Effect of justicidin B - a potent cytotoxic and pro-apoptotic arylnaphtalene lignan on human breast cancer-derived cell lines

Neoplasma. 2011;58(4):320-5. doi: 10.4149/neo_2011_04_320.


Justicidin B produced by genetically transformed cultures of Linum leonii was tested for cytotoxic activity and induction of apoptosis in MDA-MB-231 and MCF-7 breast cancer derived cell lines. The tested lignan evoked strong, concentration dependent cytotoxicity in both cell lines, whereby MCF-7 proved to be far more sensitive as compared to MDA-MB-231. The 24 h treatment of both cell lines increased the level of apoptotic DNA fragmentation; however the proapoptotic activity is completely inhibited if the cells are co-incubated with the non-selective pan-caspase inhibitor Boc-Asp(OMe)-fluoromethyl ketone (PCI), which implies that justicidin B, activates programmed cell death via caspase -dependent mechanisms. Exposure of MDA-MB-231 cells with justicidin B leads to concentration dependent decrease in the expression of NFkB; whereas the treatment of MCF-7, is consistent with strong increase in the expression of this transcription factor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Blotting, Western
  • Breast Neoplasms*
  • Cell Line, Tumor
  • DNA Fragmentation / drug effects
  • Dioxolanes / pharmacology*
  • Female
  • Humans
  • Inhibitory Concentration 50
  • Lignans / pharmacology*


  • Antineoplastic Agents
  • Dioxolanes
  • Lignans
  • justicidins