title: Trilostane, an inhibitor of 3β-hydroxysteroid dehydrogenase, has an agonistic activity on androgen receptor in human prostate cancer cells.
abstract: The intracellular androgen metabolism and cell activity in prostate cancer cells with mutated (LNCaP-FGC) or wild-type (VCaP) androgen receptors in the presence of trilostane, an inhibitor of 3β-hydroxysteroid dehydrogenase, were examined. Trilostane suppressed the intracellular production of androstenedione, testosterone, and dihydrotestosterone from dehydroepiandrosterone in LNCaP-FGC cells. In both LNCaP-FGC and VCaP cell types, the prostate-specific antigen (PSA) levels in media were increased by trilostane alone in a concentration-dependent manner. Both cells pretreated with trilostane showed a dose-dependent decrease in PSA production with bicalutamide (P<0.001). Trilostane should be used with particular concern when treating prostate cancer.
authors.affiliation: Division of Urology, Department of Regenerative and Transplant Medicine, Graduate School of Medical and Dental Sciences, Niigata University, Asahimachi 1, Niigata 951-8510, Japan.
authors.forename: Itsuhiro
authors.initials: I
authors.lastname: Takizawa
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Nishiyama
authors.forename: Noboru
authors.initials: N
authors.lastname: Hara
authors.forename: Tatsuhiko
authors.initials: T
authors.lastname: Hoshii
authors.forename: Fumio
authors.initials: F
authors.lastname: Ishizaki
authors.forename: Yoshimichi
authors.initials: Y
authors.lastname: Miyashiro
authors.forename: Kota
authors.initials: K
authors.lastname: Takahashi
mesh_terms: D015096:3-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors*; D000728:Androgens / Q000096:biosynthesis; D045744:Cell Line, Tumor; D002853:Chromatography, Liquid; D003687:Dehydroepiandrosterone / Q000378:metabolism; D013196:Dihydrotestosterone / Q000031:analogs & derivatives* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D011944:Receptors, Androgen / Q000378:metabolism; D013739:Testosterone / Q000378:metabolism
chemical_list: D000728:Androgens; D004791:Enzyme Inhibitors; D011944:Receptors, Androgen; D013196:Dihydrotestosterone; D013739:Testosterone; D003687:Dehydroepiandrosterone; D015096:3-Hydroxysteroid Dehydrogenases; C009954:trilostane