Quinoa, a globally cultivated “golden grain” belonging to Chenopodium in the Amaranthaceae family, is recognized for being gluten-free, with a balanced amino acid profile and multiple bioactive components, including peptides, polysaccharides, polyphenols, and saponins. The bioactive compounds extracted from quinoa offer multifaceted health benefits, including antioxidative, anti-inflammatory, antimicrobial, cardiovascular disease (CVD) improvement, gut microbiota regulation, and anti-cancer effects. This review aims to intricately outline quinoa’s nutritional value, functional components, and physiological benefits. Importantly, we comprehensively provide conclusions on the effects and mechanisms of these quinoa-derived bioactive components on multiple cancer types, revealing the potential of quinoa seeds as promising and effective anti-cancer agents. Furthermore, the health-promoting role of quinoa in modulating gut microbiota, maintaining gut homeostasis, and protecting intestinal integrity was specifically emphasized. Finally, we provided a forward-looking description of the opportunities and challenges for the future exploration of quinoa. However, in-depth studies of molecular targets and clinical trials are warranted to fully understand the bioavailability and therapeutic application of quinoa-derived compounds, especially in cancer treatment and gut microbiota regulation. This review sheds light on the prospect of developing dietary quinoa into functional foods or drugs to prevent and manage human diseases.