Cytotoxicity, Apoptosis, Cellular Uptake, Cell Cycle Distribution, and DNA-Binding Investigation of Ruthenium Complexes

Autor: Xin-Yan Li, Qi-Feng Guo, Qing-Hua Liu, Jian-Hua Zhao, Jian-Wei Wang, Hai-Feng Wu, Si-Hong Liu, Hui-Hua Xu
Rok vydání: 2012
Předmět:
Zdroj: DNA and Cell Biology. 31:1205-1213
ISSN: 1557-7430
1044-5498
DOI: 10.1089/dna.2011.1490
Popis: Three new ruthenium(II) polypyridyl complexes [Ru(bpy)(2)(BHIP)](2+) 1, [Ru(phen)(2)(BHIP)](2+) 2, and [Ru(dip)(2)(BHIP)](2+) 3 were synthesized and characterized. The cytotoxicity of the three complexes was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The apoptosis induced by the complexes was studied by cell morphology and flow cytometry. The results showed that the percentage of apoptotic cells is 7.19%, 75.58%, and 3.51% in the presence of complexes 1, 2, and 3, respectively. The cellular uptakes were also performed and the results indicated that complexes 1, 2, and 3 can enter into the cytoplasm and also into the nucleus. The studies on antiproliferative mechanism showed the induction of S-phase arrest by complexes 1, 2, and 3. DNA-binding constants of these complexes with calf thymus DNA (CT-DNA) were determined to be 1.07 (± 0.47) × 10(5) M(-1) (s = 2.04), 1.21 (± 0.32) × 10(5) M(-1) (s = 1.88), and 2.75 (± 0.27) × 10(5) M(-1) (s = 2.17), respectively. Upon irradiation at 365 nm, complexes 1, 2, and 3 can induce cleavage of pBR322 DNA.
Databáze: OpenAIRE