Antitumor effects of 3,3',4,4',5,5'-hexahydroxystilbene in HL-60 human promyelocytic leukemia cells.

Abstract

Resveratrol (3,4',5-trihydroxystilbene, RV) exerts remarkable cytostatic and cytotoxic effects against a multitude of human cancer cell lines. Since the introduction of additional hydroxyl groups was supposed to increase the biological activity of RV, we have synthesized a number of polyhydroxylated stilbene analogues as potential antitumor agents. In this study, the activity of 3,3',4,4',5,5'-hexahydroxystilbene (M8) was investigated in HL-60 human promyelocytic leukemia cells. Employing a growth inhibition assay, incubation with M8 and RV resulted in IC50 values of 6.25 and 12 microM, respectively. Using a specific Hoechst/propidium iodide double staining method, we found that M8 was able to induce apoptosis in concentrations significantly lower than those of RV. In addition, M8 arrested cells in the S phase and totally depleted cells in the G2-M phase of the cell cycle (143% and 0% of control after treatment with 12.5 microM M8, respectively). We therefore believe that this promising agent deserves further preclinical and in vivo testing.

• Authors: P Saiko, Z Horvath, M Murias, N Handler, W Jaeger, T Erker, M Fritzer-Szekeres, T Szekeres
• Journal: Nucleosides, nucleotides & nucleic acids (Nucleosides Nucleotides Nucleic Acids) Vol. 25 Issue 9-11 Pg. 1013-7 ( 2006) ISSN: 1525-7770 [Print] United States
• PMID: 17065056 (Publication Type: Journal Article)

Chemical References

• 3,3',4,4',5,5'-hexahydroxystilbene
• Antineoplastic Agents
• Fluorescent Dyes
• Stilbenes
• Pyrogallol
• Cytarabine
• Propidium
• Bisbenzimidazole

Topics

• Antineoplastic Agents (pharmacology)
• Antineoplastic Combined Chemotherapy Protocols (therapeutic use)
• Bisbenzimidazole (pharmacology)
• Cell Cycle (drug effects)
• Cytarabine (administration & dosage)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Drug Synergism
• Fluorescent Dyes (pharmacology)
• HL-60 Cells
• Humans
• Inhibitory Concentration 50
• Leukemia, Promyelocytic, Acute (drug therapy)
• Propidium (pharmacology)
• Pyrogallol (analogs & derivatives, pharmacology)
• Stilbenes (pharmacology)