Inhibition of Rat Ovarian 3.BETA.-Hydroxysteroid Dehydrogenase (3.BETA.-HSD), 17.ALPHA.-Hydroxylase and 17, 20 Lyase by Progestins and Danazol.

Satoko Arakawa, S Arakawa, Mizue Mitsuma, M Mitsuma, MASATO IYO, M Iyo, R Ohkawa, Ryoichi Ohkawa, A Kambegawa, Akira Kambegawa, Shoichi Okinaga, S Okinaga, Kiyoshi Arai, K Arai
Endocrinologia japonica · 1989 · vol. 36(3) , pp. 387–394 · doi:10.1507/endocrj1954.36.387 · PMID:2583058 · W2054696452
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Abstract

The site of action of synthetic progestins or danazol in the treatment of endometriosis is considered to be mainly the hypothalamo-pituitary level, but the direct action to the uterine endometrium and the ovary is also suggested. We investigated the effect of these synthetic steroids to rat ovarian steroidogenic enzymes. The effect of norethisterone, levonorgestrel, danazol, gestrinone, desogestrel and 3-keto-desogestrel was studied in vitro. The sources of the enzymes were prepared from ovaries of immature rats treated either with pregnant mare serum gonadotropin (PMS) and human chorionic gonadotropin (hCG) for 3 beta-hydroxy steroid dehydrogenase (3 beta-HSD), or with PMS for 17 alpha-hydroxylase and 17,20 lyase. The substrates used were pregnenolone (P5) for 3 beta-HSD, progesterone (P4) for 17 alpha-hydroxylase, and 17 alpha-hydroxy-progesterone (17 alpha-OH-P4) for 17,20 lyase. The substrates were incubated with the enzyme sources and coenzymes, and the products formed were measured. All the steroids inhibited 3 beta-HSD, and the inhibition by gestrinone (Ki = 3.0 microM) and 3-keto-desogestrel (17.5 microM) was particularly marked. Only desogestrel (Ki = 30.3 microM) and danazol (168 microM) inhibited 17 alpha-hydroxylase. All the steroids inhibited 17,20 lyase, and the inhibition by desogestrel (Ki = 0.70 microM), danazol (0.80 microM), and gestrinone (30 microM) was particularly marked.

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endometriosis

MeSH descriptors

3-Hydroxysteroid Dehydrogenases Aldehyde-Lyases Cytochrome P-450 Enzyme Inhibitors Danazol Ovary Pregnadienes Progesterone Congeners Steroid 17-alpha-Hydroxylase Steroid Hydroxylases 3-Hydroxysteroid Dehydrogenases 3-Hydroxysteroid Dehydrogenases Aldehyde-Lyases Aldehyde-Lyases Animals Cytochrome P-450 Enzyme System Cytochrome P-450 Enzyme System Danazol Female Kinetics Ovary

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