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

Nucleosides Nucleotides Nucleic Acids. 2006;25(9-11):1013-7. doi: 10.1080/15257770600890624.

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.

MeSH terms

  • 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*
  • Pyrogallol / pharmacology
  • Stilbenes / pharmacology*

Substances

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