Dioscin has gained immense popularity as a natural, bioactive steroid saponin, which offers numerous medical benefits. The growing global incidence of disease-associated morbidity and mortality continues to compromise human health, facilitating an increasingly urgent need for nontoxic, noninvasive, and efficient treatment alternatives. Natural compounds can contribute vastly to this field. Over recent years, studies have demonstrated the remarkable protective actions of dioscin against a variety of human malignancies, metabolic disorders, organ injuries, and viral/fungal infections. The successful usage of this phytocompound has been widely seen in medical treatment procedures under traditional Chinese medicine, and it is becoming progressively prevalent worldwide. This review provides an insight into the wide spectrum of pharmacological activities of dioscin, as reported and compiled in recent literature. The various novel approaches and applications of dioscin also verify the advantages exhibited by plant extracts against commercially available drugs, highlighting the potential of phytochemical agents like dioscin to be further incorporated into clinical practice.