Acmella oleracea (L.) R. K. Jansen (Asteraceae), commonly known as the "toothache plant" or "jambu," is a significant medicinal plant that has been traditionally used in Brazil and other tropical and subtropical regions for relieving dental pain, as an anti-inflammatory agent, and as a culinary spice. Due to its versatile utility, this plant has been extensively studied in modern medicine and pharmacy for its diverse pharmacological properties, including anesthetic, analgesic, anti-inflammatory, antioxidant, and antimicrobial activities. Analytical research on the chemical compositions responsible for these activities has led to the identification of approximately 120 secondary metabolites. These findings provide scientific validation for its traditional uses and have spurred research into the development of ingredients for functional foods and cosmetics. This review incorporates the latest research findings, focusing on biological activities and compounds that have been practically isolated or can be isolated based on quantitative experimental data, to serve as a practical reference for industrial development. Furthermore, factors influencing the content of alkylamides and phenolic compounds, two major bioactive groups, are summarized to support material development. Ultimately, this review aims to provide a clearer understanding of the plant’s utility and contribute to the development of products that enhance human health.