The application discloses an NGR
peptide coupled
ruthenium complex and a preparation method and application thereof, and belongs to the technical field of tumor
photodynamic therapy. The application couples NGR
peptide and a two-
photon active
ruthenium complex to construct a double-targeted
photosensitizer. The NGR
oligopeptide can specifically combine with CD13 receptors which are highly expressed on the surface of tumor vascular endothelial cells and
tumor cells, realize double targeting of'vessel+tumor
cell', and significantly improve the tumor enrichment efficiency of drugs. The NGR
peptide coupled
ruthenium complex provided by the application can efficiently generate
active oxygen under the excitation of 820 nm near-
infrared light, specifically kill CD13 positive target cells, and the
tissue penetration depth can reach 250 microns, which is suitable for deep tumor treatment. Meanwhile, the NGR peptide coupled ruthenium complex can efficiently destroy the
pipe forming ability of vascular endothelial cells, and significantly inhibit
tumor angiogenesis.