Zhou Zhiping, Chen Feihong, Xu Gang, Gou Shaohua
Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China; Jiangsu Province Hi-Tech Key Laboratory for Bio-medical Research, Southeast University, Nanjing 211189, China.
Bioorg Med Chem Lett. 2016 Jan 15;26(2):322-327. doi: 10.1016/j.bmcl.2015.12.019. Epub 2015 Dec 8.
Three platinum(II) complexes of (1R,2R)-N(1)-cyclopentyl-1,2-cyclohexanediamine with malonate derivatives were designed, synthesized and spectrally characterized. MTT assay showed that the complexes possessed positive cytotoxic effect on the four human solid tumor cell lines. Among the complexes, complex 2 demonstrated the strongest cytotoxic activity compared to cisplatin and oxaliplatin against HepG2 cell line (IC50=3.04μM). Furthermore, the results of gel electrophoresis revealed that complex 2 interacted with DNA in a different mode from that of cisplatin. Mechanism studies of cell proliferation inhibition and cellular uptake indicated that complex 2 entered HepG2 cell more efficiently than cisplatin, exhibited massive G2 accumulation and then induced apoptosis.
设计、合成并通过光谱表征了三种(1R,2R)-N(1)-环戊基-1,2-环己二胺与丙二酸衍生物的铂(II)配合物。MTT 法表明这些配合物对四种人类实体瘤细胞系具有阳性细胞毒性作用。在这些配合物中，与顺铂和奥沙利铂相比，配合物2对HepG2细胞系表现出最强的细胞毒性活性(IC50 = 3.04μM)。此外，凝胶电泳结果表明配合物2与DNA的相互作用方式与顺铂不同。细胞增殖抑制和细胞摄取的机制研究表明，配合物2比顺铂更有效地进入HepG2细胞，表现出大量的G2期积累，然后诱导细胞凋亡。
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