A microRNA-responsive xanthene-hemicyanine fluorescent dye, a two-component probe system thereof, a synthesis method and application thereof

By designing a two-component probe system based on oxanthracene-hemicyanine near-infrared fluorescent dye, the problem of insufficient stability of existing probes in complex biological environments was solved, enabling high-specificity and high signal-to-noise ratio microRNA detection and treatment, thus improving the effectiveness of early tumor diagnosis and treatment.

CN121673852BActive Publication Date: 2026-06-19DALIAN UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
DALIAN UNIV OF TECH
Filing Date
2026-02-09
Publication Date
2026-06-19

AI Technical Summary

Technical Problem

Existing microRNA-responsive near-infrared fluorescent probes lack stability in complex biological environments, leading to reduced signal-to-noise ratios and non-specific background reactions. This increases the difficulty of research and development and the uncertainty of clinical translation, affecting the effectiveness of early tumor diagnosis and treatment.

Method used

A microRNA-21-responsive xanthracene-hemicyanine near-infrared fluorescent dye was designed to achieve specific recognition and activation through a two-component probe system, comprising a first probe component and a second probe component. The dye utilizes a bioorthogonal reaction to activate fluorescence emission and photosensitivity in the presence of the target microRNA. A specific combination of R1, R2, X, and Y groups is used to enhance the fluorescence quantum yield. The dye is also linked to short-chain RNA via amide or ester bonds to form a ternary hybridization complex.

Benefits of technology

It achieves highly specific and high signal-to-noise ratio microRNA detection and treatment, avoids degradation and non-specific binding of single-stranded probes, significantly improves detection accuracy and treatment efficacy, and has good biosafety and tissue penetration ability, making it suitable for in vivo applications.

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Abstract

This invention discloses a microRNA-responsive oxanthracene-hemicyanine fluorescent dye, its two-component probe system, synthesis method, and applications. The fluorescent dye structure is shown in general formula I, and it can be linked to a target ligand (such as short-chain RNA) via a carboxyl group. The two-component probe system consists of two short-chain RNAs, each linked with the dye and a bioorthogonal reaction pair (such as tetrazine). The bioorthogonal reaction is triggered by hybridization mediated by the target microRNA-21, specifically activating the near-infrared fluorescence and photosensitivity of the dye. This dye and probe system can achieve high signal-to-noise ratio fluorescence imaging of overexpressed microRNA-21 in tumors and generate reactive oxygen species under laser irradiation for photodynamic therapy, thus achieving integrated diagnosis and treatment. The dye and probe system provided by this invention has advantages such as high biosafety, simple preparation, and high specificity, and has broad application prospects in the early diagnosis and treatment of malignant tumors.
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