The use of biofertilizers in developing environmentally friendly agriculture as an alternative to chemical‐based fertilizers in enhancing food production is promising in sustainable agriculture for the improvement in the yield of some commercial crops such as sunflowers and other oilseed crops in terms of quality and quantity. Sunflower is an important oilseed crop native to South America and currently cultivated throughout the world. Generally, the sunflower is considered important based on its nutritional and medicinal value. Due to its beneficial health effects, sunflower has been recognized as functional foods or nutraceutical, although not yet fully harnessed. Sunflower contains mineral elements and phytochemicals such as dietary fiber, manganese, vitamins, tocopherols, phytosterols, triterpene glycosides, α‐tocopherol, glutathione reductase, flavonoids, phenolic acids, carotenoids, peptides, chlorogenic acid, caffeic acid, alkaloids, tannins, and saponins; and these compounds contribute to their functional and nutraceutical development. The extract from sunflower is known to be a potential source of antimicrobial, anti‐inflammatory, antitumor, and antioxidants agents that protect human cells against harmful reactive oxygen molecules and pathogenic microorganisms. Also, the pharmacological survey on sunflower had revealed its curative power to different kinds of diseases. The health benefits of sunflower include blood pressure and diabetic control, skin protection, and lowering cholesterol and other functions. This review is written with appropriate referencing to previously published work and provides updated information regarding the new method of organic farming for sunflower production, nutritional and health benefits, and its by‐products as human diet and livestock feed. Also, the constraints of sunflower production are elucidated.