After wheat, rice, maize, and barley, sorghum is the fifth most widely grown cereal on the planet. Due to its high production, drought resistance, and heat tolerance, this crop is replacing maize in some areas. Sorghum is available in a variety of colors, including cream, lemon-yellow, red, and even black. The principal grain anatomical components are pericarp, germ or embryo and endosperm. This review provides an overview of key sorghum grain components, including starches, fiber, proteins, lipids, and vitamins. Also, we summarized phenolic compounds, flavonoids, tannins, carotenoids, vitamin E, amines, Policosanols and Phytosterols in sorghum grains. Sorghum is used to manufacture bread and porridge, and it provides a significant source of energy and nutrition for humans; sorghum is extensively farmed for animal feed. However, because the natural components in sorghum are useful in the development of healthy and functional foods, sorghum farming for both biofuel production and human consumption is gaining popularity. Pigmented sorghum grain is high in antioxidants such as polyphenols, primarily tannins, which have a variety of health benefits, including antiproliferative properties linked to the prevention of certain cancers, antioxidant activities linked to the prevention of diseases linked to oxidative stress, and anti-inflammatory effects, as well as improving glucose metabolism. Because these chemicals cannot be assimilated, their application in the food business has been limited, as sorghum is regarded as a lownutritional grain due to the presence of anti-nutritional components such as strong tannins, which form complexes with proteins and iron, limiting their digestibility. This review aims to show the utilization of sorghum as a source of bioactive chemicals and the value they bestow on human health due to the general biological potential it possesses.