4,9-diazapyrenium dications induce apoptosis in human tumor cells

Anticancer Res. 1996 Nov-Dec;16(6B):3705-8.

Abstract

We investigated the antiproliferative effects of two planar 4,9-diazapyrenium hydrogenasulphates against human malignant MiaPaCa 2 (pancreatic carcinoma), Hep 2 (laryngeal carcinoma) and human normal fibroblasts (WI 38) cell lines. The tested compounds were very potent in inhibiting the growth of the treated cell lines. Treatment with molar concentrations of the substances (10(-4)-10(-7) M) caused growth inhibition by more than 50%. The morphological changes of treated cells were also observed. Cells became smaller, with condensed chromatin and fragmented nuclei, the characteristics of dying cells. The identification of DNA-fragmentation and the appearance of chromatin aggregation leads us to assume the tested substances induced apoptosis of the investigated tumor cell lines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Cell Division / drug effects
  • Humans
  • Intercalating Agents / pharmacology*
  • Laryngeal Neoplasms / metabolism
  • Laryngeal Neoplasms / pathology
  • Neoplasm Proteins / metabolism
  • Pancreatic Neoplasms / metabolism
  • Pancreatic Neoplasms / pathology
  • Phenanthrolines / pharmacology*
  • Proto-Oncogene Proteins c-myc / metabolism
  • Tumor Cells, Cultured / drug effects
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • Intercalating Agents
  • Neoplasm Proteins
  • Phenanthrolines
  • Proto-Oncogene Proteins c-myc
  • Tumor Suppressor Protein p53