科研之友
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摘要
Two different series of copper complexes, [Cu(MFL)(FcAA)H2O] (C1-C4) and [Cu(MFL) (BzAA) H2O] (C5-C8), where FcAA = ferrocenyl amino acid mannich base conjugates and BzAA = benzaldehyde amino acid mannich base conjugates have been synthesized and characterized by spectroscopic methods. The complexes have been investigated for their interactions with DNA by employing fluorescence quenching measurements, UV-Vis spectroscopy and DNA viscosity measurements. High binding constants obtained from the DNA binding studies (K-b = 10(6) M-1) prompted the in-vitro cytotoxicity assay of complexes on A549 human lung carcinoma cells (employing MTT assay). The IC50 values obtained herein were found to be lower than those of the ligands for A549 cell line. Antiproliferative effects on A549 tumour cells exerted by the complexes were consistent with their intracellular uptake properties. The cellular uptake studies indicated that complexes C1-C8 enter the cytoplasm and accumulate in the nuclei. Rapid change in the nuclear morphology was observed with DAPI staining. Acridine orange/ethidium bromide dual staining revealed that most of the A549 cells enter early apoptosis within 12 h of treatment. Further all the complexes showed effective cell growth inhibition by triggering G0/G1 phase arrest and inducing apoptosis. FACScan results revealed remarkably high percentage of cell death induced by the complexes in the A549 cells, as compared to control. Annexin-V/PI staining of cells also indicated that the complexes induce cell death through the apoptotic pathway. Our data here suggests that the complexes could be good antitumor agents.
- 出版日期2017-11-1
