探究新型杀结核菌素-Pt(II)配合物的DNA反应活性及抗癌特性
Probing the DNA Reactivity and the Anticancer Properties of a Novel Tubercidin-Pt(II) Complex.
作者信息
D'Errico Stefano, Falanga Andrea Patrizia, Capasso Domenica, Di Gaetano Sonia, Marzano Maria, Terracciano Monica, Roviello Giovanni Nicola, Piccialli Gennaro, Oliviero Giorgia, Borbone Nicola
机构信息
CESTEV, University of Naples Federico II, via Tommaso De Amicis, 95, 80145 Napoli, Italy.
Dipartimento di Medicina Molecolare e Biotecnologie Mediche, University of Naples Federico II, via Sergio Pansini, 5, 80131 Napoli, Italy.
出版信息
Pharmaceutics. 2020 Jul 4;12(7):627. doi: 10.3390/pharmaceutics12070627.
Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium . In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit in the molecular scaffold. The behavior of the synthesized complex with a double-strand DNA model was monitored by CD spectroscopy and compared with that of cisplatin and tubercidin. In addition, the cell viability was evaluated against HeLa, A375 and WM266 human cancer cell lines using the MTT test. Lastly, the results of the apoptotic assay (FITC Annexin V) performed on the HeLa cancer cell line are also reported.
在此，我们报道了一种新型Pt(II)中性配合物的合成，该配合物以核苷结核菌素作为配体，结核菌素是一种从细菌中提取的强效抗肿瘤剂。具体而言，通过安装在结核菌素C6嘌呤位置的二胺连接体与金属的螯合，确保了在分子支架中引入类似顺铂的单元。通过圆二色光谱监测合成配合物与双链DNA模型的相互作用，并与顺铂和结核菌素进行比较。此外，使用MTT试验评估了该配合物对HeLa、A375和WM266人癌细胞系的细胞活力。最后，还报道了对HeLa癌细胞系进行的凋亡检测（FITC Annexin V）结果。
Zotero 插件