Broussonetia papyrifera has a wide distribution of resources in China and has received extensive attention at home and abroad due to its diverse uses. There are various chemical components such as flavonoids, terpenoids, coumarins, steroids, lignans, amino acids and volatile oils in the leaves of Broussonetia papyrifera. Its extracts or chemical components have various pharmacological effects such as anti-inflammation, anti-oxidation, diuresis, anti-cancer, and reducing fat accumulation. This article summarizes for the first time the research progress of chemical components and pharmacological activities of Broussonetia papyrifera leaves, in order to provide a basis for clinical medicine and at the same time provide a reference for the rational application and effective development of Broussonetia papyrifera leaves as a medicinal resource.