This review aims to systematize and update current knowledge on Flourensia cernua, a native shrub from northern Mexico with remarkable ethnobotanical and biotechnological value. Unlike previous reviews that have mainly focused on traditional uses, this manuscript integrates recent evidence on its phytochemical composition and biological activities, particularly its antioxidant, anti-inflammatory, antimicrobial, anticancer, and nutraceutical properties. The relevance of this review lies in bridging ancestral knowledge with modern scientific approaches, thus providing a broader understanding of the potential of F. cernua as a source of bioactive compounds. Recent advances in emerging technologies, such as ultrasound-assisted extraction, solid-state fermentation, and microencapsulation, have enabled the efficient recovery of metabolites like apigenin, quercetin, and kaempferol, improving their stability, bioavailability, and functional activity. These compounds have demonstrated therapeutic effects in both vitro and vivo models, supporting their potential application in the development of dietary supplements, functional foods and phytopharmaceuticals. Additionally, evidence suggests that extracts from F. cernua may be employed as natural preservatives and anti-fungal agents in the food industry, as well as in a sustainable agricultural practice, positioning this species as a multifunctional resource with broad economic and ecological implications. Its resilience in arid ecosystems further highlights its role as a strategic plant for sustainable innovation and biodiversity conservation. Taken together, this review highlights F. cernua as a promising candidate for the development of nutraceuticals, natural preservatives, and agro-biotechnological products aligned with the sustainable development goals. Its study not only contributes to public health by offering safe and natural alternatives but also supports conservation of biodiversity and fosters sustainable innovation in arid and semi-arid regions.