The effect of Zn2+ doping on photocatalytic and biomedical properties of CuO synthesized by the simple hydrothermal method was analyzed in this study. The phase structure, morphology, and surface chemistry of synthesized CuO and CuO:Zn2+ samples were analyzed. XRD analysis revealed the monoclinic phase of synthesized CuO. Due to the concentration of precursors and optimization of processing conditions, the morphology of CuO appears to be like pine needles. It is transformed from pine needles to blocks by incorporating Zn into the CuO matrix. In this study, CuO and CuO:Zn2+ photocatalysts were used for the degradation of Methylene Blue (MB) dye under UV light irradiation. The photocatalytic degradation process was studied under different conditions, including time-based study, pH, and catalyst concentration. Results showed that both CuO and CuO:Zn2+ photocatalysts were effective in degrading MB dye under UV light irradiation. The rate of dye degradation increased with increasing irradiation time. Moreover, the MTT approach was employed to evaluate the cell viability of MCF-7 cancer cells both in the absence and presence of UV radiation. The proportion of MCF-7 cells destroyed was elevated due to the easy diffusion of CuO and CuO:Zn2+ nano-oxides into cancer cells in anticancer activity without UV light. The anticancer activity under UV light was augmented, which was attributed to an increase in ROS generation caused by the increased dose of these CuO and CuO:Zn2+ compounds. As a result, these CuO and CuO:Zn2+ can potentially be used as drug delivery systems, and their low toxicity and therapeutic properties make them suitable for use as photosensitizers on MCF-7 cells when exposed to UV radiation.