The effects of in vivo administration of 10-propargylestr-4-ene-3,17-dione on rat ovarian aromatase and estrogen levels

Journal of Enzyme Inhibition
M E BrandtS J Zimniski

Abstract

We have previously demonstrated that 10-propargylestr-4-ene-3,17-dione (PED) functioned as an irreversible inhibitor of rat ovarian aromatase in vitro. These studies were undertaken to examine the in vivo effects of PED on rat ovarian aromatase activity and estrogen production. In the current experiments, a single injection of PED (0.5 or 2.5 mg/kg) was found to maximally inhibit aromatase at 3 h regardless of dose. Significant inhibition of enzyme activity by PED was observed beyond 18 h, although some recovery was noted at the lower dose (0.5 mg/kg). Concomitantly, ovarian estrogen levels were also maximally reduced at 3 h, however ovarian estrogen levels returned toward control values prior to the recovery in enzyme activity. Even though significant inhibition of enzyme activity was observed at 12 h following a single injection of PED, the effect of double injections of the inhibitor at 12 h intervals was surprisingly not cumulative. Similarly, continued multiple injections of PED revealed significant inhibition of enzyme activity and estrogen production several hours after the injection, but variations in effectiveness were observed by 12 h which changed in accordance with a circannual cycle in aromatase. Apparently other f...Continue Reading

References

Jan 1, 1986·Critical Reviews in Oncology/hematology·A M Brodie, R J Santen
Dec 1, 1986·American Journal of Obstetrics and Gynecology·J R Schreiber, G S diZerega
Sep 15, 1985·Biochemical Pharmacology·A M Brodie

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Citations

Mar 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·R WhomsleyV Pestellini

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