Regaloside A is a bioactive natural compound primarily studied for its anti-inflammatory, antioxidant, and neuroprotective effects. It modulates pathways involved in oxidative stress and neuronal damage, showing promise in research on neurodegenerative conditions such as Alzheimer’s and Parkinson’s diseases. Additionally, it exhibits immunomodulatory properties, with potential applications in managing autoimmune disorders, chronic inflammation, and diseases like arthritis. Preliminary studies also indicate anti-cancer activity at the cellular level, where it may inhibit the growth of certain cancer cells. Its bioactive nature supports use in cosmetic formulations for skin protection and anti-aging, helping to reduce inflammation and enhance cellular defense mechanisms. Most applications remain in the preclinical research stage, focusing on pharmacological development, mechanism validation, and future drug development.