree relatives of patients with SLE also had abnormalities of estradiol hydroxylation.

Topics: Estradiol; Estriol; Estrone; Female; Humans; Hydroxyestrones; Hydroxylation; Lupus Erythematosus, Systemic; Male; Oxidation-Reduction; Testosterone