Artemisinin-conjugated phototheranostic probe for golgi-targeted H2O2 detection and side effect attenuation

ABSTRACT Elucidating the mechanism by which artemisinin conjugated with phototheranostic probes alleviates side effects (AC-Pr-RSE) is critical for optimizing therapeutic outcomes. Herein, we report for the first time a cytotoxic artemisinin derivative conjugated with N-methyliminodiacetic acid (MIDA) boronate and labeled with a naphthalimide fluorophore, specifically tailored for Golgi apparatus-targeted H 2 O 2 detection. Comparative analysis with commercial organelle-specific dyes confirms the Golgi apparatus as the primary accumulation site of this conjugate. It effectively elevates intracellular reactive oxygen species (ROS) levels, induces cell apoptosis, and thereby reduces off-target side effects. This work underscores the potential of AC-Pr-RSE and offers a new design strategy for high-performance theranostic probes, addressing traditional limitations to further enhance bioactivity and therapeutic precision.