研究目的
To design and synthesize a new family of water-soluble and bioconjugatable aza-BODIPY fluorophores for in vivo molecular imaging, addressing the limitations of poor water solubility and aggregation in physiological media.
研究成果
The boron-functionalized aza-BODIPY dyes (Wazabys) are highly water-soluble, stable, and non-aggregating in physiological media, with good photophysical properties. They can be easily bioconjugated to antibodies and show promise for in vivo molecular imaging, as demonstrated by successful tumor targeting in mice. This represents a significant improvement over existing fluorophores like cyanines, offering a robust alternative for optical imaging and fluorescence-guided surgery.
研究不足
The quantum yields and brightness of Wazabys are lower in PBS due to non-emissive interactions, which may affect sensitivity. The study is preliminary, and further optimization for clinical applications is needed, including potential issues with penetration depth in optical imaging.
1：Experimental Design and Method Selection:
The study employed a boron-functionalization strategy to synthesize dissymmetric bis-ammonium aza-BODIPY dyes (Wazabys) to improve water solubility and prevent aggregation. Synthetic pathways involved Grignard reactions, peptide coupling, and alkylation steps.
2：Sample Selection and Data Sources:
The aza-BODIPY precursor was synthesized on a gram-scale using Vicente's optimized pathway. In vitro and in vivo studies used CT26 tumor cells and balb/c mice.
3：List of Experimental Equipment and Materials:
Instruments included FPLC for purification, SDS-PAGE for analysis, Odyssey CLx Infrared Imaging System for fluorescence detection, and IVIS Lumina for in vivo imaging. Materials included aza-BODIPY derivatives, anti-PD-L1 antibody, and various chemicals like diethyl squarate.
4：Experimental Procedures and Operational Workflow:
Synthesis involved multiple steps as per Scheme
5：Bioconjugation was done using diethyl squarate. Stability tests in mice plasma, cytotoxicity assays, confocal imaging, and in vivo imaging at time points post-injection were conducted. Data Analysis Methods:
Photophysical properties were measured in DMSO and PBS. Fluorescence quantification used reference standards. Statistical analysis included mean ± SEM and p-values for in vivo studies.
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