title: Anticancer activity and DNA-binding investigations of the Cu(II) and Ni(II) complexes with coumarin derivative.
abstract: Two new copper(II) (2) and nickel(II) (3) complexes with a new coumarin derivative have been synthesized and structurally characterized. The DNA-binding activities of the two complexes have been investigated by spectrometric titrations, ethidium bromide displacement experiments, CD (circular dichroism) spectral analysis, and viscosity measurements. The results indicate that the two complexes, especially the complex 2, can strongly bind to calf-thymus DNA (CT--DNA). The intrinsic binding constants Kb of the complexes with CT-DNA are 2.99 × 10(5) and 0.61 × 10(5) for 2 and 3, respectively. Comparative cytotoxic activities of the two complexes are also determined by MTT assay. The results show that the drugs designed here have significant cytotoxic activity against the human hepatic (HepG2), human promyelocytic leukemia (HL60), and human prostate (PC3) cell lines. Cell apoptosis was detected by Annexin V/PI flow cytometry, and the results show that the two copper complexes can induce apoptosis of the three human tumor cells. In conclusions, the two complexes show considerable cytotoxic activity against the three human cancer and induce apoptosis of the threes.
authors.affiliation: Department of Respiratory, The Affiliated Yixing Hospital of Jiangsu University, #75 Tongzhenguan Road, Yixing, Jiangsu Province, 214200, China.
authors.forename: Taofeng
authors.initials: T
authors.lastname: Zhu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Wang
authors.forename: Weiliang
authors.initials: W
authors.lastname: Ding
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
authors.forename: Ruhua
authors.initials: R
authors.lastname: Chen
authors.forename: Jing
authors.initials: J
authors.lastname: Xie
authors.forename: Wenjiao
authors.initials: W
authors.lastname: Zhu
authors.forename: Lei
authors.initials: L
authors.lastname: Jia
authors.forename: Tieliang
authors.initials: T
authors.lastname: Ma
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002417:Cattle; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D056831:Coordination Complexes / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D003300:Copper / Q000737:chemistry*; D003374:Coumarins / Q000737:chemistry*; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D053837:DNA Cleavage / Q000187:drug effects; D018922:HL-60 Cells; D056945:Hep G2 Cells; D006801:Humans; D009532:Nickel / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D003374:Coumarins; D003300:Copper; D009532:Nickel; D004247:DNA; C427203:calf thymus DNA; C030123:coumarin
keywords: DNA-binding properties; anticancer activity; cell apoptosis; coumarin derivative; human tumor cell lines