Sesame seeds (Sesamum indicum L.) are a nutrient-rich superfood with significant health benefits. They are a source of various bioactive compounds, including lignans, tocopherols, phytosterols, and polyunsaturated fatty acids (PUFAs), which contribute to cardiovascular health, cancer prevention, and neuroprotection. Sesame seeds contain 45–65% oil, 19–35% protein, and essential nutrients like calcium, iron, magnesium, and zinc. They also contain antioxidants, dietary fiber, and phytochemicals that help reduce oxidative stress and inflammation. Sesamol, sesamin, and sesamolin are key lignans with antioxidant and anti-inflammatory properties, while tocopherols (vitamin E) and tocotrienols provide additional antioxidant benefits. Phytosterols help lower cholesterol levels by competing with cholesterol absorption in the gut. Sesame oil, derived from sesame seeds, is rich in these compounds and has been shown to improve lipid metabolism and reduce the risk of chronic diseases. However, the balance of n-3 and n-6 fatty acids in sesame seed oil is important for overall health. Processing methods can influence the bioavailability of these compounds, with roasting enhancing antioxidant properties. Sesame seeds have applications in food, pharmaceuticals, and cosmetics. Research highlights their potential as a natural source of beneficial compounds for disease prevention and treatment. The review emphasizes the importance of further studies to fully understand the health benefits and optimal use of sesame seeds and their derivatives.Sesame seeds (Sesamum indicum L.) are a nutrient-rich superfood with significant health benefits. They are a source of various bioactive compounds, including lignans, tocopherols, phytosterols, and polyunsaturated fatty acids (PUFAs), which contribute to cardiovascular health, cancer prevention, and neuroprotection. Sesame seeds contain 45–65% oil, 19–35% protein, and essential nutrients like calcium, iron, magnesium, and zinc. They also contain antioxidants, dietary fiber, and phytochemicals that help reduce oxidative stress and inflammation. Sesamol, sesamin, and sesamolin are key lignans with antioxidant and anti-inflammatory properties, while tocopherols (vitamin E) and tocotrienols provide additional antioxidant benefits. Phytosterols help lower cholesterol levels by competing with cholesterol absorption in the gut. Sesame oil, derived from sesame seeds, is rich in these compounds and has been shown to improve lipid metabolism and reduce the risk of chronic diseases. However, the balance of n-3 and n-6 fatty acids in sesame seed oil is important for overall health. Processing methods can influence the bioavailability of these compounds, with roasting enhancing antioxidant properties. Sesame seeds have applications in food, pharmaceuticals, and cosmetics. Research highlights their potential as a natural source of beneficial compounds for disease prevention and treatment. The review emphasizes the importance of further studies to fully understand the health benefits and optimal use of sesame seeds and their derivatives.