Abstract: Nuciferine is a key aporphine alkaloid in the dried leaves of Nelumbo nucifera Gaertn (LNNG), which is also the quality control component of LNNG in Chinese Pharmacopoeia. It is reported that nuciferine has many pharmacological effects, such as lipid-lowering, anti-hyperglycemia, anti-tumor, anti-cerebral ischemia, and has a broad development prospect. However, there are some medicinal defects, such as poor water solubility, lack of safety data, and controversy of bioavailability, which greatly affect the in-depth research and development of nuciferine. Therefore, how to choose the most suitable clinical indications from massive pharmacological activities, improve its solubility and bioavailability through preparation or chemical method, and reduce the occurrence of toxic and side effects, are urgent to be solved. In this paper, the physicochemical property, pharmacokinetic characteristics, pharmacological activity and underling mechanism of nuciferine were systematically summarized, which can be helpful for the further study of its pharmacological action and the development of innovative products.