title: Synthesis and crystal structure determination of copper(II)-complex: In vitro DNA and HSA binding, pBR322 plasmid cleavage, cell imaging and cytotoxic studies.
abstract: New Cu(II) complex 1 of indole-3-propionic acid and 1,10-phenanthroline was synthesized and characterized by analytical, spectroscopic and single crystal X-ray diffraction. In vitro DNA binding studies of 1 was performed by employing UV-vis and fluorescence spectroscopic techniques. The binding affinity towards human serum albumin (HSA) was also investigated to understand the carrier role in body system, as the time dependent HPLC experiment of 1 revealed that bonded drug with protein releases slowly in presence of DNA. Complex 1 exhibited good anti-tumor activity (GI50 values <10 μg/ml), and to elucidate the mechanism of tumor inhibition, topoisomerase I enzymatic activity was carried out and further validated by cell imaging studies which clearly showed its nuclear localization.
authors: Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India. Electronic address: tsartaj62@yahoo.com.
authors: Sartaj
authors: S
authors: Tabassum
authors: Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
authors: Mehvash
authors: M
authors: Zaki
authors: Department of Chemistry, Indian Institute of Technology Kanpur, UP 208016, India.
authors: Musheer
authors: M
authors: Ahmad
authors: Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
authors: Mohd
authors: M
authors: Afzal
authors: Department of Biochemistry, Faculty of Science, Banaras Hindu University, Varanasi 221005, India.
authors: Saurabh
authors: S
authors: Srivastav
authors: Department of Biochemistry, Faculty of Science, Banaras Hindu University, Varanasi 221005, India.
authors: Saripella
authors: S
authors: Srikrishna
authors: Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
authors: Farukh
authors: F
authors: Arjmand
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D003300:Copper / Q000737:chemistry*; D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D053837:DNA Cleavage / Q000187:drug effects*; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000737:chemistry; D062105:Molecular Docking Simulation; D057054:Molecular Imaging; D009690:Nucleic Acid Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D010618:Phenanthrolines / Q000737:chemistry; D055668:Photochemical Processes; D010957:Plasmids / Q000235:genetics; D011487:Protein Conformation; D012709:Serum Albumin / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D009942:Organometallic Compounds; D010618:Phenanthrolines; D012709:Serum Albumin; D003300:Copper; C015292:indolepropionic acid; D004247:DNA; D004264:DNA Topoisomerases, Type I; C025205:1,10-phenanthroline
keywords: Anticancer activity; DNA cleavage; HSA binding; In vitro DNA binding; SDS-PAGE analysis; Topo-I inhibition