Abstract
Determining therapeutic efficacy is critical for tumor precision theranostics. In order to monitor the efficacy of anti-cancer drugs (e.g., Paclitaxel), a pH-sensitive ratiometric fluorescent imaging probe was constructed. The pH-sensitive ratiometric fluorescent dye ANNA was covalently coupled to the N-terminal of the cell-penetrating TAT peptide through an amidation reaction (TAT-ANNA). The in vitro cellular experiments determined that the TAT-ANNA probe could penetrate the cell membrane and image the intracellular pH in real time. The in vivo experiments were then carried out, and the ratiometric pH response to the state of the tumor was recorded immediately after medication. The TAT-ANNA probe was successfully used to monitor the pharmacodynamics of anti-cancer drugs in vivo.
Highlights
Due to high risk, tumor theranostics has become the main focus and challenge in clinical medicine and medical investigations
TAT was used as a transduction domain which was covalently coupled with ANNA through the terminal amino group of each TAT and the carboxyl group of ANNA via amidation reactions
This is the typical absorption of ANNA, which indicates that the construction of the probe was successful
Summary
Tumor theranostics has become the main focus and challenge in clinical medicine and medical investigations. Determining how to predict changes in tumors earlier, especially in consideration of the fast evaluation of drug efficacy, is a prerequisite for directing therapeutic administration. The fluorescence intensity, based on conventional fluorescent probes, always suffers from several interferences, such as self-quenching at high concentrations, autofluorescence from biological tissues, and different settings of instrumental parameters, which lead to deviations in the imaging results [16,17]. We report the findings of a novel ratiometric fluorescent pH probe based on a pH-sensitive ratiometric fluorescent dye, ANNA, and a cell-penetrating peptide, TAT (TAT-ANNA), to sensitively monitor the intracellular pH, thereby evaluating the pharmacodynamics of anti-cancer drugs in vivo. Through a series of in vitro and in vivo experiments, the performance of TAT-ANNA was evaluated This probe successfully penetrated the cell membrane and imaged the intracellular pH. It could respond to the state of the tumor immediately after medication to provide a reliable pharmacodynamic evaluation
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