期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 161, 期 -, 页码 40-51出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2016.04.031
关键词
Pt(II) complexes; Apoptosis; Plasmid DNA; Platinum accumulation; In vivo test
资金
- Slovenian Research Agency [P1-0134, P3-0003]
To assess the potential cytostatic properties of Pt(II) complexes with 3-hydroxymethylpyridine (3-hmpy) as the only carrier ligand, novel cis-[PtCl2(3-hmpy)(2)] (1) and trans-[PtCl2(3-hmpy)(2)] (2) have been prepared. Elemental analysis, FTIR spectroscopy, multinuclear NMR spectroscopy and X-ray crystallography were used to determine their structures. Based on the results obtained with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and clonogenic assay on T24 human bladder carcinoma cells (T24), the most potent compound 2 was further tested for cytotoxicity in human ovarian carcinoma cell lines - cisplatin sensitive (IGROV 1) and its resistant subclone (IGROV 1/RDDP). The cytotoxicity of compound 2 in IGROV 1/RDDP is comparable to cisplatin. Furthermore, compound 2 induced severe conformational changes in plasmid DNA, which resulted in a delayed onset of apoptosis in T24 cells, and higher amounts of Pt in tumours and serum compared to cisplatin. In addition, in vivo antitumour effectiveness was comparable to that of cisplatin with a smaller reduction of animals' body weight, thus demonstrating that it is a promising transplatin analogue which deserves further studies. (C) 2016 Elsevier Inc. All rights reserved.
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