Linlin Gai, Qianqian Wu, Weice Sun
Natural products and boron-dipyrromethene (BODIPY) dyes represent highly complementary building blocks for the construction of multifunctional theranostic systems. The integration of the intrinsic biological activities and structural diversity of natural products with the excellent photophysical properties of BODIPY fluorophores has enabled the development of a wide range of hybrid platforms for biomedical imaging, phototherapy, drug delivery, and precision medicine. This review provides a comprehensive overview of recent advances in natural product-modified BODIPY systems, with a particular focus on their design strategies, structure-activity relationships, and biomedical applications. Finally, current challenges and future opportunities are highlighted to provide a unified framework for the rational design of next-generation natural product-modified BODIPY systems with enhanced biomedical potential.