ABSTRACT Interest in plant‐derived bioactive peptides (BAPs) is increasing due to their potential therapeutic effects, low toxicity, abundance, scalability, and cost‐effectiveness. These peptides can be obtained by hydrolyzing plant proteins from a diverse range of sources, including legumes, cereals, grains, oilseeds, and tubers. This review discusses the benefits of these peptides on human health, addressing current challenges in translating research into practical use. The structural aspects of peptides combating hypertension and diabetes, encompassing structure–activity relationship studies, in vitro and in vivo methodologies, and absorption pathways are also discussed. Additionally, it explores the molecular features, physicochemical properties, gastrointestinal fate, and biological activities of various plant‐derived peptides, including their potential in reducing blood pressure and blood sugar. These peptides hold promise as therapeutic agents in functional foods, supplements, and pharmaceuticals, pending rigorous human clinical trials to ascertain efficacy and safety. Successful trials could position plant‐derived peptides as innovative antihypertensive and antidiabetic agents.