This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Schulz, P. Articles by Fittler, F. Search for Related Content PubMed PubMed Citation Articles by Schulz, P. Articles by Fittler, F.

Evaluation of the Cytotoxic Activity of Diethylstilbestrol and Its Mono- and Diphosphate towards Prostatic Carcinoma Cells¹

Institut für Physiologische Chemie der Universität München, Schillerstr. 44, D-8000 München 2 [P. S., F. F.]; Klinikum Steglitz der Freien Universität Berlin, Urologische Klinik und Poliklinik, Abteilung für Urologie, Hindenburgdamm 30, 1000 Berlin 45 [H. W. B.]; and Degussa Pharma Gruppe, Daimlerstr. 25, D-6000 Frankfurt 1 [W. P. B., A. K.], Germany

To evaluate a possible direct cytotoxic effect of diethylstilbestrol diphosphate (DESDP) in the treatment of prostate cancer we exposed three prostatic carcinoma cell lines (LNCaP, DU 145, and PC-3), 2 nonprostatic neoplastic cell lines (KB and EJ), and one nontransformed cell line (MRC-5) to diethylstilbestrol (DES), diethylstilbestrol monophosphate, and DESDP at levels occurring in patients' sera during p.o. DES therapy (2 to 5 ng/ml) or DESDP infusions (1 to 20 µg/ml), respectively. With 5 ng/ml of DES no effect was seen in LNCaP cells, even after 14 days of exposure. In contrast, drug levels attained during DESDP infusions showed marked, dose-dependent cytotoxicity towards all cell lines under study. Prostatic cells were not exceptionally sensitive. High-dose DES slightly stimulated the synthesis of prostatic acid phosphatase in LNCaP cells. Formation of foci of polygonal cells was induced by 5 µg/ml of DES in cultures of MRC-5 fibroblasts. We conclude that, at high doses, DES liberated from DESDP acts upon a regulatory or metabolic mechanism common to many if not all human cells. Preferential sensitivity of prostate cancer cells in vivo may be due to high local phosphatase activity and/or DES accumulation in prostatic tissue.

¹ This work was supported by Asta-Werke AG, Degussa Pharma Gruppe, Bielefeld (Federal Republic of Germany), Deutsche Forschungsgemeinschaft, and Fonds der Chemischen Industrie.

Received 7/ 7/87. Revised 12/31/87. Accepted 1/28/88.

This article has been cited by other articles:

				J. A. Mobley, J. O. L'Esperance, M. Wu, C. J. Friel, R. H. Hanson, and S.-M. Ho The novel estrogen 17{alpha}-20Z-21-[(4-amino)phenyl]-19-norpregna-1,3,5(10),20-tetraene-3,17{beta}-diol induces apoptosis in prostate cancer cell lines at nanomolar concentrations in vitro Mol. Cancer Ther., May 1, 2004; 3(5): 587 - 596. [Abstract] [Full Text] [PDF]