Aim: Melatonin (MLT) is a major hormone secreted by the pineal gland. In this study, a gold(III) MLT (Au⁺³/MLT) complex has been synthesized and investigating its protective effects against testicular damage. Methodology: The structural features of the complex were investigated. For biological assessment, 30 male rats were divided into three groups for 30 days. The first control group, the second received MLT and the third received Au⁺³/MLT complex. Results: The Au⁺³/MLT complex was found to be nonelectrolytic with formula (Au[MLT]₂[Cl][H₂O]). The ligand is monodentate and adopt square-planar geometry. Its particles range in diameter from 35 to 100 nm. MLT affords slight oxidative stress protection. The Au⁺³/MLT complex significantly decreases TNF-α and IL-1β levels but elevates antioxidant enzyme capacities, reducing lipid peroxidation markers and improving testicular histological structure. Conclusion: The Au⁺³/MLT complex improves the anti-inflammatory actions of MLT, exhibits potent antioxidant activity and enhances reproductive capacity.