Novel Resveratrol Derivatives Induce Apoptosis and Cause Cell Cycle Arrest in Prostate Cancer Cell Lines

• Published in: Anticancer research Vol. 27; no. 5A; pp. 3459 - 3464
• Main Authors: Horvath, Z, Marihart-Fazekas, S, Saiko, P, Grusch, M, Oezsuey, M, Harik, M, Handler, N, Erker, T, Jaeger, W, Fritzer-Szekeres, M, Djavan, B, Szekeres, T
• Format: Journal Article
• Language: English
• Published: Attiki International Institute of Anticancer Research 01-09-2007
• Subjects: Antineoplastic Agents - pharmacology; Apoptosis - drug effects; Biological and medical sciences; Cell Cycle - drug effects; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Male; Medical sciences; Nephrology. Urinary tract diseases; Phenols - pharmacology; Prostatic Neoplasms - drug therapy; Prostatic Neoplasms - pathology; Stilbenes - pharmacology; Tumors; Tumors of the urinary system; Urinary tract. Prostate gland; Urinary system disease; Prostate disease; Malignant tumor; cell cycle arrest; Stilbene derivatives; 3,4,4',5-tetramethoxy-stilbene; Polyphenol; Cancerology; Cell death; Phytoalexin; Cell cycle; Established cell line; Resveratrol; Phenols; 3,3',4,4',5,5'-hexahydroxystilbene; Male genital diseases; Prostate cancer; Tumor cell; Apoptosis
• ISSN: 0250-7005; 1791-7530

Background: Resveratrol (RV), a naturally occurring phytoalexin, exerts manifold biological effects against a variety of human
tumor cell lines. In this study, the cytotoxic and biological effects of novel RV derivatives were investigated in prostate
cancer cells. Materials and Methods: Cytotoxicity of the compounds was assessed by clonogenic assays in PC-3, LNCaP and DU-145
human prostate cancer cell lines. Induction of apoptosis was studied by Hoechst-propidium-iodide double staining. Cell cycle
phase distribution of prostate cancer cells was analyzed using flow cytometry. Results: Methoxy- and hydroxy-substituted RV
derivatives exerted cytotoxic effects against all three cell lines. The most potent compounds, 3,3′,4,4′,5,5′-hexahydroxy-stilbene
and 3,4,4′,5-tetramethoxy-stilbene, induced apoptosis at concentrations lower than RV and caused cell cycle arrest in the
cell lines investigated. Conclusion: Introducing additional hydroxy- and methoxy-moieties to the stilbene ring of RV is capable
of enhancing its cytotoxic and pro-apoptotic effects in hormone-responsive and non-responsive prostate cancer cells.