Authors: C Cabot D GonzálezMartínez J A FernándezLópez M Alemany
Publish Date: 2014/03/27
Volume: 30, Issue: 5, Pages: 376-381
Abstract
Two different oral doses of oleoylestrone 1 and 10 nmol/g a day were given once to male Wistar rats the serum levels of free estrone estrone sulphate estradiol and acylestrone were measured at intervals up to 72 h after the gavage Oleoylestrone was rapidly absorbed with the 1 nmol/g dose no changes were observed in plasma acylestrone but levels increased dramatically with 10 nmol/g peaking at 6 h high acylestrone levels were maintained up to 24 h returning to normalcy at 48 h With the 10 nmol/g dose free estrone at most doubled its levels but estrone sulphate concentrations rose by one order of magnitude in both cases the increases soon 2 h reached a plateau that was maintained for almost two days Estradiol levels remained unchanged except for a transient peak at 2 h at the 10 nmol/g dose The relationship between free estrone and its sulphate was linear and those of estrone and estrone sulphate versus acylestrone showed the existence of an upper serum concentration limit for both molecules The results hint at estrone sulphate being an important metabolite of oleoylestrone disposal confirm the limited estrogenic response to oleoylestrone administration and agree with a rapid absorption and disposal of oleoylestrone nevertheless maintaining high circulating levels of the ester for a time after its oral administration
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