Bupleurum has been used as traditional medicine in China, Japan, South Korea, and other Asian countries for more than 2,000 years. The crude extracts and pure compounds isolated from Bupleurum have a variety of biological activities, such as anti-inflammatory, anti-cancer, antipyretic, antibacterial, anti-viral, liver protection, neuroprotection, and immune regulation. The pharmacological effects of Bupleurum have been classified and summarized in this paper by consulting literatures at home and abroad. At the same time, the quality analysis methods of bupleurum, including high-performance liquid chromatography, thin layer chromatography, ultra-high-performance liquid chromatography mass spectrometry, UPLC-QTOF-MS, and so on, are discussed. This paper provides a reference for further research, development, and application of Bupleurum.