Background: The pyrrolidine and indole ring system found in the structure of various biologically important
compounds used in the treatment of various diseases (1) and has a significant place in the pharmaceutical R&D
studies (2). Thus the combination of the two ring system into compounds; A and B were attractive, we studied
apoptotic effect of these compounds on the human breast cancer MCF-7 cells. The balance between cell
proliferation and apoptosis is very important in the formation of cancer. Caspases are the major executioners which
lead to apoptotic cell death. Caspases 8 and 9 are the most important members of this group (3).
Methods: Pyrrolidine derivatives bearing the indole ring have been synthesized and characterized as indicated our
previous studies (4). Three replicates of each group were used and the experiment was ended at 100 th h. All data
have been recorded by the supplied RTCA software. MCF-7 cells were grown on six-well plate petri dishes as
monolayer culture until they reach 50-60% confluence. After 24 and 48 h of treatment, cells were harvested and
resuspanded in 100 µl of D-PBS for the biochemical investigations. Caspases 8 and 9 were determined according to
the manufacturer’s instructions (BioVision Research Product, Mountain View, CA, USA). Results were expressed as
the caspase enzyme as measured by optical density (OD 405 nm).
Results: Treatment with A at 10 and 20 μM caused a significant increase of cell index whereas at 50 and 100 µM
caused a significant drop of cell index. Our analysis of IC 50 value of A was resulted in 30 µM. Treatment with B at
10, 20 and 50 μM caused a significant increase of cell index whereas at 100 µM caused a significant drop of cell
index. B at 100 µM inhibited cell proliferation 50%. There was no significant in caspase 8 in all the groups. The
elevation in caspase 9 enzyme activity in B 48h was observed compared with the DMSO (p < 0.05).
Conclusions: Compound A and B may not be considered as an apoptotic agent on MCF-7 cells. Further investigation
is need to be made for different doses and intervals to get its real potential activity.