LAUSR

Aim and objectives: Balancing between Bax and Bcl‐2 plays critical roles in both proliferation and self‐renewal activation of cancer cells. Indole‐3‐formaldehyde derivatives limit the growth and facilitate cell death in different cell systems. In this study, we introduced a novel indole derivative (2‐AITFEI‐3‐F) with tendency to facilitate apoptosis in NB4 line in comparison to basal Indole‐3‐formaldehyde (I3F). Methods: The NB4 cells were cultured in RPMI1640 medium contained 2‐AITFEI‐3‐F and I3F (15.12–1000 &mgr;g/mL) for 24, 48 and 72 h. Inhibition of cell proliferation was assessed by trypan blue staining technique and MTT assay. The fold changes of Bax/Bcl‐2 expression against &bgr;‐actin were determined by real‐time‐PCR technique. Western blotting analysis was also applied for evaluating the expression of Bax and Bcl2 at protein level. Data were analyzed by student t and repeated measure tests. Differences were considered significant if (P < 0.01). Results: There was a significant difference in cell viability, when various concentrations of 2‐AITFEI‐3‐F (but similar to I3F) were used for 24, 48 and 72 h in comparison to I3F regarding the cellular viability (P < 0.05). Real time PCR and Western blotting analysis indicated that the gene and protein expression level of Bcl‐2 down‐regulated while Bax was up‐regulated in compare to untreated control cells and cells treated with I3F (P < 0.01). Conclusion: According to these findings, the novel indole derivative 2‐AITFEI‐3‐F probably triggered apoptosis of NB4 cells by modulating Bax/Bcl‐2 ratio. Furthermore, the 2‐AITFEI‐3‐F had markedly displayed anti‐cancer activity than I3F.