Effects of the lipidosterolic extract of Serenoa repens (Permixon®) on human prostatic cell lines

BACKGROUND. Permixon® is a drug used in the treatment of benign prostatic hyperplasia. We studied its androgenic and antiandrogenic effects in the prostatic cell line LNCaP and PC3, respectively responsive and unresponsive to androgen stimulation. METHODS. 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. RESULTS. 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. CONCLUSIONS. 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.