No inhibitory effects of gestrinone and medroxyprogesterone acetate on the estrogen production by ovaries of hypophysectomized rats stimulated by gonadotropins.
The in vivo effects of gestrinone (R2323) and medroxyprogesterone acetate (MPA) on the estrogen production by rat ovaries were investigated. Hypophysectomized immature female rats treated with 2.5 or 5 IU of pregnant mare serum gonadotropin (PMS) were daily given vehicle only, gestrinone (0.5 mg/kg body weight) or MPA (10 mg/kg body weight), and the activities of 3 beta-hydroxysteroid dehydrogenase, 17 alpha-hydroxylase, 17, 20-lyase, 17 beta-hydroxysteroid dehydrogenase and aromatase in ovaries of these rats were measured. Gestrinone suppressed the 3 beta-hydroxysteroid dehydrogenase activity and increased activities of 17 alpha-hydroxylase, 17, 20-lyase and aromatase in ovaries stimulated by 5 IU of PMS, while MPA suppressed activities of 17 alpha-hydroxylase and aromatase in these ovaries. On the other hand, the aromatase activity in ovaries stimulated by 2.5 IU of PMS was suppressed by gestrinone and increased by MPA, and neither gestrinone nor MPA affected the production of aromatizable androgens from progesterone by these ovaries. Thus, gestrinone and MPA administrated in vivo showed divergent influences on steroidogenic enzyme activities in ovaries, but they did not affect the serum concentration of estradiol-17 beta. The present results suggest that neither gestrinone nor MPA reduced estrogen production by the rat ovary under the gonadotropin stimulation although they influenced some process of its steroidogenesis.
Mizutani
T
T
Department of Obstetrics and Gynecology, Osaka University Medical School, Japan.
Sakata
M
M
Miyake
A
A
Tanizawa
O
O
Terada
N
N
Matsumoto
K
K
Terakawa
N
N
D015067:17-Hydroxysteroid Dehydrogenases / Q000096:biosynthesis; D015096:3-Hydroxysteroid Dehydrogenases / Q000096:biosynthesis; D000446:Aldehyde-Lyases / Q000096:biosynthesis; D000728:Androgens / Q000378:metabolism; D000818:Animals; D001141:Aromatase / Q000096:biosynthesis; D003577:Cytochrome P-450 Enzyme System / Q000096:biosynthesis; D004958:Estradiol / Q000096:biosynthesis* / Q000097:blood; D005260:Female; D005867:Gestrinone / Q000494:pharmacology*; D006064:Gonadotropins, Equine; D007016:Hypophysectomy; D017258:Medroxyprogesterone Acetate / Q000494:pharmacology*; D010053:Ovary / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism*; D011374:Progesterone / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013254:Steroid 17-alpha-Hydroxylase / Q000096:biosynthesis
D000728:Androgens; D006064:Gonadotropins, Equine; D005867:Gestrinone; D011374:Progesterone; D004958:Estradiol; D003577:Cytochrome P-450 Enzyme System; D017258:Medroxyprogesterone Acetate; D015067:17-Hydroxysteroid Dehydrogenases; D015096:3-Hydroxysteroid Dehydrogenases; D001141:Aromatase; D013254:Steroid 17-alpha-Hydroxylase; D000446:Aldehyde-Lyases