Wang Jinquan's research group published a new discovery in the journal "CHEMICAL COMMUNICATIONS" of metal ruthenium complexes in the diagnosis and treatment of malignant tumors

Metal ruthenium complexes have excellent photophysical activity and strong tumor cytotoxicity, and have good development prospects in the diagnosis and treatment of malignant tumors. At present, four ruthenium complexes have entered clinical research, but "poor tumor targeting" is still a serious problem in the research of this class of drugs. In order to further improve the tumor targeting of this kind of ruthenium complexes, Wang Jinquan's research group targeted integrin α v β 3 , which is specifically and highly expressed on the surface of tumor cell membranes , and used its specific ligand RGD (Arg-Gly-Asp) The oligopeptide is used as the guiding molecule to construct the RGD peptide-coupled ruthenium complex with the functions of tumor cell mitochondria targeted killing and imaging. The first stage of tumor targeting is achieved by using the characteristic of RGD peptide to specifically recognize tumor cells, and the second stage of targeting is achieved by using the characteristic of ruthenium complexes that can accumulate in mitochondria after entering cells. Through this step-by-step dual targeting difference The recognition pattern enables this kind of complexes to finally target and kill tumor cells while having little impact on normal cells, meeting the design requirements of high efficiency and low toxicity. At the same time, by using the two-photon absorption characteristics of ruthenium complexes, photodynamic therapy of tumors in mice has been realized, which is for the development of "integration of diagnosis and treatment" dual-functional targeted anti-tumor drugs with dynamic monitoring of tumor recognition and photodynamic killing activity. Establish foundation. The research results have been published in high-level international journals in the field of chemistry,【Two-photon photodynamic ablation of tumor cells using an RGD peptide-conjugated ruthenium(II) photosensitiser , Chemical Communications , 56, 12542-12545 , 2020. IF=5.9 ], and obtained the invention patent authorization [patent number: 201810290720.4 ]

Schematic diagram of the two-photon photodynamic therapy mechanism of RGD peptide-coupled ruthenium complex targeting tumor cell mitochondria