Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, P. R. China.
J Med Chem. 2023 Sep 28;66(18):13103-13115. doi: 10.1021/acs.jmedchem.3c01126. Epub 2023 Sep 19.
Herein, four planar cyclometalated platinum(II) complexes with a main ligand of enlarged aromatic rings have been assessed as effective anticancer theranostic agents for the first time. With an increased number of aromatic rings in the N∧N ligand, - exhibit increased lipophilicity and cytotoxicity selectivity. The intensity of the Pt-Pt interaction of each complex can be indicated by an enhanced near-infrared (NIR) emission in phosphate-buffered saline (PBS), their binding activity with biomolecules of bovine serum albumin (BSA) is accompanied by a vivid turn-on green emission, and the intensity gradually decreased from to , which is consistent with the docking of two complexes with BSA. Both "turn-on" NIR and green emission of can be mainly observed in nuclei of living cell within 24 h, while two phosphorescence traces of were recorded in lysosomes by confocal imaging. Moreover, shows the highest efficiency in inducing oncosis of Hela cells, and the relative process was investigated.
本文首次评估了四个具有大环主配体的平面金属铂(II)配合物作为有效的癌症治疗诊断试剂。随着 N∧N 配体中芳香环数量的增加,-表现出更高的亲脂性和细胞毒性选择性。每个配合物中 Pt-Pt 相互作用的强度可以通过增强近红外(NIR)发射在磷酸盐缓冲盐水(PBS)中指示,它们与牛血清白蛋白(BSA)生物分子的结合活性伴随着生动的绿色开启发射,强度从逐渐降低到 ,这与两个与 BSA 结合的复合物一致。在 24 小时内,“开启”NIR 和 的绿色发射可以主要在活细胞的核内观察到,而 通过共聚焦成像在溶酶体中记录了两个磷光轨迹。此外,在诱导 Hela 细胞胀亡方面表现出最高的效率,并研究了相对过程。