Natural drug research is one of the main directions for the discovery and development of new drugs. Underutilized vegetables with a rich source of medicinal value have drawn much attention from scientists in synthesizing new drugs and finding new pharmacological actions. Apigenin is a natural flavonoid with pharmacological effects including anti-inflammatory, anti-tumor, anti-oxidation, anti-radiation, antidepressant effect, cardiovascular protection, regulated glucose and lipid metabolism, protecting the kidneys, neuroprotection, antibacterial, etc. Thus, these pharmacological effects of apigenin and the interaction between apigenin and drugs were mainly reviewed in this paper. The pharmacological actions of apigenin are being elucidated not only on the molecular level but also on the apigenin-receptor interaction, changes in factors, enzymes, proteins, cells, or tissues. The apigenin derivatives and complexes with their pharmacological actions were also summarized, which is expected to provide a reference for the rational development and utilization of apigenin.