RT Journal Article
SR Electronic
T1 Formamidinodoxorubicins Are more Potent than Doxorubicin as Apoptosis Inducers in Human Breast Cancer Cells
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 1935
OP 1940
VO 35
IS 4
A1 AGNIESZKA MARCZAK
A1 MARTA DENEL-BOBROWSKA
A1 MAŁGORZATA ŁUKAWSKA
A1 IRENA OSZCZAPOWICZ
YR 2015
UL http://ar.iiarjournals.org/content/35/4/1935.abstract
AB Background/Aim: The ability of five formamidinodoxorubicins to induce apoptosis of MCF-7 breast cancer cells was tested. All these compounds were modified at C-3’ and contain a formamidine group (−N=CH–NRR), with the rest of the cyclic secondary amine (HNRR) of a gradually increasing ring size. Materials and Methods: Cytotoxicity was assessed using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. To analyze apoptosis, double staining using fluorescence probes Hoechst 33258/propidium iodide (PI) and annexin V- Fluorescein isothiocyanate/PI was carried-out. Additionally, the TdT-mediated dUTP nick-end labelling test and activity of caspase 3 were determined. Results: The four tested derivatives displayed a significant increase in antiproliferative activity in comparison to doxorubicin. All of the tested derivatives induced caspase-dependent apoptosis of MCF-7 cells. Conclusion: DOX-F MOR and DOX-F PAZ analogs are more potent apoptosis inducers than doxorubicin.