A small molecule pyroptosis inducer and its application as a tumor sonodynamic therapeutic agent

By designing the small molecule pyroptosis inducer Rd-TTPA, and utilizing the enhanced DA structure and low-frequency ultrasound-mediated reactive oxygen species generation, the problem of targeted tumor cell and deep tumor treatment has been solved, achieving efficient and safe tumor ablation and imaging monitoring.

CN117603197BActive Publication Date: 2026-04-21HUBEI UNIV
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Patent Information

Application Number
CN202311618429.2
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-11-28
Publication Date
2026-04-21
Estimated Expiration
2043-11-28

AI Technical Summary

Technical Problem

Existing pyroptosis inducers lack the ability to target tumor cells, making it impossible to monitor their retention at the tumor site and their distribution in the body. Furthermore, chemotherapy drugs have tumor resistance and serious toxic side effects, while photodynamic therapy has low killing efficiency for deep tumors and adverse side effects on normal tissues.

Method used

A small molecule pyroptosis inducer, Rd-TTPA, was developed. Through an enhanced DA structure composed of N,N-diethylimine, rhodamine scaffold, thiophene, and triphenylamine groups, it utilizes low-frequency ultrasound-mediated reactive oxygen species generation to achieve mitochondrial targeting of tumor cells and near-infrared II fluorescence imaging, thereby enhancing sonodynamic therapy.

Benefits of technology

Rd-TTPA can efficiently target tumor cell mitochondria, reduce toxic side effects on normal tissues, achieve deep tissue ablation, and has good biocompatibility and imaging monitoring capabilities, thus improving the efficiency and safety of tumor treatment.

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Abstract

This invention discloses a small-molecule pyroptosis inducer for tumor cells. It utilizes an N,N-diethylimine group as an electron acceptor (A), a rhodamine scaffold as a π-conjugated system, thiophene and triphenylamine groups as the first electron donor (D1) and second electron donor (D2), respectively, and a rotatable vinyl and C-C single bond to increase intramolecular motion, forming a novel A-π-D1-D2 type small-molecule pyroptosis inducer, Rd-TTPA, with enhanced D-A structure and intramolecular motion. This small-molecule pyroptosis inducer can efficiently target tumor cell mitochondria, inducing pyroptosis through ultrasound-mediated reactive oxygen species production. It can serve as an enhanced sonodynamic deep tumor therapeutic agent guided by near-infrared II (NIR-II) fluorescence imaging.
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