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Effect of Justicidin B - A Potent Cytotoxic and Pro-Apoptotic Arylnaphtalene Lignan on Human Breast Cancer-Derived Cell Lines

G Momekov, S Konstantinov, I Dineva, I Ionkova

Neoplasma. 2011;58(4):320-5.

PMID: 21520988

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP187389533 Boc-Asp(OMe)-fluoromethyl ketone Boc-Asp(OMe)-fluoromethyl ketone 187389-53-3 Price
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