As a naturally occurring furanocoumarin, the medicinal value of imperatorin has been studied more and more. We hope to provide useful information for the further development of imperatorin by analyzing the literature of imperatorin in recent years. By collating the literature on the pharmacology of imperatorin, we found that the pharmacological activity of imperatorin is wide and imperatorin can be used for anti-cancer, neuroprotection, anti-inflammatory, anti-hypertension and antibacterial. In addition, we found that some researchers confirmed the toxicity of imperatorin. Pharmacokinetic studies demonstrated that oxidation metabolism is the main metabolic pathways of imperatorin. At present, the shortcomings of research on imperatorin mainly include: most pharmacological studies are concentrated in vitro, lacking enough in vivo experimental data; more and more studies showed that imperatorin has synergistic effect with other drugs in anticancer and other aspects, but lacking the detailed explanation of the mechanism of the synergistic effect; imperatorin has side effect, but it lacks enough experimental conclusions. Based on the above defects, we believe that more in vivo experiments of imperatorin should be carried out in the future; future research need to explore synergistic mechanisms of imperatorin with other drugs, especially in anticancer; the dose affects both the pharmacological activity and the side effect of imperatorin. The relationship between the dose and the two aspects need to be further studied in order to reduce the side effect. In addition, through structural modification of imperatorin, it is possible to improve the treatment effect and reduce side effect.Copyright © 2020. Published by Elsevier B.V.