Alkamides in Asteraceae Family: Bioactivity and Structural Relationships

Abstract

Introduction: Plants from the Family Asteraceae are rich in nutraceuticals, mainly diterpenoids, alkamides, flavonoids, and polyphenols that possess a variety of pharmacological activities, such as antitumor, insecticidal, antibacterial, anti-inflammatory, and antifungal. This article seeks to highlight the importance of alkamides found in this Family to assist researchers working on drug development based on alkamides. Methods: This article is the first study performing an exhaustive review of literature for data published in 1980-2025, related to the phytochemistry, distribution, biological activities, and structure- activity relationships of alkamides from the Family Asteraceae. Results: The results revealed that Artemisia, Echinaceae, Acmella, Anacyclus, Heliopsis, Wedelia, and Spilanthes are the major genera belonging to the Asteraceae family that produce alkamides including olefinic alkamides, such as spilanthol and affinin; polyunsaturated alkamides, exemplified by dodeca-2E,4E,8Z,10E-tetraenamides and related polyene isobutylamides found in Echinacea species; acetylenic alkamides, reported in Echinacea and Heliopsis; saturated alkamides, such as N-isobutyl decanamide. Discussion: The documented biological activities include notable anti-inflammatory effects by the inhibition of pro-inflammatory mediators like TNF-α. Several alkamides also demonstrate anticancer potential by triggering apoptotic pathways in various tumor cell lines. In addition, these compounds show analgesic properties through modulation of TRPV1-related mechanisms, exhibit neuroprotective effects by limiting oxidative injury, and contribute antioxidant benefits. An important observation is their structural similarity to anandamide, which allows them to interact effectively with CB2 receptors and may account for their immunomodulatory and antiinflammatory actions. Collectively, these characteristics position alkamides as promising starting points for the development of non-psychoactive cannabinoid-inspired analgesics, antiinflammatory therapeutics, immune regulatory agents, and supportive anticancer formulations. Conclusion: Moreover, the evaluation of structure-activity relationship studies related to these bioactive compounds, and the biosynthesis pathways of Asteraceae-specific alkamides have revealed various mechanisms of action that could be useful in novel drug discovery. However, future studies should be performed for further exploration of their pharmacokinetics and safety.