Abstract
Progesterone, 5-pregnene-3,20-dione, and desoxycorticosterone were found to be partial but significant inhibitors of estrone-induced growth of the uterus of hypophysectomized rats but they did not depress the amount of growth elicited by testosterone. The presence of both the 2-carbon side chain at position 17 and an oxygenated function at position 3 is necessary for the inhibitory activity of progesterone. The introduction of a hydroxyl group in the progesterone molecule at positions 6 (β), 11 (α), 16 (α) or 17 (α) destroyed its growth-inhibitory activity. 11β-Hydroxyprogesterone is weaker than progesterone in the inhibition of estrone-induced uterine growth; unlike progesterone it has the capacity to depress growth elicited by testosterone. The introduction of a flourine atom in the 9 (α) position resulted in a striking increase of the growth-inhibitory activity of 11β-hydroxyprogesterone and hydrocortisone. 9α-Flouro-11β-hydroxyprogesterone is a partial but significant inhibitor of growth of the uterus in hypophysectomized rats injected simultaneously with large doses of estrone or testosterone. It is more powerful than progesterone in transforming the vaginal epithelium to mucus cells in the presence of estrone. Administered alone, the only detectable growth was a slight increase in size of the preputial glands. 9α-Flouro-11β-hydroxyprogesterone suppresses in part the growth of the adrenals, ovaries, and uterus in intact rats at a dose level which does not cause loss of body weight or inhibit body growth. Many rats treated with this compound in small amount had extensive mucification of the vagina resembling that of late pregnancy.
Full Text
The Full Text of this article is available as a PDF (984.9 KB).
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- BYRNES W. W., STAFFORD R. O., OLSON K. J. Anti-gonadal hormone activity of 11a-hydroxyprogesterone. Proc Soc Exp Biol Med. 1953 Feb;82(2):243–247. [PubMed] [Google Scholar]
- HUGGINS C., JENSEN E. V., CLEVELAND A. S. Chemical structure of steroids in relation to promotion of growth of the vagina and uterus of the hypophysectomized rat. J Exp Med. 1954 Sep 1;100(3):225–240. doi: 10.1084/jem.100.3.225. [DOI] [PMC free article] [PubMed] [Google Scholar]
- HUGGINS C., JENSEN E. V. The depression of estrone-induced uterine growth by phenolic estrogens with oxygenated functions at positions 6 or 16: the impeded estrogens. J Exp Med. 1955 Sep 1;102(3):335–346. doi: 10.1084/jem.102.3.335. [DOI] [PMC free article] [PubMed] [Google Scholar]
- HUGGINS C., PARSONS F. M., JENSEN E. V. Promotion of growth of preputial glands by steroids and the pituitary growth hormone. Endocrinology. 1955 Jul;57(1):25–32. doi: 10.1210/endo-57-1-25. [DOI] [PubMed] [Google Scholar]
- Huggins C., Clark P. J. QUANTITATIVE STUDIES OF PROSTATIC SECRETION : II. THE EFFECT OF CASTRATION AND OF ESTROGEN INJECTION ON THE NORMAL AND ON THE HYPERPLASTIC PROSTATE GLANDS OF DOGS. J Exp Med. 1940 Nov 30;72(6):747–762. doi: 10.1084/jem.72.6.747. [DOI] [PMC free article] [PubMed] [Google Scholar]
- LIPSCHUTZ A., MARDONES E., IGLESIAS R., FUENZALIDA F., BRUZZONE S. Comparative antifibromatogenic action of cortical steroids. Science. 1952 Oct 24;116(3017):448–452. doi: 10.1126/science.116.3017.448. [DOI] [PubMed] [Google Scholar]
- MARDONES E., IGLESIAS R., LIPSCHUTZ A. Antioestrogenic potencies of various progesterone derivatives with oxidation at C11. Nature. 1954 Oct 30;174(4435):839–840. doi: 10.1038/174839a0. [DOI] [PubMed] [Google Scholar]
- MARDONES E., IGLESIAS R., LIPSCHUTZ A. Physiological action of 19-norprogesterone in the guinea pig. Proc Soc Exp Biol Med. 1954 Jul;86(3):451–453. doi: 10.3181/00379727-86-21129. [DOI] [PubMed] [Google Scholar]
- Robson J. M. The action oe progesterone on the uterus of the rabbit and its antagonism by oestrone. J Physiol. 1936 Oct 16;88(1):100–111. doi: 10.1113/jphysiol.1936.sp003425. [DOI] [PMC free article] [PubMed] [Google Scholar]