Abstract: Tigliane-type diterpenoids are the main active components of croton and a diverse group of macrocyclic diterpenes with diverse biological activities. Their anti-HIV activity have unique advantages and great potential in the treatment of acquired immunodeficiency syndrome (AIDS), and were expected to be developed as a candidate drug for clinical trials of anti-AIDS. This article reviews the research progress on the components of tigliane-type diterpenoids in croton and their anti-HIV activity in recent years, conducts systematic comparisons, summarizes the currently discovered tigliane-type diterpenoids in croton. Their chemical structures and biological activity relationship were summarized. The research progress on the mechanism of tigliane-type diterpenoids' anti-HIV activity was briefly discussed. This research could provide guidance for further development and utilization of coumarin type diterpenes, as well as new ideas for the application of croton.