In the recent years, due to the increasing resistance of pathogens to synthetic antimicrobial drugs, the use of highly active compounds from plants, which have proven their effectiveness in traditional medicine practices, is increased. Extracts of medicinal plants often contain a unique species ‒ specific combination of active ingredients that have a synergistic therapeutic effect. Therefore, the analysis of the biochemical composition of cultivated plants and the range of their potential biotechnological application is an urgent task. Aim. To summarize the information on the potential of the xerophytic plant Tetragonia tetragonioides as a source of functional food ingredients and biologically active substances that increase nonspecific organism resistance and contribute to the prevention and treatment of various diseases. Results. T. tetragonioides is a salt-tolerant and heat-resistant plant containing valuable nutrients and biologically active substances, a significant amount of vitamins, minerals, and dietary fibers. The high level of antioxidant compounds, especially flavonoids and carotenoids, helps to reduce the risk of degenerative pathologies developing associated with excessive oxidative stress. The unique complex of biologically active substances in T. tetragonioides, which includes 6-methoxyflavonols, predominantly derivatives of 6-methoxykaempferol, as well as megastigmanes and their glucosides, lignanamide, provides significant antioxidant, anti-inflammatory, antitumor, and antimicrobial activity and may be beneficial for the prevention of chronic diseases and age-related health problems. The effectiveness of T. tetragonioides has been demonstrated in animal models in the treatment of metabolic disorders such as obesity, hyperlipidemia, and hyperuricemia. Conclusions. T. tetragonioides, containing a specific complex of biologically active compounds, primarily 6-methoxyflavonols, may be a promising raw material for obtaining effective medications for the treatment and prevention of various chronic diseases and metabolic disorders.