DNA-binding affinity,cytotoxicity, apoptosis,cell cycle inhibition and molecular docking studies of a new stilbene derivative |
| |
Authors: | Maryam Mehdipour Reza Yekta Mina Hanifeh Ahagh Majid Mahdavi Zarrin Ghasemi |
| |
Institution: | 1. Department of Biology, Faculty of Natural Sciences, University of Tabriz, Tabriz, Iran;2. Department of Organic Chemistry and Biochemistry, Faculty of Chemistry, University of Tabriz, Tabriz, Iran |
| |
Abstract: | Stilbene derivatives have been found to possess promising anticancer activities against human cancer cell lines in vitro. In the present study, we have investigated cytotoxic, apoptosis induction and DNA binding activity of new stilbene derivative, (E)-1-(4-Chlorophenyl)-4,5-diphenyl-2-4-(4-methoxystryl)phenyl]-1H-imidazol (STIM) on K562 chronic myeloid leukemia cell line. Via MTT assay STIM demonstrated cytotoxic activity against K562 cell line with IC50 value of 150?µM. Apoptosis, as the mechanism of cell death, was evaluated by morphological study and flow cytometric analysis. In vitro DNA binding property of STIM has been studied by vital spectroscopic techniques, which indicated that STIM interact with ctDNA through groove binding mode and binding constant (Kb) was estimated to be 6.9?×?104?M?1. Docking studies revealed that hydrophobic is the most important interaction in STIM-DNA complex, and that the ligand (STIM) interacts with DNA via groove binding mode and the bindiyspng energy was calculated as ?13.37?kcal/mol. Taken together, the present study suggests that STIM exhibits anticancer effect on K562 cell line through the induction of apoptosis as well as cell cycle arrest at Sub-G1 phase and also can bind to double helix DNA in vitro. |
| |
Keywords: | Cytotoxicity groove binding molecular docking K562 stilbene derivatives |
|
|