Abstract: Neohesperidin dihydrochalcone (NHDC) is a sweetener with non-toxic, highly sweet and low-calorie characteristics. It has abilities of adding sweetness, adding fragrance and masking the bitterness, together with modifying flavours, as well as pharmacological activities such as antioxidant, anti-inflammatory, hypolipidemic and has potential for development in the fields of food and pharmaceutical. NHDC is usually obtained by hydrogenated reduction of neohesperidin (NHP) after hydrolysis under alkaline conditions, while neohesperidin is synthesized from hesperidin (HSD) and naringenin (NRG), they are called as synthesis precursors of NHDC. The synthetic precursors of NHDC have various biological activities, including antioxidant, liver and kidney protection, antibacterial and improving gastrointestinal function, etc. The pharmacological effects of NHDC are characterized by slow development process, lack of research systems and lack of depth of mechanisms compared to other dihydrochalcone compounds. In this paper, we searches the scientific databases including SciFinder, Web of Science and CNKI with the keywords of NHDC and its synthetic precursors, and reads its relevant literature. The pharmacological activity is systematically discussed and synthetic precursors mechanism is summarized for the NHDC, which will provide reference for the further utilization and development of NHDC and produce high value-added products in future.