Androgens and androgen-receptors in prostate tissue from patients with benign prostatic hyperplasia: effects of cyproterone acetate.
Testosterone, 5 alpha-dihydrotestosterone and cyproterone acetate (CPA) were estimated in samples of prostate tissue, obtained from benign prostatic hyperplasia (BPH) patients who were or were not pretreated with CPA. Furthermore, these steroids were estimated in various fractions of the BPH tissue, and the number of nuclear androgen-receptor sites was determined. CPA-treatment caused a 4-fold, significant suppression of 5 alpha-dihydrotestosterone levels in total prostate tissue and its subfractions, without affecting testosterone levels or the androgen-receptor contents of the nuclear extracts. Nuclear concentrations of CPA were twice as high as those of 5 alpha-dihydrotestosterone. It is concluded that effects of CPA may have been caused through a combination of the following mechanisms: (1) suppression of peripheral androgen levels; (2) competition with androgens for (nuclear) androgen-receptors; and (3) suppression of prostatic 5 alpha-reductase.
Department of Endocrinology and Reproduction, Erasmus University Rotterdam, The Netherlands.
F H
FH
de Jong
P J
PJ
Reuvers
J
J
Bolt-de Vries
E
E
Mulder
J H
JH
Blom
F H
FH
Schroeder
D058891:5-alpha Reductase Inhibitors; D000728:Androgens / Q000378:metabolism*; D001667:Binding, Competitive; D002467:Cell Nucleus / Q000378:metabolism; D003534:Cyproterone / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D017373:Cyproterone Acetate; D013196:Dihydrotestosterone / Q000378:metabolism; D006801:Humans; D008297:Male; D011467:Prostate / Q000187:drug effects / Q000378:metabolism*; D011470:Prostatic Hyperplasia / Q000378:metabolism*; D011944:Receptors, Androgen / Q000378:metabolism*; D013739:Testosterone / Q000378:metabolism
D058891:5-alpha Reductase Inhibitors; D000728:Androgens; D011944:Receptors, Androgen; D013196:Dihydrotestosterone; D013739:Testosterone; D017373:Cyproterone Acetate; D003534:Cyproterone