Apoptosis and suppression of tumor growth by artepillin C extracted from Brazilian propolis

Cancer Detect Prev. 1998;22(6):506-15. doi: 10.1046/j.1525-1500.1998.00020.x.

Abstract

Artepillin C was extracted from Brazilian propolis. Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) has a molecular weight of 300.40 and possesses antibacterial activity. When artepillin C was applied to human and murine malignant tumor cells in vitro and in vivo, artepillin C exhibited a cytotoxic effect and the growth of tumor cells was clearly inhibited. The artepillin C was found to cause significant damage to solid tumor and leukemic cells by the MTT assay, DNA synthesis assay, and morphological observation in vitro. When xenografts of human tumor cells were transplanted into nude mice, the cytotoxic effects of artepillin C were most noticeable in carcinoma and malignant melanoma. Apoptosis, abortive mitosis, and massive necrosis combined were identified by histological observation after intratumor injection of 500 microg of artepillin C three times a week. In addition to suppression of tumor growth, there was an increase in the ratio of CD4/CD8 T cells, and in the total number of helper T cells. These findings indicate that artepillin C activates the immune system, and possesses direct antitumor activity.

MeSH terms

  • Animals
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Apoptosis / drug effects*
  • Brazil
  • DNA Replication / drug effects
  • Growth Inhibitors / isolation & purification
  • Growth Inhibitors / pharmacology*
  • Growth Inhibitors / toxicity
  • Humans
  • Mice
  • Mice, Nude
  • Neoplasms / pathology*
  • Nucleic Acid Synthesis Inhibitors / pharmacology
  • Phenylpropionates / isolation & purification
  • Phenylpropionates / pharmacology*
  • Phenylpropionates / toxicity
  • Propolis / chemistry*
  • Rats
  • Transplantation, Heterologous / pathology
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Growth Inhibitors
  • Nucleic Acid Synthesis Inhibitors
  • Phenylpropionates
  • artepillin C
  • Propolis