Ravenna L, Di Silverio F, Russo M A, Salvatori L, Morgante E, Morrone S, Cardillo M R, Russo A, Frati L, Gulino A, Petrangeli E
Department of Experimental Medicine and Pathology, University La Sapienza, Rome, Italy.
Prostate. 1996 Oct;29(4):219-30. doi: 10.1002/(SICI)1097-0045(199610)29:4<219::AID-PROS3>3.0.CO;2-6.
Permixon is a drug used in the treatment of benign prostatic hyperplasia. We studied its androgenic and antiandrogenic effects in the prostatic cell lines LNCaP and PC3, respectively responsive and unresponsive to androgen stimulation.
We performed FACScan analysis to investigate toxicity, 3H thymidine and 35S methionine incorporation to determine antiproliferative and metabolic effects, electron microscopy to study ultrastructural changes and cotransfection experiments to elucidate the role of wild type androgen receptor.
In LNCaP cell line, Permixon induced a double proliferative/differentiative effect, not observed in PC3 cells. In PC3 cells cotransfected with wild-type androgen receptors and CAT reporter genes under the control of a androgen responsive element, the drug inhibited androgen-induced CAT transcription.
Our data indicate a role of the androgen receptor in mediating the effects of Permixon in LNCaP cells. Cotransfection experiments in PC3 cells support a clear antiandrogenic action of the drug.
