Bioactivities and Structure‐Activity Relationships of Harmine and Its Derivatives: A Review

Natural products and their derivatives play a crucial role in treating various diseases. Harmine, a tricyclic β‐carboline alkaloid sourced from the seeds of Peganum harmala L., has been explored as a candidate molecule for a variety of diseases due to its diverse bioactivities. In recent years, harmine derivatives have demonstrated even more significant therapeutic potential. To assess the current research landscape on harmine and its derivatives, we examined the studies published between 2019 and 2024 in the scientific databases, such as PubMed, Web of Science, and Google Scholar. In this review, the possible applications of harmine and its derivatives were systematically illustrated, including biological activities, structure‐activity relationships, and nanotechnology applications. Notably, the biological activities of harmine and its derivatives mainly contained anti‐tumor, neuroprotective, anti‐parasitic, anti‐inflammatory, and anti‐diabetic properties. Additionally, structural modifications and the application of nanocarriers make harmine and its derivatives more druggable. The aim of this review is to summarize the recent advancements in harmine and its derivatives research, analyze emerging trends, and explore their clinical value.