4.6 Article

Systematic evaluation of the antitumor activity of three ruthenium polypyridyl complexes

期刊

JOURNAL OF INORGANIC BIOCHEMISTRY
卷 225, 期 -, 页码 -

出版社

ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2021.111616

关键词

Antitumor activity; Ruthenium(II) complexes; Cell cycle arrest; Apoptosis; Mitochondria

资金

  1. Guangxi Natural Science Foundation [2018GXNSFBA050024, 2020GXNSFAA297227]
  2. Guangxi Science and Technology Base and Special Fund for Talents [AD19245008]
  3. Key Laboratory of Electrochemical and Magneto-chemical Function Materials [EMFM20211123]
  4. Ph.D. Scientific Research Foundation of Guilin University of Technology

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Ruthenium-containing complexes show excellent cytotoxicity against HepG-2 cells, exhibit better antitumor activity than cisplatin, and have no obvious toxicity to normal cells. DNA binding results suggest interaction with DNA, and the complexes induce apoptosis through different pathways.
Ruthenium-containing complexes have emerged as good alternative to the currently used platinum-containing drugs for malignant tumor therapy. In this work, cytotoxic effects of recently synthesized ruthenium polypyridyl complexes [Ru(bpy)(2)(CFPIP)](ClO4) ( )(bpy = 2,2'-bipyridine, CFPIP = (E)-2-(4 fluorostyryl)-1H-imidazo [4, 5-f][1,10]phenanthmline, Ru(II)-1), [Ru(phen) 2 (CFPIP)](ClO4)(2) (phen = 1,10-phenanthroline, Ru(II)-2) and [Ru(dmb)(2) (CFPIP)](ClO4)(2) (dmb = 4,4'-dimethyl-2,2'-bipyridine, Ru(II)-3) toward different tumor cells were investigated in vitro and compared with cisplatin, the most widely used chemotherapeutic drug against hepatocellular carcinoma (HepG-2). The results demonstrate that target complexes show excellent cytotoxicity against HepG-2 cells with low IC50 value of 21.4 +/- 1.5, 18.0 +/- 2.1 and 22.3 +/- 1.7 mu M, respectively. It was important noting that target Ru(II) complexes exhibited better antitumor activity than cisplatin (IC50 = 28.5 +/- 2.4 mu M) against HepG-2 cells, and has no obvious toxicity to normal cell L02. DNA binding results suggest that Ru(II)-1, Ru(II)-2 and Ru(II)-3 interact with CT DNA (calf thymus DNA) through intercalative mode. Complexes exerted its antitumor activity through increasing anti-migration and inducing cell cycle arrest at the S phase. In addition, the apoptosis was tested by AO (acridine orange)/EB (ethidium bromide) staining and flow cytometry. Mitochondrial membrane potential (MMP), reactive oxygen species (ROS), and colocalization tests were also evaluated by ImageXpress Micro XLS system. Overall, the results show that the ruthenium polypyridyl complexes induce apoptosis in HepG-2 cells through ROS-mediated mitochondria dysfunction pathway.

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