The genus Tilia contains is mainly distributed in subtropical and north temperate zones. The species of the genus have a long history of traditional uses in China and abroad. This paper summarize the research progress on chemical constituents and pharmacological effects of Tilia. The aim is to provide a certain scientific basis for clinical medicinal use of the Tilia species, and a reference for the effective development and rational utilization of the medicinal plant resources of the genus. The main active ingredients in the genus species include flavonoids, phenylpropanoids, alkaloids, terpenoids, essential oils, steroids and glycosides. They exhibit diverse activities including anti-inflammatory, analgesic, neuroprotective, anxiolytic and immunomodulatory effects.