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However, their significance extends beyond their natural origin, as they represent the products of chemo\u2010biodiversity shaped by millions of years of evolutionary adaptation to diverse ecological pressures. This review examines natural photosensitizers through a chemo\u2010biodiversity perspective, emphasizing how evolutionary diversification has generated structurally distinct photoactive scaffolds with unique photophysical and photobiological properties relevant to cancer therapy. Attention is given to the relationships between molecular architecture, excited\u2010state dynamics, reactive oxygen species generation, and therapeutic performance, highlighting how structural features govern photodynamic efficiency and biological responses. The review further discusses how nanotechnology\u2010based engineering strategies can overcome intrinsic limitations, including poor aqueous solubility, aggregation, photoinstability, and limited tumor selectivity. Recent advances in multifunctional nanoplatforms, molecular engineering, and combination therapies are critically evaluated alongside current translational challenges, including manufacturing, regulatory considerations, and clinical development. By integrating natural product chemistry, photophysics, photobiology, and nanotechnology within a unified conceptual framework, this review demonstrates that chemo\u2010biodiversity provides a rational foundation for the discovery of next\u2010generation natural photosensitizers. 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