| Autor: |
Scherbakov AM; Department of Experimental Tumor Biology, Blokhin N.N. National Medical Research Center of Oncology, Moscow, Russia., Stasevich OV; Department of Physical-Chemical Methods for Products Certification, Belarusian State Technological University, Minsk, Belarus., Salnikova DI; Department of Experimental Tumor Biology, Blokhin N.N. National Medical Research Center of Oncology, Moscow, Russia.; Faculty of Medicine, Lomonosov Moscow State University, Moscow, Russia., Andreeva OE; Department of Experimental Tumor Biology, Blokhin N.N. National Medical Research Center of Oncology, Moscow, Russia., Mikhaevich EI; Department of Experimental Tumor Biology, Blokhin N.N. National Medical Research Center of Oncology, Moscow, Russia. |
| Abstrakt: |
Secoisolariciresinol diglucoside (SDG) is isolated from Linum usitatissimum seeds. The antiproliferative effects of SDG (1) and its derivatives secoisolariciresinol (2) and secoisolariciresinol-4', 4″-diacetate ( 3) have been evaluated on MCF-7 breast cancer cells and normal breast epithelial line MCF-10A. Lignan 1 has not shown cytotoxic effects on MCF-7 cells, while derivatives 2 and 3 have inhibited cell growth with IC 50 values of 25 and 11 µM, respectively. Estrogen receptor alpha is a key growth driver in MCF-7 cells. Compound 1 did not affect the activity of ERα, while derivatives 2 and 3 showed significant antiestrogenic effects. Compounds 2 and 3 caused apoptosis in the MCF-7 line, determined by the cleavage of PARP. SDG derivative 3 enhanced the effect of doxorubicin. SDG derivatives can be considered as promising agents that exhibit a combined antiestrogen and proapoptotic effect in hormone-dependent breast cancer cells. |
