基于配合物[Ru(phen)(mitatp)] 的光断裂性质和抗肿瘤活性研究.doc

基于配合物[Ru(phen)2(mitatp)]2+的光断裂性质和抗肿瘤活性研究  Synthesis, visible light photocleavage, antiproliferative and 5 10 15 20 25 30 35 40 cellular uptake properties of ruthenium complex [Ru phen 2 mitatp ]2+# Yu Huijuan, Yu Lin, Hao Zhifeng, Zhou Lihua, Xie Zhenming* Faculty of Chemical Engineering and Light Industry, Guangdong University of Technology, GuangZhou 510006 Abstract: A new ruthenium complex [Ru phen 2 mitatp ]2+ phen 1,10-phenanthroline, mitatp 5-methoxy-isatino[1,2-b]-1,4,8,9-tetraazatriphenylene has been synthesized and characterized. The interaction of the complex with DNA has been studied and the results indicate that [Ru phen 2 mitatp ]2+ could efficiently photocleave pBR322 DNA under irradiation at visible light and the singlet oxygen 1O2 was proved to be reactive species in the photocleavage process. The cytotoxicity has also been evaluated by MTT method, and [Ru phen 2 mitatp ]2+ shows prominent anticancer activity against various cancer cells. Live cell imaging study and flow cytometric analysis demonstrate that the complex could cross cell membrane accumulating in the nucleus and inducing cell death by induction of G0/G1 cells cycle arrest and apoptosis. Keywords: Ruthenium complex; DNA photocleavage; Cytotoxicity; Apoptosis 0 Introduction Although cis-platinum and other platinum complexes as anticancer drugs has acquired remarkable success in treatment of various cancers, such as testicular, ovarian, cervical, bladder, head and neck, and lung cancers, their clinical drawbacks are also apparent, including the limited applicability, the acquired resistance, and the serious side effects [1-4]. The limitations of cis-platinum have motivated extensive investigations into alternative metal-based anticancer agents. Among the non-platinum metal anticancer agents, ruthenium complexes have drawn much attention due to their favorable properties, such as high cytotoxicity against cancer cells, lower toxicity toward healthy tissue