An icd inducer ru(ii) complex with the ability of photodynamic DNA cleavage, and a preparation method and application thereof

By designing ICD inducer Ru(II) complexes with photodynamic DNA-breaking capabilities, highly efficient nuclear-targeted damage and immune activation of tumor cells were achieved, overcoming the shortcomings of existing Ru(II) complexes in tumor therapy, enhancing anti-tumor immune responses, and demonstrating good biosafety.

CN120682279BActive Publication Date: 2026-03-17DONGGUAN SOUTHEAST CENTRAL HOSPITAL (DONGGUAN SOUTHEAST TRADITIONAL CHINESE MEDICINE MEDICAL SERVICE CENTER DONGGUAN FIRST HOSPITAL AFFILIATED TO GUANGDONG MEDICAL UNIVERSITY)
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Patent Information

Application Number
CN202510871196.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-06-26
Publication Date
2026-03-17
Estimated Expiration
2045-06-26

AI Technical Summary

Technical Problem

Existing Ru(II) complexes have several drawbacks in tumor therapy, including insufficient apoptosis/necrosis induction, lack of clear nuclear-targeted DNA breakage ability, unclear activation mechanism of the cGAS-STING immune pathway, and lack of systematic verification of in vivo anti-tumor immune effects.

Method used

We designed an ICD inducer Ru(II) complex with photodynamic DNA breaking ability to induce mitochondrial damage and endoplasmic reticulum stress through a cascade delivery mechanism from mitochondria and endoplasmic reticulum to the nucleus, thereby breaking DNA in the nucleus and activating pyroptosis and immunogenic death mediated by the cGAS-STING pathway.

Benefits of technology

It enhances the anti-tumor immune effect of tumor cells, strengthens the body's anti-tumor immune response, and demonstrates good biosafety and immune cell efficacy in in vivo experiments.

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Abstract

The application discloses an ICD inducer Ru(II) complex with a light-driven DNA breaking ability, a preparation method and application thereof, relates to the field of antitumor drugs, and the structural formula of the Ru(II) complex is [Ru(dip)2(L)](PF6)2. The Ru(II) complex can enter a cell nucleus to break DNA and activate immunogenic death mediated by the pyroptosis and cGAS-STING pathways by using photodynamic therapy, so that the antitumor immune effect of the body is improved. In the in-vivo experiment, the immune cells in the tumor microenvironment of the mice in the vaccine group are good, and the antitumor immune effect of the three injections of the vaccine is better. The results of H&E staining show that the vaccine does not cause obvious pathological damage to the main organs of the mice, and the vaccine has good biological safety.
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