Asarone, a phytochemical compound prevalent in various plant species such as Acorus and Guatteria gaumeri Greenman, has emerged as a subject of extensive scientific investigation. Its two primary isomeric forms, alpha and beta asarone, have been the focus of numerous studies due to their diverse pharmacological activities. These activities encompass a wide range of therapeutic potentials, including antidepressant, anxiolytic, anti-Alzheimer's, anti-Parkinson's, antiepileptic, anticancer, antihyperlipidemic, antithrombotic, anticholestatic, and radioprotective effects. The mechanisms underlying these pharmacological actions involve the modulation of various molecular targets within the central nervous system, cardiovascular system, and other physiological pathways. While the pharmacological properties of asarone compounds offer considerable therapeutic promise, it is essential to consider their potential adverse effects. Toxicological studies have revealed concerns regarding the mutagenic, genotoxic, and teratogenic properties of both alpha and beta asarone. These findings underscore the importance of cautious evaluation and monitoring when considering the therapeutic application of these compounds. In summary, this comprehensive review provides valuable insights of pharmacological profiles of alpha and beta asarone. By elucidating their mechanisms of action, metabolic pathways, and potential risks, this body of knowledge serves as a foundation for further research aimed at harnessing the therapeutic benefits of asarone compounds while mitigating their associated risks.