This review examines the pharmacological properties and therapeutic possibilities of α-asarone, a phenylpropene compound derived from Acorus calamus Linn. (sweet flag), a plant widely utilized in traditional medicine. α-Asarone, represented by the chemical formula C12H16O3, demonstrates a wide range of pharmacological effects, such as neuroprotection, hepatoprotection, nephroprotection, analgesia, antidepressant, anticancer, antimicrobial, anticholinesterase, antidiabetic, anti-inflammatory, antioxidant, and immunomodulatory activities. The main cause of these effects is mainly due to the antioxidant characteristics of α-asarone and its capacity to regulate several metabolic pathways. α-asarone has exhibited notable neuroprotective benefits through the reduction of oxidative stress and inhibition of N-methyl-D-aspartate (NMDA) receptor activity. Additionally, it has demonstrated hepatoprotective and nephroprotective capabilities, effectively mitigating acetaminophen-induced damage. Furthermore, α-asarone shows promise in the therapy of cancer by controlling the growth and death of cells. Furthermore, its ability to reduce inflammation, fight against microorganisms, and regulate blood sugar levels emphasizes its wide range of therapeutic benefits. The results indicate that α-asarone, obtained from Acorus calamus, shows great potential as a natural remedy for several human conditions.