期刊
JOURNAL OF COORDINATION CHEMISTRY
卷 69, 期 10, 页码 1653-1662出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/00958972.2016.1180373
关键词
Platinum(II) complexes; cytotoxicity; flow cytometry; interaction with DNA
资金
- National Natural Science Foundation of China [21271041]
- New Drug Creation Project of the National Science and Technology Major Foundation of China [2013ZX09402102-001-006]
- Fundamental Research Funds for the Central Universities [2242013K30011]
- Natural Science Foundation of Jiangsu Province [BK20151402]
- Open Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University
- Scientific Research Innovation Project for College Graduates of Jiangsu Province [KYLX15_0128]
(1R,2R)-N-1-2-amyl-1,2-diaminocyclohexane, which has an amyl substituent as compared with 1,2-diaminocyclohexane, was used as the carrier group to construct three platinum(II) complexes. MTT assay revealed that the complexes showed decent cytotoxicity against all of the four tested tumor cell lines with the IC50 values ranging from 1.08 to 253.36M. Particularly, the IC50 values of 2 against A549 and HCT-116 reached 3.32 and 1.08M, respectively, which were much lower than those of cisplatin and oxaliplatin. Flow cytometry demonstrated that 2 inhibited HepG2 cells proliferation and caused cytotoxicity by inducing apoptosis and arresting cells in the G2 phase. Furthermore, agarose gel electrophoresis showed that 2 had the ability to interact with DNA in a manner different from cisplatin and oxaliplatin, indicating the carrier ligand with an alkyl moiety had an influence on the action mode of the complex. [GRAPHICS] .
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