Details

Autor(en) / Beteiligte

• Ma, Tieliang
• Xu, Jun
• Wang, Yuan
• Yu, Hao
• Yang, Yong
• Liu, Yang
• Ding, Weiliang
• Zhu, Wenjiao
• Chen, Ruhua
• Ge, Zhijun
• Tan, Yongfei
• Jia, Lei
• Zhu, Taofeng

Titel

Ternary copper(II) complexes with amino acid chains and heterocyclic bases: DNA binding, cytotoxic and cell apoptosis induction properties

Ist Teil von

• Journal of inorganic biochemistry, 2015-03, Vol.144, p.38-46

Ort / Verlag

United States: Elsevier Inc

Erscheinungsjahr

2015

Quelle

MEDLINE

Beschreibungen/Notizen

• Nowadays, chemotherapy is a common means of oncology. However, it is difficult to find excellent chemotherapy drugs. Here we reported three new ternary copper(II) complexes which have potential chemotherapy characteristics with reduced Schiff base ligand and heterocyclic bases (TBHP), [Cu(phen)(TBHP)]H2O (1), [Cu(dpz)(TBHP)]H2O (2) and [Cu(dppz)(TBHP)]H2O (3) (phen=1,10-phenanthroline, dpz=dipyrido [3,2:2′,3′-f]quinoxaline, dppz=dipyrido [3,2-a:2′,3′-c]phenazine, H2TBHP=2-(3,5-di-tert-butyl-2-hydroxybenzylamino)-2-benzyl-acetic acid). The DNA-binding properties of the complexes were investigated by spectrometric titrations, ethidium bromide displacement experiments and viscosity measurements. The results indicated that the three complexes, especially the complex 13, can strongly bind to calf-thymus DNA (CT-DNA). The intrinsic binding constants Kb of the ternary copper(II) complexes with CT-DNA were 1.37×105, 1.81×105 and 3.21×105 for 1, 2 and 3 respectively. Comparative cytotoxic activities of the copper(II) complexes were also determined by 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results showed that the ternary copper(II) complexes had significant cytotoxic activity against the human lung cancer (A549), human esophageal cancer (Eca109) and human gastric cancer (SGC7901) cell lines. Cell apoptosis were detected by AnnexinV/PI flow cytometry and by Western blotting with the protein expression of p53, Bax and Bcl-2. All the three copper complexes can effectively induce apoptosis of the three human tumor cells. Three new ternary copper(II) complexes which have potential chemotherapy characteristics with reduced Schiff base ligand and heterocyclic bases, and the ternary copper(II) complexes had significant cytotoxic activity against the human cancer cell lines. They also can induce the cancer cell apoptosis. [Display omitted] •The biological activity of three dinuclear copper(II) complexes was investigated.•The three complexes can cause DNA damage.•Cell apoptosis was detected by AnnexinV/PI flow cytometry and Western blotting.•All the complexes can effectively induce apoptosis of the human tumor cells.