The invention relates to the technical field of antitumor drugs, in particular to a Ru (II) complex and a preparation method and application thereof, and the Ru (II) complex has a structure as shown in a formula I. The Ru (II) complex synthesized by the method disclosed by the invention not only has relatively high
cytotoxicity, but also has good photodynamic
antitumor activity. After the complex is illuminated, the efficiency of the complex entering cells in an active transportation mode can be accelerated, mitochondria and
endoplasmic reticulum are targeted at the same time, mitochondrial
membrane potential decline and
endoplasmic reticulum stress are caused to form a dual
organelle damage effect,
immunogenic cell death is caused, the
tumor microenvironment is adjusted, and the tumor
cell immunogenicity is improved. The enrichment of dendritic cells (DCs) in
tumor cells is realized, the chemotactic activity of
effector T cells is improved, the proportion of CD4 < + > and Foxp3 < + >
cell populations is reduced, and finally the anti-tumor immune response is activated. Meanwhile, the complex provided by the invention can also induce the
cell to generate pan
apoptosis, retard the
cell cycle in the G2 / M period and enhance the effect of the complex in inhibiting tumor proliferation.