Bicalutamide dose-dependently inhibits proliferation in human prostatic carcinoma cell lines and primary cultures.
OBJECTIVE
Androgen antagonists inhibit prostatic cell proliferation in normal and pathological conditions and are useful antitumor agents in prostatic carcinoma (PCa). Bicalutamide (BCLT) is a well-known non-steroidal antiandrogenic agent able to interfere with androgen receptor (AR). We tested the efficacy of BCLT in inhibiting proliferation of human PCa cell lines and of primary cultures from biopsies of PCa patients.


METHODS
Human prostatic carcinoma cell lines (PC3, DU145, LNCaP ALVA 31 and ND1) and short-term primary tissue cultures from PCa patients were treated with BCLT. Cell proliferation and orange acridine and ethidium bromide fluorescence staining studies were performed.


RESULTS
BCLT was able to inhibit, significantly and dose-dependently, cell proliferation in AR-positive human PCa cell lines and in 10 cases of primary cultures with Gleason grades 4 to 8. Its action appears to be mainly apoptotic in AR-positive cells and cytotoxic in AR-negative cells.


CONCLUSIONS
BCLT, which inhibits growth in both human PCa cell lines and PCa primary cultures from patients with medium and low-grade tumors, deserves attention as a potential widely effective antiandrogenic monotherapy in prostatic carcinoma. However, its efficacy in AR-negative cells requires further research.
Vicentini
Carlo
C
Chair of Urology, Department of Surgery, University of L'Aquila Medical School, Via Vetoio, Coppito-2, 67100 L'Aquila, Italy.
Festuccia
Claudio
C
Angelucci
Adriano
A
Gravina
Giovanni Luca
GL
Muzi
Paola
P
Eleuterio
Enrica
E
Miano
Roberto
R
Marronaro
Angelo
A
Tubaro
Andrea
A
Bologna
Mauro
M
D000165:Acridine Orange; D000726:Androgen Antagonists / Q000494:pharmacology*; D000813:Anilides / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004996:Ethidium; D005456:Fluorescent Dyes; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D009570:Nitriles; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013194:Staining and Labeling / Q000379:methods; D014105:Tosyl Compounds; D014407:Tumor Cells, Cultured
D000726:Androgen Antagonists; D000813:Anilides; D000970:Antineoplastic Agents; D005456:Fluorescent Dyes; D009570:Nitriles; D014105:Tosyl Compounds; C053541:bicalutamide; D004996:Ethidium; D000165:Acridine Orange