Black sesame, as a kind of “medicine and food homologous” ingredient,has been regarded as a good health care product since ancient times, and its nutritional and health value is well known. Black sesame which is rich in proteins, minerals, unsaturated fatty acids, vitamins, lignin substances and melanin, has unique nutritional and healthy functions and medical prevention functions. Through the specific cases, this review briefly described the typical functional components of black sesame and their corresponding common mechanisms, and illustrated the structure activity relationship between the typical functional components and healthcare functions, such as the effect of melanin on hair growth, sesamin on anti-oxidation, lowering cholesterol, reducing blood sugar, blood fat reduction, anti-cancer, anti-tumor, microelements on anemia treatment, and dental care, respectively. Furthermore, this work demonstrated the research trend and hot spots of the structure-activity relationship of black sesame functional ingredients. It put forward the research trend of simplification and refinement of the functional ingredients of black sesame, and proposed to establish a health information database of black sesame functional ingredients, aiming to provide an important scientific basis for further development of new black sesame functional products.