PM-3, a benzo-gamma-pyran derivative isolated from propolis, inhibits growth of MCF-7 human breast cancer cells

Anticancer Res. May-Jun 2001;21(3B):1665-71.

Abstract

Propolis has numerous biologic activities including antibiotic, antifungal, antiviral and anti-inflammatory properties. Several components isolated from propolis have been shown to have anticancer activity. This study demonstrates that the compound PM-3 (3-[2-dimethyl-8-(3-methyl-2-butenyl)benzopyran]-6-propenoic acid) isolated from Brazilian propolis markedly inhibits the growth of MCF-7 human breast cancer cells. This effect was associated with inhibition of cell cycle progression and induction of apoptosis. Treatment of MCF-7 cells with PM-3 arrested cells in the G1 phase and resulted in a decrease in the protein levels of cyclin D1 and cyclin E. PM-3 also inhibited the expression of cyclin D1 at the transcriptional level when examined in cyclin D1 promoter luciferase assays. Induction of apoptosis by PM-3 occurred within 48 hours after treatment of MCF-7 cells. The MCF-7 treated cells also displayed a decrease in the level of the estrogen receptor (ER) protein and inhibition of estrogen response element (ERE) promoter activity. Therefore, PM-3 merits further investigation with respect to breast cancer chemoprevention or therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Annexin A5 / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Benzopyrans / chemistry
  • Benzopyrans / pharmacology*
  • Blotting, Northern
  • Blotting, Western
  • Breast Neoplasms / drug therapy*
  • Cell Cycle / drug effects
  • Cell Division
  • Coloring Agents / pharmacology
  • Cyclin D1 / biosynthesis
  • Cyclin E / biosynthesis
  • Dose-Response Relationship, Drug
  • Down-Regulation
  • Enzyme-Linked Immunosorbent Assay
  • Flow Cytometry
  • Genes, Reporter
  • Humans
  • Methacrylates / chemistry
  • Methacrylates / pharmacology*
  • Models, Chemical
  • Plant Extracts / pharmacology*
  • Promoter Regions, Genetic
  • Propolis / metabolism*
  • Receptors, Estrogen / biosynthesis
  • Receptors, Estrogen / drug effects
  • Response Elements
  • Tetrazolium Salts / pharmacology
  • Thiazoles / pharmacology
  • Time Factors
  • Transcription, Genetic
  • Transfection
  • Tumor Cells, Cultured

Substances

  • 3-(2-dimethyl-8-(3-methyl-2-butenyl)benzopyran)-6-propenoic acid
  • Annexin A5
  • Antineoplastic Agents
  • Benzopyrans
  • Coloring Agents
  • Cyclin E
  • Methacrylates
  • Plant Extracts
  • Receptors, Estrogen
  • Tetrazolium Salts
  • Thiazoles
  • Cyclin D1
  • Propolis
  • thiazolyl blue