title: Formamidinodoxorubicins are more potent than doxorubicin as apoptosis inducers in human breast cancer cells.
abstract: OBJECTIVE
  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.
  
  
  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.
  
  
  CONCLUSIONS
  DOX-F MOR and DOX-F PAZ analogs are more potent apoptosis inducers than doxorubicin.
authors: Department of Thermobiology, Institute of Biophysics, Faculty of Biology and Environmental Protection, Lodz University Pomorska, Lodz, Poland.
authors: Agnieszka
authors: A
authors: Marczak
authors: Department of Thermobiology, Institute of Biophysics, Faculty of Biology and Environmental Protection, Lodz University Pomorska, Lodz, Poland.
authors: Marta
authors: M
authors: Denel-Bobrowska
authors: Department of Modified Antibiotics, Institute of Biotechnology and Antibiotics, Warsaw, Poland lukawskam@iba.waw.pl.
authors: Małgorzata
authors: M
authors: Łukawska
authors: Department of Modified Antibiotics, Institute of Biotechnology and Antibiotics, Warsaw, Poland.
authors: Irena
authors: I
authors: Oszczapowicz
mesh_terms: D017304:Annexin A5 / Q000378:metabolism; D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D053148:Caspase 3 / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000031:analogs & derivatives; D019008:Drug Resistance, Neoplasm / Q000235:genetics; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects
chemical_list: D017304:Annexin A5; D004317:Doxorubicin; D053148:Caspase 3
keywords: Apoptosis; cytotoxicity; formamidine anthracyclines; necrosis