Potential apoptosis inducing agents based on a new benzimidazole schiff base ligand and its dicopper(II) complex

作者：Paul, Anup; Gupta, Rakesh Kumar; Dubey, Mrigendra; Sharma, Gunjan; Koch, Biplob; Hundal, Geeta; Hundal, Maninderjeet Singh; Pandey, Daya Shankar^*

来源：RSC Advances, 2014, 4(78): 41228-41236.

DOI：10.1039/c4ra08680e

• METAL-COMPLEXES
• COPPER(II) COMPLEXES
• ANTIFUNGAL ACTIVITY
• CU(II) COMPLEXES
• ANTICANCER
• WATER
• CYTOTOXICITY
• EFFICACY

Synthesis, characterization and antiproliferative activity of a new benzimidazole based Schiff base 2-(1-methyl-1-H-benzimidazol-2-yl) phenyl)imino)methyl)phenol (HL) and dicopper(II) complex [{Cu(L)NO3}(2)] (CuL) containing L- has been described. Both HL and CuL have been meticulously characterized by satisfactory elemental analyses, FT-IR, NMR, ESI-MS, electronic absorption and emission spectroscopy, and their structures unambiguously determined by X-ray single crystal analyses. Titration studies (absorption and emission) revealed interaction of the ligand and its dicopper(II) complex with DNA/BSA and stronger affinity of the CuL relative to HL. Binding of the HL and CuL with DNA/BSA have been validated by in silico studies and their cytotoxic effect on human breast cancer cell lines (MCF-7) by MTT assay. IC50 values (458 mu M and 22 mu M for HL, CuL) clearly suggested substantial cytotoxicity of the complex CuL toward MCF-7 compared to the ligand HL. Greater antiproliferative efficacy of the CuL in contrast to HL has been evidenced by fluorescence activated cell sorting (FACS) and AO/EB fluorescence staining. The possible mode of the apoptotic pathway for CuL has further been affirmed by reactive oxygen species (ROS) generation studies.

• 出版日期2014