Curcumin is recognized as an important natural biomaterial which has a wide range of biological importance, unfortunately it lacks in bioavailability predominantly due to its poor aqueous solubility. The intention of the present investigation was to develop a novel nanocomposite of curcumin with ZnO nanoparticle in order to improve its aqueous-phase solubility and develop its efficiency on microbes and cancer cells. Therefore, we have constructed an aqueous solvable curcumin/ZnO nanocomposite from the insoluble commercial curcumin and poorly soluble ZnO nanoparticles, consequently enhancing its biological importance. The synthesized ZnO nanoparticles, nanocurcumin, and the nanocomposite were analyzed with transmission electron microscope (TEM), and X-ray diffraction (XRD) along with spectral techniques. The calculated average particle size of ZnO nanoparticle and nanocomposite from XRD was found to be 21.44 nm and 24.66 nm respectively. The TEM image reveals that this new nanocomposite was found to have narrow particle size of 53 nm. The observed results declared that the title nanomaterials showed excellent antibacterial activity against, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, and Staphylococcus aureus. Their cytotoxicity performance against gastric cancer (AGS) cells was also carried out and observed that they showed concentration dependency. All the observed results declared that it has great potential for antibacterial and anticancer applications. The observed results of this investigation demonstrate that the present nano-conjugate can effectively deliver the antibacterial, anticancer drug curcumin towards the targeted biomolecules and hence appears to be a promising nano-formulation for chemotherapy and other biomedical applications after a series of in-vivo tests on animal models.