Abstract: The present invention discloses a capsaicin-derived photosensitizer, and a preparation method and use thereof. Boron-dipyrromethene is used as a core of the photosensitizer, which has a maximum absorption peak red-shifted to the near infrared region by expanding the ? system and is introduced with a capsaicin-targeting group to construct a capsaicin-derived photosensitizer cap-BDP with high-performance targeting of TRPV1 protein. The photosensitizer can generate singlet oxygen under low-power LED irradiation, which specifically activates the TRPV1 protein pathway, causes significant calcium influx, and induces apoptosis of tumor cells. Moreover, the generated singlet oxygen directly oxidizes endogenous substances in cells to cause cell apoptosis, eventually achieving light-induced bifunctional synergistic therapy.